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(Z)-Orantinib

CAS No. : 210644-62-5

MCE 国际站：(Z)-Orantinib

产品活性：(Z)-Orantinib ((Z)-SU6668) 是一种有效，选择性，具有口服活性和 ATP 竞争性的 Flk‐1/KDR，PDGFRβ 和 FGFR1 抑制剂，IC₅₀ 值分别为 2.1，0.008 和 1.2 µM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂，可诱导已建立的肿瘤消退。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR  |  PDGFR  |  FGFR

In Vitro: SU6668 (5-15 min) inhibits Flk-1 trans-phosphorylation (K_i=2.1 μM), FGFR1 trans-phosphorylation (K_i=1.2 μM), and PDGFR autophosphorylation (K_i=0.008 μM).
SU6668 (0.03-10 μM; 60 min) inhibits the VEGF-stimulated increase of KDR tyrosine phosphorylation in HUVECs.
SU6668 inhibits mitogenesis of HUVECs induced by both VEGF and FGF in a dose-dependent manner with IC₅₀s of 0.34 and 9.6 μM, respectively.

In Vivo: SU6668 (4-200 mg/kg/day; p.o. for 21 d) induces dose-dependent inhibition of A431 tumor growth in athymic mice.
SU6668 (75 mg/kg/day; i.p. for 22 d) significantly suppresses tumor angiogenesis and vascularization in mice.
SU6668 (200 mg/kg/day; p.o. for 11-27 d) induces striking regression of large established A431 xenografts in athymic mice.

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