| 货号 | 18873-1mg |
| 描述 | Crenolanib is an orally bioavailable, selective inhibitor of type III tyrosine kinases with nanomolar potencies against platelet-derived growth factor receptor α (PDGFRα) and PDGFRβ and Fms-related tyrosine kinase 3 (FLT3; IC50s = 11, 3.2, and 4 nM, respectively).1,2 It also inhibits medically-relevant mutant forms of these kinases, including the D842V-containing form of PDGFR and D835Y and internal tandem duplication mutations of FLT3, at nanomolar concentrations.1,3,4 Crenolanib is more than 100-fold selective for these kinases over other tyrosine and serine/threonine kinases. It is effective when used in cells and in vivo.1,2,4 |
| 别名 | CP 868,596; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Heinrich, M.C.,Griffith, D.,McKinley, A., et al. Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clinical Cancer Research 18(16), 4375-4385 (2012). 2.Smith, C.C.,Lasater, E.A.,Lin, K.C., et al. Crenolanib is a selective type I pan-FLT3 inhibitor. Proceedings of the National Academy of Sciences of the United States of America 111(14), 5319-5324 (2014). 3.Dai, J.,Kong, Y.,Si, L., et al. Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib. Clinical Cancer Research 19(24), 6935-6942 (2013). 4.Galanis, A.,Ma, H.,Rajkhowa, T., et al. Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants. Blood 123(1), 94-100 (2014). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 443.5 |
| 分子式 | C26H29N5O2 |
| CAS号 | 670220-88-9 |
| 稳定性 | ≥ 2 years |
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