BIBF 1120 (esylate)

VEGFR、FGFR和PDGFR抑制剂（VEGFR1-3、FGFR1-4、PDGFRα和PDGFRβ的IC50s分别为13-34、37-610、59和65nM）；在33种激酶中对VEGFR、FGFR和PDGFR具有选择性，但抑制FLT3、LCK、LYN和Src（IC50s=16-156nM）；抑制HUVEC、HSMEC、HUASMC和BRP的生长因子依赖性增殖（EC50s=7-290nM）；在100mg/kg下降低FaDu头颈部小细胞癌小鼠异种移植模型中的肿瘤微血管密度和表达PDGFRβ的血管周围细胞的数量；抑制Caki-1肾癌小鼠异种移植模型中的肿瘤生长。A VEGFR, FGFR, and PDGFR inhibitor (IC50s = 13-34, 37-610, 59, and 65 nM for VEGFR1-3, FGFR1-4, PDGFRα, and PDGFRβ, respectively); selective for VEGFR, FGFR, and PDGFR over a panel of 33 kinases but does inhibit FLT3, LCK, LYN, and Src (IC50s = 16-156 nM); inhibits growth factor-dependent proliferation of HUVECs, HSMECs, HUASMCs, and BRPs (EC50s = 7-290 nM); reduces tumor microvessel density and the number of PDGFRβ-expressing perivascular cells in a FaDu head and neck small cell carcinoma mouse xenograft model at 100 mg/kg; inhibits tumor growth in a Caki-1 renal cancer mouse xenograft model.分子式C31H33N5O4 • C2H6O3S分子量649.8O=C1NC2=CC(C(OC)=O)=CC=C2/C1=C(C3=CC=CC=C3)/NC4=CC=C(N(C(CN5CCN(C)CC5)=O)C)C=C4.O=S(O)(CC)=O