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| | PD 166285 Basic information |
| Product Name: | PD 166285 | | Synonyms: | 6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one Hydrochloride;PD 166285;6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-onedihydrochloride;PD 166285 dihydrochloride;6-(2,6-Dichloro-phenyl)-2-[4-(2-diethylaMino-ethoxy)-phenylaMino]-8-Methyl-8H-pyrido[2,3-d]pyriMidin-7-one hydrochloride;6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimi;6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylaMino)ethoxy]phenyl]aMino]-8-Methylpyrido[2,3-d]pyriMidin-7(8H)-one;PD 166285 - CAS 212391-63-4 - Calbiochem | | CAS: | 212391-63-4 | | MF: | C26H29Cl4N5O2 | | MW: | 585.37 | | EINECS: | | | Product Categories: | Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators | | Mol File: | 212391-63-4.mol |  |
| | PD 166285 Chemical Properties |
| Melting point | 239-242?C | | storage temp. | Desiccate at RT | | solubility | DMSO, Methanol | | form | Pale yellow solid | | color | Yellow | | Stability: | Hygroscopic |
| | PD 166285 Usage And Synthesis |
| Chemical Properties | Yellow Solid | | Uses | A broad-spectrum receptor tyrosine kinase (RTK) inhibitor which shows anti-angiogenic activity and anti-tumor efficacy in combination with photodynamic therapy (PDT). | | General Description | 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. | | Biological Activity | Potent inhibitor of the tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β (PDGFR β ) (IC 50 values are 8.4, 39.3 and 98.3 nM respectively). Also inhibits the checkpoint kinases Wee1 and Myt1; abolishes Cdc2 phosphorylation in numerous tumor cell lines and abrogates the G 2 checkpoint. | | storage | Desiccate at RT |
| | PD 166285 Preparation Products And Raw materials |
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