| 货号 | 4274/50 |
| 别名 | 3-(2-Imidazo[1,2-b]pyridazin-3-ylet |
| 供应商 | Tocris |
| 生物活性 | Potent multi-kinase and pan-Bcr-Abl inhibitor. Displays potent activity against cell lines expressing native Bcr-Abl or Bcr-AblT3151(IC50 values are 0.37 and 2.0 nM respectively); also inhibits other Abl kinase domain mutants at nanomolar potencies. Exhibits inhibitory activity against PDGFRα, c-Src and c-Kit (IC50 values are 1.1, 5.4 and 12.5 nM respectively); potently inhibits FGFR and VEGFR family kinases. Orally active. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 532.56 |
| 分子式 | C29H27F3N6 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 50 mM in ethanol |
| 参考文献 | Gozgitet al (2011) Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol.Cancer Ther. 10 1028. PMID: 21482694. Huanget al (2010) Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)-methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-Abelson (BCR-ABL) kinase including the T3151 mutant. J.Med.Chem. 53 4701. PMID: 20513156. O'Hareet al (2009) AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 16 401. PMID: 19878872. |