Vatalanib succinate_product_DataBase

Bioactivity	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].
Invitro	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]。 0 --> Vatalanib succinate 相关抗体:
In Vivo	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]。
Name	Vatalanib succinate
CAS	212142-18-2
Formula	C24H21ClN4O4
Molar Mass	464.90
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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