Ponatinib
货号：
11494-1mg 基本售价：
406.0 元 规格：
1 mg
产品信息
概述| 货号 | 11494-1mg |
| 描述 | Ponatinib is an orally available, pan-Bcr-Abl tyrosine kinase inhibitor developed for the treatment of an advanced phase of chronic myeloid leukemia in which mutations of the kinase endow resistance to other Bcr-Abl inhibitors.1 Ponatinib potently inhibits native Bcr-Abl (IC50 = 0.37 nM) as well as various clinically important mutant forms including Bcr-AblT315I (IC50 = 2 nM).1 It can also inhibit c-Src (IC50 = 5.4 nM) and VEGFR, FGFR, and PDGFR receptor tyrosine kinases (IC50s = 1-2 nM), yet is >1,000-fold selective against family members of Aurora kinase, insulin receptor kinase, or cyclin-dependent kinase.1 Ponatinib has been shown to inhibit proliferation of Ba/F3 cells expressing native (IC50 = 0.5 nM) or mutant (IC50s = 0.5-36 nM) Bcr-Abl by inducing apoptosis.1 In a Ba/F3 Bcr- AblT315I xenograft model, tumor growth was inhibited in mice upon oral dosing at 10-30 mg/kg.1 |
| 别名 | AP 24534;Iclusig; |
性能| 供应商 | Cayman |
| 应用文献 |
1.OHare, T.,Shakespeare, W.C.,Zhu, X., et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 16(5), 401-412 (2009).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 532.6 |
| 分子式 | C29H27F3N6O |
| CAS号 | 943319-70-8 |
| 稳定性 | ≥ 2 years |
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