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PD 166285-CAS 212391-63-4-Calbiochem
产品编号: | 4084124 |
规格: | A cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor that suppresses angiogenesis both in vitro and in vivo. |
CAS NO: | 212391-63-4 |
包装规格: | 5 MG |
产品类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
产品别名
212391-63-4
PD 166285-CAS 212391-63-4-Calbiochem
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
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
基本信息
Empirical Formula【经验(实验)分子式】 | C26H27Cl2N5O2 · 2HCl |
Molecular weight | 585.35 |
General description【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. 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. |
Warning【警告】 | Toxicity: Standard Handling (A) |
Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
Other Notes【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. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥97% (HPLC) |
form【形式】 | solid |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze desiccated (hygroscopic) protect from light |
color【颜色】 | pale yellow |
solubility【溶解性】 | DMSO: 50 mg/mL |
shipped in【运输】 | ambient |
storage temp.【储存温度】 | 2-8℃ |
packaging【包装】 | Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |