同义名 :	RXDX-106
	CAS号 :	1437321-24-8
	货号 :	A525104
	分子式 :	C31H26F2N4O6
	纯度 :	99%+
	分子量 :	588.56
	MDL号 :	MFCD28502441
	存储条件：	Pure form Inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	CEP-40783 is a robust, selective, and orally bioavailable antagonist of AXL and c-Met, exhibiting IC50 values of 7 nM and 12 nM, respectively. In cells transfected with AXL, such as 293GT, CEP-40783's activity is enhanced 27 times more than that of the recombinant enzyme, with an IC50 of 0.26 nM. Additionally, CEP-40783's efficacy against c-Met is pronounced in GTL-16 cells, with an IC50 of 6 nM. This heightened activity in cellular environments may be due to CEP-40783's prolonged binding to AXL and c-Met, aligning with a Type II mechanism. Furthermore, CEP-40783 is highly selective within the kinome, inhibiting over 90% of 298 kinases at a concentration of 1 µM, as indicated by an S90 value of 0.04[1].
作用机制	ATP-competitive inhibitor that targets all three TAM receptors.

临床研究
NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03454243	Advanced or Metastatic Solid T... 展开 >>umors 收起 <<	Early Phase 1	Terminated(Sponsor's decision)	-	United States, Texas ... 展开 >> START San Antonio, Texas, United States, 78229 收起 <<

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.70mL 0.34mL 0.17mL	8.50mL 1.70mL 0.85mL	16.99mL 3.40mL 1.70mL