ホームページ Protein Tyrosine Kinase ALK inhibitor - IGF-1R inhibitor - FLT3 inhibitor - Serine/threonin kinase inhibitor Ceritinib For research use only.

Ceritinib

別名：LDK378

Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.

Ceritinib化学構造

CAS No. 1032900-25-6

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 70500 国内在庫あり
JPY 145500 国内在庫あり
JPY 448500 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]
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文献中Selleckの製品使用例（112）

製品安全説明書

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99.96

Ceritinib関連製品

シグナル伝達経路

ALK Signaling Pathways

ALKシグナル伝達経路

ALK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
KARPAS299 Apoptosis assay 60 nM 24 hrs Induction of apoptosis in human KARPAS299 cells harboring NPM-ALK at 60 nM after 24 hrs by acridine orange/ethidium bromide staining based fluorescence microscopic method 29174809
SU-DHL1 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human SU-DHL1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 200 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay 20 to 200 nM 1 hr Inhibition of ALK phosphorylation at Y1278 residue in human SU-DHL1 cells at 20 to 200 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human NCI-H3122 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 200 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human NCI-H3122 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 200 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human SU-DHL1 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 200 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human SU-DHL1 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 200 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay 20 to 200 nM 1 hr Inhibition of ALK phosphorylation at Y1278 residue in human NCI-H3122 cells at 20 to 200 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay 20 to 200 nM 1 hr Inhibition of ALK in human NCI-H3122 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 200 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay 30 nM 16 hrs Inhibition of ALK autophosphorylation at Y1507 residue in human SU-DHL1 cells at 30 nM after 16 hrs by Western blot analysis 29627725
SU-DHL1 Function assay 30 nM 16 hrs Inhibition of ALK in human SU-DHL1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 30 nM after 16 hrs by Western blot analysis 29627725
NCI-H3122 Function assay 50 to 250 nM 16 hrs Induction of ALK degradation in human NCI-H3122 cells assessed as decrease in ALK phosphorylation at Y1604 at 50 to 250 nM after 16 hrs by immunoblot method 29660984
KARPAS299 Function assay 50 to 250 nM 16 hrs Induction of ALK degradation in human KARPAS299 cells assessed as decrease in ALK phosphorylation at Y1604 at 50 to 250 nM after 16 hrs by immunoblot method 29660984
KARPAS299 Apoptosis assay 50 nM 24 hrs Induction of apoptosis in human KARPAS299 cells assessed as unclear cell shrinkage at 50 nM after 24 hrs by Hoechst 33258 staining based inverted fluorescence microscopy 30223120
KARPAS299 Apoptosis assay 50 nM 24 hrs Induction of apoptosis in human KARPAS299 cells assessed as late apoptotic cells at 50 nM after 24 hrs by AO/EB double staining based inverted fluorescence microscopy 30223120
KARPAS299 Apoptosis assay 50 nM 24 hrs Induction of apoptosis in human KARPAS299 cells assessed as fragmentation at 50 nM after 24 hrs by Hoechst 33258 staining based inverted fluorescence microscopy 30223120
Ba/F3 NA C1156Y Growth Inhibition Assay 72 h IC50=0.071 μM 25727400
Ba/F3 NA WT Growth Inhibition Assay 72 h IC50=0.020 μM 25727400
C1156F/D1203N 2809 Growth Inhibition Assay 72 h IC50=254 ± 99 nM 25749034
E1210K 748 Growth Inhibition Assay 72 h IC50=187 ± 84 nM 25749034
N1178H 169 Growth Inhibition Assay 72 h IC50=42 ± 6 nM 25749034
F1174I 184 Growth Inhibition Assay 72 h IC50=13 ± 0.1 nM 25749034
I1171T 445 Growth Inhibition Assay 72 h IC50=82 ± 12 nM 25749034
I1171N 519 Growth Inhibition Assay 72 h IC50=187 ± 87 nM 25749034
C1156F 1293 Growth Inhibition Assay 72 h IC50=217 ± 115 nM 25749034
G1128S 1022 Growth Inhibition Assay 72 h IC50=102 ± 38 nM 25749034
WT 70 Growth Inhibition Assay 72 h IC50=21 ± 8 nM 25749034
Parental(+IL3) Growth Inhibition Assay 72 h IC50=1586 ± 173 nM 25749034
Ba/F3 NA L1196M Growth Inhibition Assay 72 h IC50=0.042 μM 25727400
Ba/F3 NA L1152R Growth Inhibition Assay 72 h IC50=0.288 μM 25727400
Ba/F3 NA G1202R Growth Inhibition Assay 72 h IC50=0.277 μM 25727400
Ba/F3 NA G1269A Growth Inhibition Assay 72 h IC50=0.019 μM 25727400
Ba/F3 NA S1206Y Growth Inhibition Assay 72 h IC50=0.037 μM 25727400
Ba/F3 EA WT Growth Inhibition Assay 72 h IC50=0.021 μM 25727400
Ba/F3 EA C1156Y Growth Inhibition Assay 72 h IC50=0.026 μM 25727400
Ba/F3 EA L1196M Growth Inhibition Assay 72 h IC50=0.019 μM 25727400
Ba/F3 EA L1152R Growth Inhibition Assay 72 h IC50=0.099 μM 25727400
Ba/F3 EA G1202R Growth Inhibition Assay 72 h IC50=0.467 μM 25727400
Ba/F3 EA G1269A Growth Inhibition Assay 72 h IC50=0.033 μM 25727400
Ba/F3 EA S1206Y Growth Inhibition Assay 72 h IC50=0.038 μM 25727400
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.0107 μM. 29288940
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.015 μM. 26568289
NCI-H2228 Growth inhibition assay 3 days Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay, IC50 = 0.015 μM. 29627725
SU-DHL1 Growth inhibition assay 3 days Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay, IC50 = 0.015 μM. 29627725
DFCI114 Antiproliferative assay 72 hrs Antiproliferative activity against human DFCI114 cells expressing EML4-ALK G1269A mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.018 μM. 26568289
HCC78 Cytotoxicity assay 72 hrs Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.018 μM. 27474925
KARPAS299 Cytotoxicity assay 2 to 3 days Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.0228 μM. 23742252
NCI-H3122 Function assay 72 hrs Inhibition of EML4 fused ALK in human NCI-H3122 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.025 μM. 27915169
BAF3 Function assay 2 to 3 days Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.026 μM. 23742252
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.026 μM. 29174809
NCI-H2228 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.026 μM. 30223120
KARPAS299 Cytotoxicity assay 72 hrs Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay, IC50 = 0.027 μM. 27474925
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.033 μM. 26568289
NCI-H3122 Function assay 72 hrs Inhibition of EML4-ALK in human NCI-H3122 cells assessed as inhibition of cell proliferation after 72 hrs by SRB assay, CC50 = 0.038 μM. 26923695
NCI-H3122 Function assay 72 hrs Inhibition of EML4-ALK in human NCI-H3122 cells assessed as inhibition of cell proliferation after 72 hrs by SRB assay, CC50 = 0.038 μM. 26923695
NCI-H3122 Function assay 72 hrs Inhibition of EML4 fused ALK in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB assay, CC50 = 0.038 μM. 28385505
Ba/F3 Function assay 72 hrs Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.041 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.041 μM. 26568289
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay, IC50 = 0.041 μM. 30223120
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.0549 μM. 29288940
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.057 μM. 26568289
HCC78 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.058 μM. 29174809
HCC78 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay, IC50 = 0.058 μM. 30223120
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.064 μM. 26568289
DFCI76 Antiproliferative assay 72 hrs Antiproliferative activity against human DFCI76 cells expressing EML4-ALK L1152R mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.072 μM. 26568289
BA/F3 Function assay 72 hrs Inhibition of ALK L1196M mutant in mouse BA/F3 cells assessed as inhibition of cell proliferation after 72 hrs by WST1 assay, CC50 = 0.075 μM. 26923695
BA/F3 Function assay 72 hrs Inhibition of EML4 fused ALK L1196M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.075 μM. 27915169
BA/F3 Function assay 72 hrs Inhibition of EML4 fused ALK (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay, CC50 = 0.075 μM. 27915169
BAF3 Function assay 72 hrs Inhibition of ALK L1196M mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by WST-1 assay, CC50 = 0.075 μM. 28385505
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.084 μM. 29288940
SMS-KCNR Antiproliferative assay 72 hrs Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.092 μM. 26568289
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.096 μM. 29288940
NCI-H2228 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay, IC50 = 0.099 μM. 29174809
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.101 μM. 26568289
NCI-H2228 Cytotoxicity assay 72 hrs Cytotoxicity against human NCI-H2228 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.1026 μM. 25644671
LAN5 Antiproliferative assay 72 hrs Antiproliferative activity against human LAN5 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.122 μM. 26568289
SU-DHL1 Antiproliferative assay 72 hrs Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.122 μM. 29288940
Kelly Antiproliferative assay 72 hrs Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.142 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.164 μM. 26568289
SH-SY5Y Antiproliferative assay 72 hrs Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.186 μM. 26568289
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.234 μM. 29288940
SK-N-SH Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.303 μM. 26568289
BAF3 Function assay 2 to 3 days Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 0.3195 μM. 23742252
SK-N-FI Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.349 μM. 26568289
CHLA20 Antiproliferative assay 72 hrs Antiproliferative activity against human CHLA20 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.363 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.444 μM. 26568289
LAN1 Antiproliferative assay 72 hrs Antiproliferative activity against human LAN1 cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.549 μM. 26568289
SK-N-BE(2) Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-BE(2) cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.593 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.668 μM. 26568289
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.726 μM. 29288940
Ba/F3 Function assay 72 hrs Inhibition of human EGFR del19/T790M/C797S mutant expressed in mouse Ba/F3 cells assessed as cell growth inhibition after 72 hrs by CellTiter-Glo assay, GI50 = 0.7805 μM. 29136465
SK-N-AS Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.045 μM. 26568289
BAF3 Cytotoxicity assay 2 to 3 days Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay, IC50 = 2.477 μM. 23742252
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 2.747 μM. 26568289
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 5.512 μM. 26568289
SH-SY5Y Antiproliferative assay 72 hrs Antiproliferative activity against human SH-SY5Y cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
CHLA20 Antiproliferative assay 72 hrs Antiproliferative activity against human CHLA20 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
SH-SY5Y Antiproliferative assay 72 hrs Antiproliferative activity against human SH-SY5Y cells after 72 hrs in presence of ABCB1 inhibitor tariquidar by CellTiter-Glo luminescent cell viability assay 29660984
CHLA20 Antiproliferative assay 72 hrs Antiproliferative activity against human CHLA20 cells after 72 hrs in presence of ABCB1 inhibitor tariquidar by CellTiter-Glo luminescent cell viability assay 29660984
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
SU-DHL1 Antiproliferative assay 72 hrs Antiproliferative activity against human SU-DHL1 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay 29660984
KARPAS299 Cytotoxicity assay Cytotoxicity against human KARPAS299 cells expressing NPM-ALK fusion gene assessed as growth inhibition, IC50 = 0.0228 μM. 23837797
BA/F3 Cytotoxicity assay Cytotoxicity against mouse BA/F3 cells expressing NPM-ALK fusion gene assessed as growth inhibition, IC50 = 0.026 μM. 23837797
NCI-H3122 Antiproliferative assay Antiproliferative activity against wild type human NCI-H3122 cells, CC50 = 0.038 μM. 26235945
BA/F3 Function assay Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cells, IC50 = 0.0407 μM. 23837797
BAF3 Antiproliferative assay Antiproliferative activity against mouse BAF3 cells expressing ALK L1196M mutant, CC50 = 0.075 μM. 26235945
BA/F3 Cytotoxicity assay Cytotoxicity against mouse BA/F3 cells transfected with Tel-InsR gene assessed as growth inhibition, IC50 = 0.32 μM. 23837797
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生物活性

製品説明 Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.
特性 Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.
Targets
ALK [1]
(Cell-free assay)		 Insulin Receptor [1]
(Cell-free assay)		 IGF-1R [1]
(Cell-free assay)		 STK22D [1]
(Cell-free assay)		 FLT3 [1]
(Cell-free assay)
0.2 nM 7 nM 8 nM 23 nM 60 nM
In Vitro
In vitro LDK378 shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells. [1]
Kinase Assay Enzymatic kinase profiling description
All kinases are expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which is produced in E. coli. The kinase activity is measured in the LabChip mobility shift assay. The assay is performed at 30°C for 60 min. The effect of LDK378 on the enzymatic activity is obtained from the linear progress curves in the absence and presence of LDK378 and routinely determines from one reading (end point measurement)
細胞実験 細胞株 Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 cells
濃度 ~100 μM
反応時間 2-3 days
実験の流れ Luciferase-expressing cells are incubated with serial dilutions of LDK378 or DMSO for 2-3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-ALK / ALK / p-AKT / AKT / p-ERK / ERK pROS1 / ROS1 / pSTAT3 / STAT3 28425916
Growth inhibition assay Cell viability 29067644
In Vivo
In Vivo LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg. [1]
動物実験 動物モデル RNU nude rats bearing the Karpas299/H2228 tumors
投与量 ~50 mg/kg
投与経路 Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02450903 Completed
Non-Small-Cell Lung Cancer
Novartis Pharmaceuticals|Novartis
 August 21 2015 Phase 2
NCT02040870 Completed
Non-Small Cell Lung Cancer
Novartis Pharmaceuticals|Novartis
 March 7 2014 Phase 1|Phase 2
NCT01950481 Completed
Normal Hepatic Function|Impaired Hepatic Function
Novartis Pharmaceuticals|Novartis
 January 2014 Phase 1
NCT01772797 Completed
Anaplastic Lymphoma Kinase (ALK)|Non-small Cell Lung Cancer
Novartis Pharmaceuticals|Novartis
 June 2013 Phase 1
NCT01685060 Completed
Non-Small Cell Lung Cancer
Novartis Pharmaceuticals|Novartis
 November 26 2012 Phase 2
NCT01634763 Completed
Tumors Characterized by Genetic Alterations in Anaplastic Lymphoma Kinase (ALK)
Novartis Pharmaceuticals|Novartis
 June 2012 Phase 1

化学情報

分子量 558.14 化学式

C28H36ClN5O3S
CAS No. 1032900-25-6 SDF Download Ceritinib SDFをダウンロードする
Smiles CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl
保管

In vitro
Batch:

DMSO : 4 mg/mL ( (7.16 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

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）

mg/kg g μL 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

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Handling Instructions

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よくある質問（FAQ）

質問1:
how to reconstitute the inhibitor for oral administration to mice?

回答
You can resuspend LDK378 in 30% PEG400/0.5% Tween 80/5% propylene glycol and use the suspension for oral gavage feeding.

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