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CEP-40783
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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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