Nintedanib esylate (BIBF 1120 esylate) 是一種有效的 VEGFR1/2/3,F(xiàn)GFR1/2/3 和 PDGFRα/β 三重抑制劑,IC50 值分別為 34 nM/13 nM/13 nM,69 nM/37 nM/108 nM 和 59 nM/65 nM。
中文名稱:
(3Z)-2,3-二氫-3-[[[4-[甲基[2-(4-甲基-1-基)乙酰]氨基]苯基]氨基]苯亞甲基]-2-氧代-1H-吲哚-6-甲酸甲酯乙磺酸鹽
英文名稱:
(3Z)-2,3-Dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid methyl ester ethanesulfonate
參考文獻
[1]. Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 2008, 68(12), 4774-4782.
[2]. Roth GJ, et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J Med Chem, 2009, 52(14), 4466-4480.