General description
一种有效的 VEGFR2 抑制剂,IC50:0.035nM,也可抑制c-Met、Ret、Kit、Flt-1/3/4、Tie2和AXL的活性,IC50值分别为1.3nM、4nM、4.6nM、12nM/11.3nM/6 nM、14.3nM和7nM。
Cabozantinib malate is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several RTKs, which are often overexpressed in a variety of cancer cell types, including hepatocyte growth factor receptor (MET), RET (rearranged during transfection), vascular endothelial growth factor receptor types 1 (VEGFR-1), 2 (VEGFR-2), and 3 (VEGFR-3), mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (FLT-3), TIE-2 (TEK tyrosine kinase, endothelial), tropomyosin-related kinase B (TRKB) and AXL. This may result in an inhibition of both tumor growth and angiogenesis, and eventually lead to tumor regression. Cabozantinib was approved by the U.S. FDA in November 2012 for the treatment of medullary thyroid cancer。
苹果酸卡波替尼是卡波替尼的s-苹果酸盐形式,卡波替尼是一种口服生物利用的小分子受体酪氨酸激酶(RTK)抑制剂,具有潜在的抗肿瘤活性。 卡波替尼强烈结合并抑制多种RTK,RTK在多种癌细胞中通常过表达,包括肝细胞生长因子受体(MET),RET(在转染过程中重新排列),血管内皮生长因子受体1(VEGFR-1), 2(VEGFR-2)和3(VEGFR-3),肥大/干细胞生长因子(KIT),FMS样酪氨酸激酶3(FLT-3),TIE-2(TEK酪氨酸激酶,内皮),原肌球蛋白- 相关激酶B(TRKB)和AXL。 这可能导致肿瘤生长和血管生成的抑制,并最终导致肿瘤消退。 卡博替尼于2012年11月获得美国FDA的批准,用于治疗甲状腺髓样癌。
Properties
Iupac Name: | (2S)-2-hydroxybutanedioic acid compound with N~1~-{4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl}-N~1~-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1) |
Inchi Code | 1S/C28H24FN3O5.C4H6O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18;5-2(4(8)9)1-3(6)7/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34);2,5H,1H2,(H,6,7)(H,8,9)/t;2-/m.0/s1 |
Inchi Key | HFCFMRYTXDINDK-WNQIDUERSA-N |
安全信息