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CEP-40783

CAS No. : 1437321-24-8

MCE 站：CEP-40783

产品活性：CEP-40783是高效选择性，有口服活性的AXL和c-Met抑制剂，IC₅₀值分别为7 nM 和12 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：TAM Receptor  |  c-Met/HGFR

In Vitro: In AXL-transfected 293GT cells, CEP-40783 is 27-fold more active compared to recombinant enzyme with an IC₅₀ value of 0.26 nM. CEP-40783 also demonstrates superior activity against c-Met in GTL-16 cells (IC₅₀=6 nM). The increased inhibitory activity of CEP-40783 in cells could be attributed to its extended residence time on both AXL and c-Met, consistent with a Type II mechanism. CEP-40783 shows high kinome selectivity against 298 kinases with an S90 of 0.04 (fraction of kinases showing >90% inhibition at 1 ?M).

In Vivo: CEP-40783 shows dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with 80% target inhibition at 0.3 mg/kg 6 h post dose and complete target inhibition to >90% inhibition at 1 mg/kg between 6-24 h, while a 10 mg/kg po dose resulted in complete AXL inhibition up to 48 h post dosing. In 3/5 (60%) of the tumor models, CEP-40783 shows in vivo efficacy, including tumor regressions, significantly superior to that achieved with an optimal regimen of paclitaxel. In 4/4 (100%) of the erlotinib-insensitive tumor models, CEP-40783 demonstrates significant efficacy (66 to 118% TGI) compared to the control group at the 30 mg/kg dose. Additionally, CEP-40783 in combination with erlotinib demonstrate superior anti-tumor efficacy compared to CEP-40783 and erlotinib single agents in the one erlotinib-sensitive model evaluated. CEP-40783 as a single agent and in combination with erlotinib are well tolerated.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Orally Active Compound Library  |  Anti-Lung Cancer Compound Library  |  2-D08  |  PHA-665752  |  2-Phospho-L-ascorbic acid trisodium  |  SGI-7079  |  SU11274  |  SRI 31215 TFA  |  c-Met inhibitor 1  |  X-376  |  TAM-IN-2  |  Tyrosine kinase inhibitor  |  c-met-IN-1  |  Meleagrin  |  Norleual  |  RU-302  |  Ensartinib

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