PDGFR酪氨酸激酶抑制剂III是酪氨酸激酶PDGFR家族的细胞可渗透，有效，选择性和ATP竞争性抑制剂（PDGFR-α为IC | 50 | = 50 nM，PDGFR-β为80 nM，PDGFR-β为50 nM c-Kit，Flt-3 / Flk-2为230 nM）。PDGFR酪氨酸激酶抑制剂III仅在更高浓度下（EGFR，FGFR，Src，PKA和PKC的IC50>30μM）才抑制其他激酶的活性。有报道阻止PDGF-BB诱导的猪主动脉平滑肌细胞增殖（IC | 50 | = 250 nM）。 PDGFR Tyrosine Kinase Inhibitor III is a cell-permeable, potent, selective, and ATP-competitive inhibitor of the PDGFR family of tyrosine kinases (IC|50|= 50 nM for PDGFR-α, 80 nM for PDGFR-β, 50 nM for c-Kit, and 230 nM for Flt-3/Flk-2). PDGFR Tyrosine Kinase Inhibitor III inhibits the activities of other kinases only at much higher concentrations (IC50 > 30μM for EGFR, FGFR, Src, PKA, and PKC). Reported to block PDGF-BB-induced proliferation of porcine aorta smooth muscle cells (IC|50|= 250 nM).
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PDGFR Tyrosine Kinase Inhibitor III
CAS number：205254-94-0 molecular formula：C27H27N5O4
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| Chinese alias | - | ||
| English alias | 4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carboxylic acid (4-phenoxy-phenyl)-amide | N-(4-Phenoxyphenyl)-4-(6,7-dimethoxyquinazoline-4-yl)piperazine-1-carboxamide | NCGC00185729-01 | IUN54940 | J-013383 | PD015743 | 4-(6,7-dimethoxy-4-quinazolinyl)-N | ||
| CAS number | 205254-94-0 | molecular formula | C27H27N5O4 |
| molecular weight | 485.53 g/mol | Exact mass | - |
| PSA | 89.100 Ų | logp | 4.100 |
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