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概述
Vatalanib dihydrochloride (PTK787 dihydrochloride) 是VEGFR2/KDR的抑制剂，其IC50值为37nM。
Information
Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor ofVEGFR2/KDRwithIC50of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.
In vitro
Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Furthermore, Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2.
In vivo
Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes.
Cell Data
cell lines：
Concentrations：0-10 μM
Incubation Time：48 hours
Powder Purity:≥99%
规格
别名
瓦他拉尼(PTK787)2HCl
英文别名
ZK 222584 (cpg-79787) 2HCl | N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine dihydrochloride
规格或纯度
10mM in DMSO
英文名称
Vatalanib (PTK787) 2HCl
生化机理
Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787)是一种 VEGFR2/KDR 抑制剂，在无细胞试验中的 IC50 为 37 nM，对 VEGFR1/Flt-1 的抑制作用较弱，对 VEGFR3/Flt-4 的抑制作用为 18 倍。第 3 阶段。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC=C2C(=C1)C(=NN=C2NC3=CC=C(C=C3)Cl)CC4=CC=NC=C4.Cl.Cl
关联CAS
PubChem CID
分子量
419.74
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 54 mg/mL (198.34 mM);
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 A2303675 |
分析证书 | V408583 |
技术文档和文章
VEGFR Inhibitors
目录： 技术文章
溶液计算器
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