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CEP-40783  ≥98%(HPLC)

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：一种高效、选择性和口服有效的axl和c-Met抑制剂，IC50值分别为7nM和12nM。
溶解性：溶于DMSO(7mg/mL)
储备液保存：-80°C, 2 years -20°C, 1 year
靶点：IC50: 7 nM (AXL) and 12 nM (c-Met)
体外研究：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 µM).
体内研究：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.
细胞实验：细胞系：3T3细胞 浓度：0.25, 1, 2.5, 10, 25, 100, 250 nM 处理时间：30 min 方法：用vehicle或RXDX-106处理表达Tyro3, Axl 或 Mer的3T3细胞，处理30分钟，检测受体磷酸化情况。
动物实验：动物模型：SCID Beige mice 剂量：30 mg/kg 给药处理：p.o.
保存条件：-20℃
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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