Osimertinib mesylate

別名：AZD9291 mesylate

製品コード：S5078 純度：99.99%

Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.

CAS No. 1421373-66-1

サイズ	価格(税別)	在庫状況
25mg	JPY 22000	国内在庫あり
1g	JPY 145500	国内在庫なし(納期7~10日)

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（106）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Osimertinib mesylate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
NCI-H1975	Function assay	1 to 1000 nM	2 hrs	Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant phosphorylation in human NCI-H1975 cells at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method	27396610
NCI-H1975	Function assay	1 to 1000 nM	2 hrs	Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method	27396610
NCI-H1975	Function assay	1 uM	4 hrs	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
NCI-H1975	Function assay	1 uM	4 hrs	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
HCC827	Function assay	1 uM	4 hrs	Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
HCC827	Function assay	1 uM	4 hrs	Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis	28282122
NCI-H1975	Function assay	1 uM	48 hrs	Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as caspase3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
PC9	Function assay	1 uM	48 hrs	Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Function assay	1 uM	48 hrs	Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
H3255	Function assay	1 uM	48 hrs	Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting	28282122
NCI-H1975	Function assay	1 uM	48 hrs	Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
PC9	Function assay	1 uM	48 hrs	Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
HCC827	Function assay	1 uM	48 hrs	Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
H3255	Function assay	1 uM	48 hrs	Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting	28282122
NCI-H1975	Antitumor assay	10 mg/kg	21 days	Antitumor activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells xenografted in BALB/c athymic nude mouse assessed as tumor growth inhibition at 10 mg/kg, po bid for 21 days	29730192
BAF3	Function assay	1 to 3 uM	2 hrs	Inhibition of EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis	30429956
BAF3	Function assay	1 to 3 uM	2 hrs	Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis	30429956
NCI-H1975	Function assay	up to 10 uM	4 hrs	Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis	30442506
A431	Function assay	up to 10 uM	4 hrs	Inhibition of WT EGFR in human A431 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis	30442506
HeLa	Function assay	0.1 to 5 uM	24 hrs	Inhibition of EFGR protein expression in human HeLa cells at 0.1 to 5 uM after 24 hrs by Western blot analysis	31683104
DFCI032	Function assay	0.1 to 1 uM		Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM by Western blot analysis	28528303
DFCI032	Function assay	0.1 to 1 uM		Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis	28528303
DFCI032	Function assay	0.1 to 1 uM		Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR mediated ERK phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis	28528303
NCI-H1975	Function assay	1 to 100 nM		Inhibition of EGFR L858R/T790M double mutant phosphorylation in EGF-stimulated human NCI-H1975 cells at 1 to 100 nM by Western blot method	29906114
NCI-H1975	Function assay	100 nM		Inhibition of EGFR L858R/T790M double mutant in EGF-stimulated human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Ser-473 residue at 100 nM by Western blot method	29906114
PC9	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.023μM	25271963
NCI-H1975	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.024μM	25271963
Calu3	Cytotoxicity assay		72 hrs	Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.264μM	25271963
NCI-H1975	Function assay		2 hrs	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay, IC50=15μM	25271963
PC9	Function assay		2 hrs	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay, IC50=17μM	25271963
PC9-DRH	Function assay		2 hrs	Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISA, IC50=0.013μM	26756222
NCI-H1975	Function assay		2 hrs	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA, IC50=0.015μM	26756222
HCC827	Function assay		2 hrs	Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISA, IC50=0.023μM	26756222
H3255	Function assay		2 hrs	Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISA, IC50=0.036μM	26756222
PC9	Function assay		2 hrs	Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA, IC50=0.056μM	26756222
H1975	Function assay		2 hrs	Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs by ELISA, IC50=0.015μM	26968253
PC9	Function assay		2 hrs	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA, IC50=0.017μM	26968253
LoVo	Function assay		2 hrs	Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA, IC50=0.48μM	26968253
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay, IC50=0.052μM	27131639
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay, IC50=0.893μM	27131639
HCC827	Function assay		3 hrs	Inhibition of EGFR E746 to A750 deletion mutant phosphorylation in human patient derived HCC827 cells incubated for 3 hrs by ELISA method, IC50=0.0025μM	27433829
H1975	Function assay		3 hrs	Inhibition of EGFR L858R/T790M mutant phosphorylation in human patient derived H1975 cells incubated for 3 hrs by ELISA method, IC50=0.0025μM	27433829
H3255	Function assay		3 hrs	Inhibition of EGFR L858R mutant phosphorylation in human patient derived H3255 cells incubated for 3 hrs by ELISA method, IC50=0.0041μM	27433829
HaCaT	Function assay		3 hrs	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method, IC50=0.0737μM	27433829
LoVo	Function assay		2 hrs	Inhibition of EGF-stimulated wild type EGFR phosphorylation in human LoVo cells incubated for 2 hrs followed by EGF stimulation for 10 mins by ELISA, IC50=0.48μM	27996267
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay, IC50=0.03μM	28033579
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay, IC50=1.604μM	28033579
HCC827	Function assay		96 hrs	Inhibition of EGFR delE746_A750 mutant in human HCC827 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50<0.014μM	28225269
NCI-H1975	Function assay		96 hrs	Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50=0.019μM	28225269
A431	Function assay		96 hrs	Inhibition of wild-type EGFR in human A431 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50=0.667μM	28225269
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50<0.0003μM	28282122
BAF3	Function assay		72 hrs	Inhibition of full length EGFR T790M/L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50<0.0003μM	28282122
BAF3	Function assay		72 hrs	Inhibition of full length EGFR exon 19 deletion mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.001μM	28282122
HCC827	Function assay		72 hrs	Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.001μM	28282122
PC9	Function assay		72 hrs	Inhibition of EGFR exon 19 deletion mutant in human PC9 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.002μM	28282122
BAF3	Function assay		4 hrs	Inhibition of EGFR T790M/L858R mutant (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis, EC50=0.002μM	28282122
NCI-H1975	Function assay		72 hrs	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.005μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.013μM	28282122
H3255	Function assay		72 hrs	Inhibition of EGFR L858R mutant in human H3255 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.033μM	28282122
BAF3	Function assay		4 hrs	Inhibition of wild-type EGFR (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis, EC50=0.043μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.3μM	28282122
BAF3	Function assay		72 hrs	Inhibition of full length EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.31μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused INSR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.5μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.55μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused IGF1R (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.56μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.59μM	28282122
BAF3	Function assay		72 hrs	Inhibition of Tel-fused EGFR L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.59μM	28282122
BAF3	Growth inhibition assay		72 hrs	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50=1.2μM	28282122
NCI-H2122	Function assay		72 hrs	Inhibition of wild-type EGFR in human NCI-H2122 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=1.2μM	28282122
CHL	Growth inhibition assay		72 hrs	Growth inhibition of CHL cells after 72 hrs by CellTiter-Glo assay, GI50=2.9μM	28282122
H1355	Function assay		72 hrs	Inhibition of wild-type EGFR in human H1355 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3μM	28282122
A549	Function assay		72 hrs	Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3.5μM	28282122
H1703	Function assay		72 hrs	Inhibition of wild-type EGFR in human H1703 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3.5μM	28282122
CHO	Growth inhibition assay		72 hrs	Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay, GI50=4.2μM	28282122
Sf9	Function assay		20 mins	Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50=0.278μM	28482151
BAF3	Function assay		72 hrs	Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.006μM	28528303
BAF3	Function assay		72 hrs	Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.016μM	28528303
BAF3	Function assay		72 hrs	Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.018μM	28528303
BAF3	Function assay		72 hrs	Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.02μM	28528303
BAF3	Function assay		72 hrs	Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.066μM	28528303
DFCI032	Function assay		72 hrs	Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs in presence of ceritinib by MTS assay, EC50=0.19μM	28528303
BAF3	Function assay		72 hrs	Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=1.748μM	28528303
DFCI076	Function assay		72 hrs	Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay in presence of ceritinib, EC50=3.21μM	28528303
DFCI032	Function assay		72 hrs	Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=4.73μM	28528303
DFCI076	Function assay		72 hrs	Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=7.93μM	28528303
NCI-H1975	Antiproliferative assay		96 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay, EC50=0.019μM	28603991
A431	Antiproliferative assay		96 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay, EC50=0.7μM	28603991
PC9	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay, IC50=0.0065μM	28716641
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay, IC50=0.0105μM	28716641
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay, IC50=0.4159μM	28716641
BEAS2B	Antiproliferative assay		72 hrs	Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay, IC50=14.9μM	28716641
HCC827	Antiproliferative assay		96 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50<0.014μM	28853575
NCI-H1975	Antiproliferative assay		96 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50<0.014μM	28853575
A431	Antiproliferative assay		96 hrs	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50=0.67μM	28853575
A549	Antiproliferative assay		96 hrs	Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50=1.83μM	28853575
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=0.019μM	29466773
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay, IC50=0.027μM	29466773
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50=0.53μM	29466773
NCI-H1975	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.06μM	29486953
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.65μM	29486953
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50=0.87μM	29486953
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=0.023μM	29534926
NCI-H1975	Function assay		1 hr	Inhibition of EGFR L858R/T790M mutant phosphorylation in human NCI-H1975 cells after 1 hr by ELISA, IC50=0.041μM	29534926
A431	Function assay		1 hr	Inhibition of wild-type EGFR phosphorylation in human A431 cells preincubated for 1 hr followed by EGF stimulation measured after 45 mins by ELISA, IC50=0.141μM	29534926
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay, IC50=0.685μM	29534926
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay, IC50=0.0254μM	29576272
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.0472μM	29576272
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.486μM	29576272
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay, IC50=0.041μM	29730192
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay, IC50=1.26μM	29730192
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=0.019μM	29853340
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay, IC50=0.027μM	29853340
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=0.53μM	29853340
NCI-H1975	Function assay		2 hrs	Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells preincubated for 2 hrs followed by compound washout measured up to 24 hrs by Western blot method	29906114
NCI-H1975	Function assay		2 hrs	Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in ERK1/2 phosphorylation preincubated for 2 hrs followed by compound washout measured after 12 hrs by Western blot method	29906114
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay, IC50=0.13μM	30429956
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay, IC50=1.24μM	30429956
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50=4.61μM	30429956
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50=5.15μM	30429956
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay, GI50=0.0028μM	30442506
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay, IC50=0.011μM	30442506
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay, GI50=0.0401μM	30442506
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay, IC50=0.06μM	30442506
PC9	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay, IC50=0.16μM	30442506
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=0.61μM	30442506
Calu3	Antiproliferative assay		72 hrs	Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=0.75μM	30442506
Calu6	Antiproliferative assay		72 hrs	Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=5.86μM	30442506
NCI-H1975	Function assay		4 hrs	Inhibition of EGFR T790M/L858R double mutant phosphorylation at Y1068 residue in human NCI-H1975 cells up to 10 uM after 4 hrs by Western blot analysis	30442506
A431	Function assay		4 hrs	Inhibition of WT EGFR phosphorylation at Y1068 residue in human A431 cells up to 10 uM after 4 hrs by Western blot analysis	30442506
Sf9	Function assay		60 mins	Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay, IC50=0.0208μM	30471829
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay, IC50=0.096μM	30471829
Sf9	Function assay		60 mins	Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay, IC50=0.5675μM	30471829
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay, IC50=0.945μM	30471829
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=3.242μM	30471829
Aspc-1	Antiproliferative assay		72 hrs	Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay, IC50=3.985μM	30471829
NCI-H1975	Growth inhibition assay		72 hrs	Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.1μM	30472599
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.073μM	30530173
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.615μM	30530173
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50=1.605μM	30530173
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay, IC50=0.03μM	31223440
A431	Antiproliferative assay		72 hrs	Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay, IC50=1.44μM	31223440
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay, IC50=3.93μM	31223440
BAF3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay, IC50=5.11μM	31223440
PC9	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50<0.01μM	31446247
CL68	Antiproliferative assay		72 hrs	Antiproliferative activity against human CL68 cells harbouring EGFR delE746-A750/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.01μM	31446247
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.05μM	31446247
CL97	Antiproliferative assay		72 hrs	Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.1μM	31446247
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=5μM	31446247
A431	Cytotoxicity assay		96 hrs	Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method, CC50=0.967μM	31560541
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.014μM	31581004
PC9	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.016μM	31581004
NCI-H292	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=1.084μM	31581004
LO2	Cytotoxicity assay		72 hrs	Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=1.602μM	31581004
HEK293A	Cytotoxicity assay		72 hrs	Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=2.418μM	31581004
HK2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=3.565μM	31581004
HLF	Cytotoxicity assay		72 hrs	Cytotoxicity against human HLF cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=8.741μM	31581004
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.073μM	31683104
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.462μM	31683104
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.975μM	31683104
BAF3	Function assay		72 hrs	Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.001μM	31689114
BAF3	Function assay		72 hrs	Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.081μM	31689114
A431	Antiproliferative assay		96 hrs	Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.084μM	31689114
BAF3	Function assay		72 hrs	Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.78μM	31689114
BAF3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=1.1μM	31689114
BaF3	Function assay		4 hrs	Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay, IC50=3.1μM	31689114
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay, IC50=0.07μM	31718182
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay, IC50=3.1μM	31718182
NCI-H1975	Cytotoxicity assay		4 days	Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay, IC50=0.013μM	ChEMBL
A549	Cytotoxicity assay		4 days	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay, IC50=0.31μM	ChEMBL
Vero	Antiviral assay		24 hrs	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50=3.26μM	ChEMBL
Vero	Cell viability assay		72hrs	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr, CC50=13.23μM	ChEMBL
NCI-H1975	Function assay		16 hrs	Inhibition of EGFR T790M/L858R double mutant phosphorylation in human NCI-H1975 cells up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis	ChEMBL
NCI-H1975	Function assay		16 hrs	Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as AKT phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis	ChEMBL
NCI-H1975	Function assay		16 hrs	Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as ERK1/2 phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis	ChEMBL
A549	Function assay			Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA, IC50=0.15μM	26756222
Sf21	Function assay			Inhibition of N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (696-end residues) expressed in baculovirus infected Sf21 insect cells, IC50=0.012μM	27996267
HCC827	Antiproliferative assay			Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant, IC50=0.0616μM	28426996
NCI-H1975	Antiproliferative assay			Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant, IC50=0.067μM	28426996
HEK293	Function assay			Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis, IC50=0.57μM	28426996
A431	Antiproliferative assay			Antiproliferative activity against human A431 cells harboring wild-type EGFR, IC50=0.6156μM	28426996
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生物活性

製品説明

Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.

Targets

EGFR ^[1]

In Vitro
In vitro	Osimertinib-resistant lung adenocarcinoma (LUAD) cells express higher level of METTL7B in comparison to Osimertinib-sensitive cells. Knock-down of METTL7B by GNC-siRNA re-sensitized LUAD cells to osimertinib.^[1]
細胞実験	細胞株	lung adenocarcinoma (LUAD) cell lines
	濃度	0.001 -1 µM
	反応時間	72 h
	実験の流れ	Cells are plated at a density of 3,000 cells/well in 96 well plates. Osimertinib is added to the medium and treated for 72 h. Cell viability assays are performed by Cell Counting Kit-8.

In Vivo
In Vivo	METTL7B is significantly increased in both mRNA and protein level in osimertinib -resistant xenografts as compared with those in osimertinib-sensitive xenografts. In LUAD CDX mouse model, combination treatment with GNC-siMETTL7B (6 mg siRNA per mouse equivalent) significantly suppresses tumor growth as compared with treatment of osimertinib (30 mg/kg) alone.

参考
[1] Song H, et al. Mol Cancer. 2022 Feb 10;21(1):43. [2] Alessandro Leonetti, et al. Br J Cancer . 2019 Oct;121(9):725-737.

参考

化学情報

分子量	595.71	化学式	C₂₉H₃₇N₇O₅S
CAS No.	1421373-66-1	SDF	--
Smiles	CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC.CS(=O)(=O)O
保管	3 years -20°C powder	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 years -20°C powder	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个月-20°Cin solvent

In vitro
Batch:

DMSO : 5 mg/mL ( (8.39 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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電話番号

* 内容 お問い合わせ内容をご入力ください

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):