Vatalanib succinate  (Synonyms: PTK787 succinate; ZK-222584 succinate; CGP-79787 succinate)

Vatalanib (PTK787) succinate is a potent and orally active VEGFR inhibitor with IC₅₀s of 37 nM, 77 nM, 270 nM, 660 nM, 730 nM, 1400 nM, and 580 nM for KDR, Flt-1, Flk, Flt-4, c-Kit, c-Fms, and PDGFR-β, respectively^[1].

在基于细胞的检测中，Vatalanib (PTK787) 在纳摩尔范围内抑制 VEGF 诱导的激酶插入结构域受体 (KDR) 自身磷酸化、内皮细胞增殖、迁移和存活。在浓度高达 1 µM 时，Vatalanib (PTK787) 对不表达 VEGF 受体的细胞没有任何细胞毒性或抗增殖作用^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

小鼠口服给药（50 mg/kg）后，Vatalanib (PTK787) 的血浆浓度在 8 小时以上保持在 1 μM 以上。Vatalanib (PTK787) 在生长因子植入模型以及每日口服一次（25-100 mg/kg）后的肿瘤细胞驱动的血管生成模型中诱导 VEGF 和 PDGF 诱导的血管生成的剂量依赖性抑制^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

464.90

C₂₄H₂₁ClN₄O₄

212142-18-2

瓦他拉尼琥珀酸盐

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. J M Wood, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000 Apr 15;60(8):2178-89.  [Content Brief]