Lapatinib

別名：GSK572016, GW2016

製品コード：S2111 純度：99.95%

Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

CAS No. 231277-92-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
25mg	JPY 22000	国内在庫あり
100mg	JPY 40500	国内在庫あり
1g	JPY 145500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（473）

製品安全説明書

現在のバッチを見る：純度： 99.95%

99.95

Lapatinib関連製品

関連ターゲット	EGFR/ErbB1 HER2/ErbB2 ErbB3 ErbB4 mutant EGFR	もっと見る
関連製品	AG-490 AG-1478 Canertinib (CI-1033) Rociletinib (CO-1686) WZ4002 Genistein Poziotinib PD153035 PD153035 HCl Allitinib tosylate AEE788 (NVP-AEE788) Pelitinib (EKB-569) Canertinib dihydrochloride Varlitinib Icotinib (BPI-2009H) Nazartinib (EGF816) NSC228155 PD168393 Olmutinib (BI 1482694) Zorifertinib (AZD3759) AZ5104 Lazertinib CL-387785 (EKI-785) TAK-285 Daphnetin Pyrotinib dimaleate Alflutinib (Furmonertinib) mesylate EGFR Inhibitor Chrysophanic Acid Norcantharidin WZ8040 Butein Cyasterone Avitinib (Abivertinib) CNX-2006 MTX-211 Naquotinib(ASP8273) Tuxobertinib (BDTX-189) WZ3146 Sunvozertinib (DZD9008) Tyrphostin 9 EAI045 zipalertinib (TAS6417) Almonertinib (HS-10296) AG-18	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Cell Cycle compound library Angiogenesis Related compound Library	もっと見る

シグナル伝達経路

EGFRシグナル伝達経路

EGFR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
A431	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
A431	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
BT474	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
BT474	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
A431	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER1 phosphorylation (unknown origin) expressed in human A431 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
BT474	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER2 phosphorylation (unknown origin) expressed in human BT474 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
MCF7	Function assay	10 uM	2 hrs	Inhibition of HER2 delta16 mutant autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2delta16 at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2 at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting	24355130
A549	Function assay	50 uM	2 hrs	Inhibition of EGFR phosphorylation at Y1068 in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method	28238614
A549	Function assay	50 uM	2 hrs	Inhibition of EGFR phosphorylation at Tyr residue in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method	28238614
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50 = 0.011 μM.	25151582
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.017 μM.	19028425
BT474	Antiproliferative assay		72 hrs	Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method, IC50 = 0.025 μM.	21887403
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.029 μM.	19888761
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay, IC50 = 0.029 μM.	22372864
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0301 μM.	25305330
BT474	Cytotoxicity assay		72 hrs	Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay, IC50 = 0.031 μM.	27288180
CAL27	Function assay		16 hrs	Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot, IC50 = 0.032 μM.	21080629
NCI-N87	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay, IC50 = 0.036 μM.	22372864
insect cells	Function assay		5 mins	Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.03755 μM.	30096580
MDA-MB-175	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-175 cells expressing Src, Ret and low HER-2 after 72 hrs by SRB assay, IC50 = 0.0444 μM.	22372864
SK-BR-3	Antiproliferative assay		48 hrs	Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.06 μM.	27769671
BT474	Cytotoxicity assay		72 hrs	Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0639 μM.	25305330
NCI-N87	Antiproliferative assay		3 days	Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining, IC50 = 0.09 μM.	22101132
BT474	Antiproliferative assay		3 days	Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining, IC50 = 0.1 μM.	22101132
Calu3	Antiproliferative assay		72 hrs	Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay, IC50 = 0.1 μM.	28092860
BT474	Cytotoxicity assay		48 hrs	Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.1 μM.	27769671
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.104 μM.	19888761
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay, IC50 = 0.104 μM.	22372864
HeLa	Antiproliferative assay		12 hrs	Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay, IC50 = 0.12 μM.	26652482
A431	Antiproliferative assay		48 hrs	Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.15 μM.	27769671
MDA-MB-453	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.19 μM.	25305330
BT474	Cytotoxicity assay		72 hrs	Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 0.2 μM.	29089259
B16F10	Antiproliferative assay		12 hrs	Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay, IC50 = 0.21 μM.	26652482
Sf21	Function assay		5 mins	Inhibition of N-terminal GST-tagged recombinant human EGFR T790M mutant expressed in baculovirus infected Sf21 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.22489 μM.	30096580
Calu3	Cytotoxicity assay		72 hrs	Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.23 μM.	25305330
DIFI	Cytotoxicity assay		4 days	Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.235 μM.	22169601
HepG2	Antiproliferative assay		12 hrs	Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay, IC50 = 0.27 μM.	26652482
EOL-1	Cytotoxicity assay		72 hrs	Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 0.41 μM.	29089259
MCF7	Antiproliferative assay		12 hrs	Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay, IC50 = 0.47 μM.	26652482
SKBR3	Antiproliferative assay		48 hrs	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay, IC50 = 0.49 μM.	27187856
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.51 μM.	27769671
CAL27	Cytotoxicity assay		4 days	Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.53 μM.	22169601
MDA-MB-453	Cytotoxicity assay		72 hrs	Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay, IC50 = 0.555 μM.	22372864
SKOV3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.59 μM.	25305330
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay, IC50 = 0.6 μM.	29421573
A431NS	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431NS cells after 72 hrs by MTT assay, IC50 = 0.6 μM.	28092860
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.6431 μM.	25305330
BT474	Cytotoxicity assay		72 hrs	Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay, GI50 = 0.93 μM.	26475520
MDA-MB-361	Cytotoxicity assay		72 hrs	Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay, IC50 = 1.029 μM.	22372864
GXF251L	Cytotoxicity assay		4 days	Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 1.48 μM.	22169601
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.6 μM.	22595177
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.62 μM.	22182581
LXFA 629L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.87 μM.	22169601
DU145	Cytotoxicity assay		4 days	Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.99 μM.	22169601
SKOV3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay, IC50 = 2.99 μM.	22182581
NCI-H1781	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H1781 cells expressing HER-2 G776insV_G/C after 72 hrs by SRB assay, IC50 = 3.047 μM.	22372864
OVXF 899L	Cytotoxicity assay		4 days	Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.35 μM.	22169601
LXFL 529L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFL 529L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.51 μM.	22169601
LNCAP	Cytotoxicity assay		4 days	Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.68 μM.	22169601
Bel7402	Antiproliferative assay		72 hrs	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50 = 3.7 μM.	28092860
LXFA 526L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFA 526L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.21 μM.	22169601
NIH/3T3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay, IC50 = 4.3 μM.	22595177
UXF 1138L	Cytotoxicity assay		4 days	Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.4 μM.	22169601
SK-BR-3	Antiproliferative assay		72 hrs	Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay, IC50 = 4.4 μM.	28092860
PC3M	Cytotoxicity assay		4 days	Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.55 μM.	22169601
COLO205	Antiproliferative assay		72 hrs	Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay, IC50 = 4.6 μM.	28092860
HT-29	Cytotoxicity assay		4 days	Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.62 μM.	22169601
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM.	29421573
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM.	28711703
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 4.8 μM.	28238614
MCF7	Cytotoxicity assay		4 days	Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.83 μM.	22169601
MEXF 1341L	Cytotoxicity assay		4 days	Cytotoxicity against human MEXF 1341L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.85 μM.	22169601
MCF7	Cytotoxicity assay		24 hrs	Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay, IC50 = 5.02 μM.	30096580
SKBR3	Antiproliferative assay		72 hrs	Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay, IC50 = 5.05 μM.	23927972
SKHEP1	Antiproliferative assay		hrs	Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50 = 5.3 μM.	20143778
RKO	Cytotoxicity assay		4 days	Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.35 μM.	22169601
MDA-MB-231	Antiproliferative assay		hrs	Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay, IC50 = 5.4 μM.	20143778
Hep3B2	Antiproliferative assay		hrs	Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay, IC50 = 5.49 μM.	20143778
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 5.7 μM.	29089259
LXFA 289L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.79 μM.	22169601
MAXF 401NL	Cytotoxicity assay		4 days	Cytotoxicity against human MAXF 401NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.8 μM.	22169601
HCT116	Cytotoxicity assay		24 hrs	Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay, IC50 = 5.92 μM.	30096580
22Rv1	Cytotoxicity assay		4 days	Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.06 μM.	22169601
PAXF 546L	Cytotoxicity assay		4 days	Cytotoxicity against human PAXF 546L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.12 μM.	22169601
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 6.2 μM.	28092860
NCI-H522	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay, IC50 = 6.4 μM.	28092860
MCF7	Antiproliferative assay		hrs	Antiproliferative activity against human MCF7 cells after hrs by ATP content assay, IC50 = 6.6 μM.	20143778
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 6.74 μM.	27187856
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.8 μM.	29684708
PXF 1118L	Cytotoxicity assay		4 days	Cytotoxicity against human PXF 1118L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.86 μM.	22169601
LIXF 575L	Cytotoxicity assay		4 days	Cytotoxicity against human LIXF 575L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.18 μM.	22169601
RXF 1781L	Cytotoxicity assay		4 days	Cytotoxicity against human RXF 1781L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.67 μM.	22169601
MDA231	Cytotoxicity assay		4 days	Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.7 μM.	22169601
LXFL 1121L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFL 1121L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.73 μM.	22169601
RXF 393NL	Cytotoxicity assay		4 days	Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.77 μM.	22169601
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 8.1 μM.	29089259
PANC1	Cytotoxicity assay		4 days	Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.12 μM.	22169601
CXF 269L	Cytotoxicity assay		4 days	Cytotoxicity against human CXF 269L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.36 μM.	22169601
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 8.4 μM.	28092860
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 8.468 μM.	25305330
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50 = 9.08 μM.	28711703
NCI-H1975	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 9.08 μM.	28238614
RXF 486L	Cytotoxicity assay		4 days	Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.1 μM.	22169601
Saos2	Cytotoxicity assay		4 days	Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.38 μM.	22169601
PXF 1752L	Cytotoxicity assay		4 days	Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.46 μM.	22169601
PXF 698L	Cytotoxicity assay		4 days	Cytotoxicity against human PXF 698L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.49 μM.	22169601
BXF T24	Cytotoxicity assay		4 days	Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.65 μM.	22169601
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 10.12 μM.	29684708
MEXF 462NL	Cytotoxicity assay		4 days	Cytotoxicity against human MEXF 462NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.13 μM.	22169601
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50 = 10.4 μM.	29684708
TE671	Cytotoxicity assay		4 days	Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.95 μM.	22169601
RAW264.7	Antileishmanial assay		96 hrs	Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay, EC50 = 11 μM.	28337329
PAXF 1657L	Cytotoxicity assay		4 days	Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.11 μM.	22169601
MEXF 276L	Cytotoxicity assay		4 days	Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.37 μM.	22169601
MKN45	Cytotoxicity assay		4 days	Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.48 μM.	22169601
BXF 1352L	Cytotoxicity assay		4 days	Cytotoxicity against human BXF 1352L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.53 μM.	22169601
HepG2	Cytotoxicity assay		24 hrs	Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay, IC50 = 11.71 μM.	30096580
BXF 1218L	Cytotoxicity assay		4 days	Cytotoxicity against human BXF 1218L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.77 μM.	22169601
Caco	Cytotoxicity assay		24 hrs	Cytotoxicity against human Caco cells after 24 hrs by SRB assay, IC50 = 12.11 μM.	30096580
SW480	Antiproliferative assay		72 hrs	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM.	29421573
SW480	Antiproliferative assay		72 hrs	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM.	28711703
SW480	Cytotoxicity assay		72 hrs	Cytotoxicity against human SW480 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 12.58 μM.	28238614
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50 = 12.68 μM.	29421573
3T3	Antitrypanosomal assay		48 hrs	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay, EC50 = 13 μM.	28337329
HCT116	Cytotoxicity assay		4 days	Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.14 μM.	22169601
OVCAR3	Cytotoxicity assay		4 days	Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.44 μM.	22169601
H460	Cytotoxicity assay		4 days	Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.46 μM.	22169601
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50 = 14.9 μM.	29421573
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay, IC50 = 14.9 μM.	28711703
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 14.9 μM.	28238614
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 15.71 μM.	24355130
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 15.79 μM.	24355130
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 19.22 μM.	24355130
MDA-MB-468	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay, IC50 = 20 μM.	28092860
HCC827	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 22.3 μM.	29089259
ETK-1	Growth Inhibition Assay			IC50=10.623 μM	SANGER
IST-MES1	Growth Inhibition Assay			IC50=10.2565 μM	SANGER
TE-15	Growth Inhibition Assay			IC50=10.245 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=9.98291 μM	SANGER
HCC2998	Growth Inhibition Assay			IC50=9.96307 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=9.66287 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=9.5742 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=9.47395 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=9.11675 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=7.76159 μM	SANGER
D-502MG	Growth Inhibition Assay			IC50=7.48894 μM	SANGER
EVSA-T	Growth Inhibition Assay			IC50=7.42811 μM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=7.22744 μM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=7.07183 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=6.51682 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=6.43694 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=6.26561 μM	SANGER
NB5	Growth Inhibition Assay			IC50=6.21001 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=5.80046 μM	SANGER
COLO-668	Growth Inhibition Assay			IC50=5.72667 μM	SANGER
SW954	Growth Inhibition Assay			IC50=5.39245 μM	SANGER
SW962	Growth Inhibition Assay			IC50=5.02159 μM	SANGER
UACC-812	Growth Inhibition Assay			IC50=4.56153 μM	SANGER
TK10	Growth Inhibition Assay			IC50=4.16522 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=4.0373 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=3.55356 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=3.54501 μM	SANGER
DJM-1	Growth Inhibition Assay			IC50=3.46975 μM	SANGER
LS-513	Growth Inhibition Assay			IC50=3.40041 μM	SANGER
RL95-2	Growth Inhibition Assay			IC50=3.1567 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=2.0483 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=1.99199 μM	SANGER
A253	Growth Inhibition Assay			IC50=1.97335 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=1.55201 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=1.38244 μM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=1.36228 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=0.02544 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=0.05326 μM	SANGER
OCUB-M	Growth Inhibition Assay			IC50=0.0574 μM	SANGER
ECC12	Growth Inhibition Assay			IC50=0.09231 μM	SANGER
DSH1	Growth Inhibition Assay			IC50=0.09396 μM	SANGER
BT-474	Growth Inhibition Assay			IC50=0.21315 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=0.24654 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=0.44874 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=0.49057 μM	SANGER
A388	Growth Inhibition Assay			IC50=0.72258 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=0.74453 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=1.15403 μM	SANGER
RCC10RGB	Growth Inhibition Assay			IC50=10.961 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=11.7255 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=12.1712 μM	SANGER
SR	Growth Inhibition Assay			IC50=12.2064 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=12.8985 μM	SANGER
ES6	Growth Inhibition Assay			IC50=13.078 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=13.2577 μM	SANGER
D-392MG	Growth Inhibition Assay			IC50=13.6428 μM	SANGER
NB7	Growth Inhibition Assay			IC50=14.2374 μM	SANGER
SK-LMS-1	Growth Inhibition Assay			IC50=14.5145 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=14.7889 μM	SANGER
CA46	Growth Inhibition Assay			IC50=15.0586 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=15.1901 μM	SANGER
BC-1	Growth Inhibition Assay			IC50=15.3314 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=15.8173 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=16.0924 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=16.7313 μM	SANGER
LB647-SCLC	Growth Inhibition Assay			IC50=16.9372 μM	SANGER
NCI-H1694	Growth Inhibition Assay			IC50=17.1529 μM	SANGER
NCI-H322M	Growth Inhibition Assay			IC50=17.4366 μM	SANGER
ES7	Growth Inhibition Assay			IC50=18.3914 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=18.4386 μM	SANGER
SF268	Growth Inhibition Assay			IC50=18.7409 μM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=19.0742 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=20.2344 μM	SANGER
A101D	Growth Inhibition Assay			IC50=20.8587 μM	SANGER
MRK-nu-1	Growth Inhibition Assay			IC50=20.913 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=21.038 μM	SANGER
NALM-6	Growth Inhibition Assay			IC50=21.1967 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=21.4813 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=22.1402 μM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=22.2149 μM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=22.3965 μM	SANGER
SKM-1	Growth Inhibition Assay			IC50=22.7351 μM	SANGER
DMS-153	Growth Inhibition Assay			IC50=23.4204 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay			IC50=23.5452 μM	SANGER
LP-1	Growth Inhibition Assay			IC50=23.8097 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=24.292 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=25.2036 μM	SANGER
U-698-M	Growth Inhibition Assay			IC50=25.2503 μM	SANGER
HC-1	Growth Inhibition Assay			IC50=25.6418 μM	SANGER
HCC2157	Growth Inhibition Assay			IC50=25.673 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=26.273 μM	SANGER
LS-411N	Growth Inhibition Assay			IC50=26.3369 μM	SANGER
Becker	Growth Inhibition Assay			IC50=26.5181 μM	SANGER
NCI-H23	Growth Inhibition Assay			IC50=26.7575 μM	SANGER
IST-SL1	Growth Inhibition Assay			IC50=27.3867 μM	SANGER
MZ2-MEL	Growth Inhibition Assay			IC50=27.4566 μM	SANGER
RKO	Growth Inhibition Assay			IC50=28.1446 μM	SANGER
TE-441-T	Growth Inhibition Assay			IC50=28.789 μM	SANGER
EW-24	Growth Inhibition Assay			IC50=29.1259 μM	SANGER
no-10	Growth Inhibition Assay			IC50=29.1631 μM	SANGER
D-542MG	Growth Inhibition Assay			IC50=29.9221 μM	SANGER
ST486	Growth Inhibition Assay			IC50=30.6451 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=30.8057 μM	SANGER
ES8	Growth Inhibition Assay			IC50=31.5972 μM	SANGER
BL-41	Growth Inhibition Assay			IC50=32.1054 μM	SANGER
NB6	Growth Inhibition Assay			IC50=32.3855 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=32.4967 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=32.7751 μM	SANGER
MFH-ino	Growth Inhibition Assay			IC50=34.3224 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=34.6748 μM	SANGER
HUTU-80	Growth Inhibition Assay			IC50=35.3667 μM	SANGER
EB2	Growth Inhibition Assay			IC50=36.6189 μM	SANGER
L-540	Growth Inhibition Assay			IC50=37.2308 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=38.8846 μM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=39.9651 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=42.415 μM	SANGER
BC-3	Growth Inhibition Assay			IC50=45.4896 μM	SANGER
SJSA-1	Growth Inhibition Assay			IC50=45.5474 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=45.666 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=46.018 μM	SANGER
SKBR3	Cytotoxicity assay			Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.002 μM.	21080629
SKOV3	Cytotoxicity assay			Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.003 μM.	21080629
CAL27	Cytotoxicity assay			Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.007 μM.	21080629
4T1	Cytotoxicity assay			Cytotoxicity against mouse triple negative 4T1 cells, IC50 = 0.01037 μM.	24890652
MDA-MB-231	Cytotoxicity assay			Cytotoxicity against human triple negative MDA-MB-231 cells, IC50 = 0.02 μM.	24890652
BT474	Antiproliferative assay			Antiproliferative activity against human BT474 cells overexpressing ErB2, IC50 = 0.025 μM.	18653333
HEK293	Function assay			Inhibition of recombinant human C-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.02706 μM.	28711703
HEK293	Function assay			Inhibition of recombinant human N-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.0271 μM.	29421573
HepG2	Function assay			Inhibition of EGFR in human HepG2 cells, IC50 = 0.0271 μM.	30096580
MDA-MB-435	Cytotoxicity assay			Cytotoxicity against human MDA-MB-435 cells, IC50 = 0.0297 μM.	24890652
SK-BR-3	Antiproliferative assay			Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50 = 0.04 μM.	20143778
A431	Function assay			Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.052 μM.	20346655
MCF7	Cytotoxicity assay			Cytotoxicity against human ER-positive MCF7 cells, IC50 = 0.0649 μM.	24890652
MDA-MB-468	Cytotoxicity assay			Cytotoxicity against human triple negative MDA-MB-468 cells, IC50 = 0.0832 μM.	24890652
N87	Function assay			Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50 = 0.1 μM.	20346655
MIAPaCa	Function assay			Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.14 μM.	20817523
MIAPaCa	Function assay			Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.433 μM.	20817523
A431	Cytotoxicity assay			Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.97 μM.	21080629
SK-BR-3	Antiproliferative assay			Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay, IC50 = 4.35 μM.	21570843
HeLa	Cytotoxicity assay			Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 5.9 μM.	21080629
HepG2	Antiproliferative assay			Antiproliferative activity against human HepG2 cells after hrs by ATP content assay, IC50 = 6.27 μM.	20143778
HepG2	Cytotoxicity assay			Cytotoxicity against human HepG2 cells assessed as reduction in cell viability, TC50 = 6.27 μM.	29049963
HepG2	Cytotoxicity assay			Cytotoxicity against human HepG2 cells, TC50 = 6.3 μM.	30344906
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 8.5 μM.	21080629
MDA-MB-468	Antiproliferative assay			Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay, IC50 = 23.46 μM.	21570843
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 42.36 μM.	21570843
NCI-N87	Antitumor assay			Antitumor activity against human NCI-N87 cells xenografted in athymic mouse assessed as tumor growth inhibition at 20 mg/kg, po QD for 14 days measured after 19 days	22101132
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
NCI-H522	Antitumor assay			Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 100 mg/kg, ig administered once daily for 28 days relative to control	28092860
LLC	Antitumor assay			Antitumor activity against mouse LLC cells implanted in in C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, po qd for 14 days	27187856
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生物活性

製品説明

Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

Targets

ErbB2 ^[1] (Cell-free assay)	EGFR ^[1] (Cell-free assay)	ErbB4 ^[1] (Cell-free assay)
9.2 nM	10.8 nM	367 nM

In Vitro
In vitro	Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation. ^[1]
Kinase Assay	In vitro kinase assays
Kinase Assay	The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl₂, 10 μM ATP, 1 μCi of [γ³³P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.
細胞実験	細胞株	HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2 cells
	濃度	Dissolved in DMSO, final concentrations ~100 μM
	反応時間	72 hours
	実験の流れ	Cells are exposed to various concentrations of Lapatinib for 72 hours. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1		29799521
	Immunofluorescence	LC3 Vimentin / E-cadherin		26637440
	Growth inhibition assay	Cell viability (OE19) Cell viability (A431 cells)		25350844

In Vivo
In Vivo	Oral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner. ^[1]
動物実験	動物モデル	CD-1 nude female mice implanted s.c. with HN5 cells, and C.B-17 SCID female mice implanted s.c. with BT474 cells
	投与量	~100 mg/kg
	投与経路	Orally twice daily

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00455039	Withdrawn	Breast Cancer	University of New Mexico	July 31 2023	Phase 1\|Phase 2
NCT04608409	Active not recruiting	Ovarian Cancer	Frederick R. Ueland M.D.\|National Cancer Institute (NCI)\|University of Kentucky	March 17 2021	Phase 1
NCT03075995	Unknown status	Breast Cancer	Sun Yat-sen University	April 12 2017	Not Applicable
NCT02338245	Completed	Metastatic Breast Cancer	ASLAN Pharmaceuticals	December 29 2014	Phase 2
NCT02294786	Terminated	Cancer	Novartis Pharmaceuticals\|Novartis	December 17 2014	Phase 2
NCT02158507	Active not recruiting	Metastatic Triple Negative Breast Cancer	University of Alabama at Birmingham\|Breast Cancer Research Foundation of Alabama\|GlaxoSmithKline\|AbbVie	September 2014	Not Applicable

参考
[1] Rusnak DW, et al. Mol Cancer Ther, 2001, 1(2), 85-94.

参考

[1] Rusnak DW, et al. Mol Cancer Ther, 2001, 1(2), 85-94.

化学情報

分子量	581.06	化学式	C₂₉H₂₆ClFN₄O₄S
CAS No.	231277-92-2	SDF	Download Lapatinib SDFをダウンロードする
Smiles	CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (172.09 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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* 大学・企業名 大学・企業名を記入してください

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よくある質問（FAQ）

質問1:
If I want to use this compound(S2111, Lapatinib) in tumor-bearing mice via injection, how could I prepare the solution?

回答
For I.P. administration, the compound solution should be clear solution. S2111 Lapatinib can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):