CEP-40783

一种多激酶抑制剂；抑制Axl和c-MET（半数抑制浓度IC50分别为7纳摩尔和12纳摩尔）；抑制表达Axl的293GT细胞中的Axl以及NCI H1299非小细胞肺癌（NSCLC）细胞中的c-MET（IC50分别为0.26纳摩尔和6纳摩尔）；抑制TYRO3和MER（IC50分别为3.5纳摩尔和1.89纳摩尔）；在Axl/NIH3T3小鼠异种移植模型中，以0.3毫克/千克的剂量可诱导肿瘤完全消退；在EBC-1非小细胞肺癌小鼠异种移植模型中，分别以3毫克/千克和10毫克/千克的剂量可诱导肿瘤停滞生长和消退；在MC38小鼠同基因模型中减缓肿瘤生长，同时激活先天性和适应性免疫细胞。A multi-kinase inhibitor; inhibits Axl and c-MET (IC50s = 7 and 12 nM, respectively); inhibits Axl in 293GT cells expressing Axl and c-MET in NCI H1299 NSCLC cells (IC50s = 0.26 and 6 nM, respectively); inhibits TYRO3 and MER (IC50s = 3.5 and 1.89 nM, respectively); induces complete regression of tumors in an Axl/NIH3T3 mouse xenograft model at 0.3 mg/kg; induces tumor stasis and regression in an EBC-1 NSCLC mouse xenograft model at 3 and 10 mg/kg, respectively; reduces tumor growth in an MC38 mouse syngeneic model concomitantly with innate and adaptive immune cell activation.