513028

PD 166285

A cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor that suppresses angiogenesis both in vitro and in vivo.

• 别名: PD 166285, PD166285, PD0166285, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, PDGFR Tyrosine Kinase Inhibitor XIX, Wee1 Inhibitor IV, PDGFR Tyrosine Kinase Inhibitor XIX, Wee1 Inhibitor IV, 6-(2,6-Dichlorophenyl)-2-(4-(2-(diethylaminoethoxy)-phenylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one, 2HCl, PD166285, PD0166285
• 经验公式（希尔记法）: C₂₆H₂₇Cl₂N₅O₂ · 2HCl
• CAS号: 212391-63-4
• 分子量: 585.35
• UNSPSC代码: 12352200

属性

• 质量水平: 100
• 方案: ≥97% (HPLC)
• 表单: solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; desiccated (hygroscopic); protect from light
• 颜色: pale yellow
• 溶解性: DMSO: 50 mg/mL
• 运输: ambient
• 储存温度: 2-8°C
• InChI: 1S/C26H27Cl2N5O2.2ClH/c1-4-33(5-2)13-14-35-19-11-9-18(10-12-19)30-26-29-16-17-15-20(25(34)32(3)24(17)31-26)23-21(27)7-6-8-22(23)28;;/h6-12,15-16H,4-5,13-14H2,1-3H3,(H,29,30,31);2*1H
• InChI key: NADLBPWBFGTESN-UHFFFAOYSA-N

说明

一般描述

A cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor (IC₅₀ against against c-Src, Wee1, FGFR-1, Myt1, EGFR, and PDGFRβ = 8.4, 24, 39.3, 72, 87.5 and 98.3 nM, respectively) that suppresses angiogenesis both in vitro (max inhibition dose at 100 nM in HUVEC microcapillary formation assays) and in vivo (max inhibition achieved via 5 mg/kg p.o. in murine Matrigel plug angiogenesis assays), while exhibiting much reduced potency against Chk1, MAPK, and PKC (IC₅₀ = 3.4, 5, and 22.7 µM, respectively) and little activity toward IRTK and Cdk4/D1 even at concentrations as high as 50 µM. Shown to effectively block PDGF-, EGF-, and bFGF-stimulated receptor phosphorylations (IC₅₀ = 6.5, 1600, and 97.3 nM, respectively) and other cellular responses in rat aortic smooth muscle cells. Inhibition of cellular Wee1 activity by 500 nM PD 166285 in combination with 50 ng/ml nocodazole (Cat. No. 487928) treatment is also reported to result in a blockage of radiation-induced Cdc2 phosphorylation on Tyr15 and Thr14 in 7 human cancer cells and specifically demonstrated to sensatize PA-1 cultures to radiation-induced cell death in a p53-dependent manner.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Wang, Y., et al. 2001. Cancer Res.61, 8211.
Dimitroff, C.J., et al. 1999. Invest. New Drugs17, 121.
Roginskaya, V., et al. 1999. Leukemia13, 855.
Panek, R.L., et al. 1997. J. Pharmacol. Exp. Ther.283, 1433.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable