| 货号 | 5111/50 |
| 别名 | 2-[[2-[[1-[(Dimethylamino)ethanoyl] |
| 供应商 | Tocris |
| 生物活性 | Potent insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) inhibitor (IC50 values are 1.6 and 2 nM, respectively). Also inhibits anaplastic lymphoma kinase (ALK) (IC50 = 0.5 nM). Displays > 800-fold selectivity for IR, IGFR1 and ALK over a panel of 44 kinases including JNK. Blocks proliferation of cancer cell lines in vitro, and causes complete regression of ALK-dependent tumors in vivo. Orally bioavailable. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 532.57 |
| 分子式 | C27H29FN8O3< |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| 参考文献 | Gaoet al (2014) Site-specific activation of AKT protects cells from death induced by glucose deprivation. Oncogene 33 745. PMID: 23396361. Chamberlainet al (2009) Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg.Med.Chem.Lett. 19 360. PMID: 19071018. Sabbatiniet al (2009) GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol.Cancer.Ther. 8 2811. PMID: 19825801. |