(Z)-Orantinib

Name: (Z)-Orantinib
Brand: TargetMol
SKU: T9684
Rating: 4.5 (1 reviews)

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产品编号 T9684Cas号 210644-62-5

(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，可诱导已形成的肿瘤消退。

(Z)-Orantinib

还可以

产品编号 T9684Cas号 210644-62-5

规格	价格	库存
2 mg	¥ 194	5日内发货
5 mg	¥ 297	5日内发货
10 mg	¥ 497	5日内发货
1 mL x 10 mM (in DMSO)	¥ 547	5日内发货

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生物活性

产品描述	(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC 50 s of 2.1, 0.008, and 1.2 μM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces established tumor regression[1] [2].
体外活性	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) [1]. SU6668 (0.03-10 μM; 60 min) inhibits the VEGF-stimulated increase of KDR tyrosine phosphorylation in HUVECs [1]. SU6668 inhibits HUVECs mitogenesis induced by both VEGF and FGF in a dose-dependent manner with IC 50 s of 0.34 and 9.6 μM, respectively [1].
体内活性	SU6668 (4-200 mg/kg/day; p.o. for 21 d) induces dose-dependent inhibition of A431 tumor growth in athymic mice [1]. SU6668 (75 mg/kg/day; i.p. for 22 d) significantly inhibits tumor angiogenesis and vascularization in mice [1]. SU6668 (200 mg/kg/day; p.o. for 11-27 d) induces striking regression of large established A431 xenografts in athymic mice [1]. Animal Model: Female athymic mice (BALB/c, nu/nu ) were implanted A431 tumor cells [1] Dosage: 4, 40, 75, 200 mg/kg Administration: P.o. daily for 21 days Result: Induced 97% growth inhibition against A431 tumor at the dose of 97%. No mortality was observed in any treatment group.