BMS-536924

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-536924 是一种 ATP 竞争性 IGF-1R/IR 抑制剂，IC50 为 100 nM/73 nM，对 Mek、Fak 和 Lck 活性适中，对 Akt1、MAPK1/2 活性极低。

BMS-536924 is a potent small molecule inhibitor of IGF-IR, which shows antitumor activity in multiple tumor models, including sarcoma.(In Vitro):BMS-536924 inhibits FAK and Lck with IC50s of 150 nM and 341 nM, respectively.BMS-536924 (1 μM; every four days for 12 days) blocks pBabe-MCF10A and CD8-IGF-IR-MCF10A acinar proliferation.BMS-536924 (0.01-1 μM; 24 hours) inhibits growth of CD8-IGF-IR-MCF10A cells and has an IC50 of 0.48 μM.BMS-536924 (1 μM; for 4 days) induces apoptosis in CD8-IGF-IR-MCF10A acini.BMS-536924 (0.1-1 μM; for 24 hours) decreases in S-phase cells and causes a G0/G1 block.BMS-536924 (1 μM; 10 min, 1, 8, 24, 48 hours) inhibits IGF-IR signaling in pBabe-MCF10A cells and inhibits phosphorylation of CD8-IGF-IR. BMS-536924 time-dependently inhibits AKT phosphorylation.(In Vivo):BMS-536924 (100 mg/kg; gavage; daily; for 35 days) causes regression of xenografts in vivo and an average reduction of 76% tumor volume after 2 weeks.

Cell Proliferation Assay Cell Line:pBabe-MCF10A and CD8-IGF-IR-MCF10A acini Concentration:1 μM Incubation Time:Every four days for 12 daysResult:Blocked acinar proliferation.Cell Viability Assay Cell Line:CD8-IGF-IR-MCF10A cells Concentration:0.01, 0.1, 1 μM Incubation Time:24 hours Result:Has an IC50 of 0.48 μM.Apoptosis AnalysisCell Line:CD8-IGF-IR-MCF10A acini Concentration:1 μM Incubation Time:For 4 days Result:Resulted in a dramatic induction of apoptosis.Cell Cycle Analysis Cell Line:CD8-IGF-IR-MCF10A cells and pBabe-MCF10A control cells Concentration:0.1, 0.5, 1 μM Incubation Time:For 24 hours Result:Decreased in S-phase cells and caused a G0/G1 block.Western Blot Analysis Cell Line:CD8-IGF-IR-MCF10A cells Concentration:1 μM Incubation Time:10 min, 1, 8, 24, 48 hours Result:Caused maximal inhibition of phosphorylated IGF-IR at 10 min and retained its ability to inhibit IGF-IR phosphorylation for up to 48 hours.

Animal Model:Athymic nude mice with CD8-IGF-IRMCF10A cells Dosage:100 mg/kg Administration:Gavage; daily; for 35 days Result:Caused an average reduction of 76% tumor volume after 2 weeks.

BMS536924 | BMS-536924 | BMS 536924

Others

Other Targets

FAK| IGF-1R| Insulin Receptor| MEK| Lck

Cancer

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468740-43-4

479.96

C25H26ClN5O3

>98% (HPLC)

DMSO : 50 mg/mL. 104.18 mM; H2O : < 0.1 mg/mL

CC1=C2N=C(NC2=CC(=C1)N1CCOCC1)C1=C(NC[C@@H](O)C2=CC=CC(Cl)=C2)C=CNC1=O

(S)-4-((2-(3-chlorophenyl)-2-hydroxyethyl)amino)-3-(4-methyl-6-morpholino-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one

(-20℃)

With Ice Pack

≥ 2 years