| 货号 | 15552-50mg |
| 描述 | CCT137690 is a potent inhibitor of Aurora kinases (IC50s = 15, 25 and 19 nM for Aurora A, B, and C, respectively).1 It also inhibits the receptor tyrosine kinase FLT3 as well as the constitutively active form of FLT3 bearing internal-tandem duplications (FLT3-ITD; IC50s = 1.2 and 4.9 nM, respectively).1 CCT137690 is orally bioavailable, inhibiting the growth of SW620 colon carcinoma xenografts in mice without inducing body weight loss.1 It blocks signaling through Aurora kinases in MYCN-amplified neuroblastoma cells, suppressing N-Myc expression and preventing proliferation.2 It inhibits growth of FLT3-ITD cells harboring a D835Y mutation, which confers resistance to other FLT3 inhibitors.3 CCT137690 also sensitizes colorectal carcinoma cells to radiotherapy.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bavetsias, V.,Crumpler, S.,Sun, C., et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: Identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. Journal of Medicinal Chemistry 55(20), 8721-8734 (2012). 2.Faisal, A.,Vaughan, L.,Bavetsias, V., et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Molecular Cancer Therapeutics 10(11), 2115-2123 (2011). 3.Moore, A.S.,Faisal, A.,Gonzalez de Castro, D., et al. Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns. Leukemia 26(7), 1462-1470 (2012). 4.Wu, X.,Liu, W.,Cao, Q., et al. Inhibition of Aurora B by CCT137690 sensitizes colorectal cells to radiotherapy. J.Exp.Clin.Cancer Res. 33, 1-9 (2014). | |
| 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 | 551.5 |
| 分子式 | C26H31BrN8O |
| CAS号 | 1095382-05-0 |
| 稳定性 | ≥ 2 years |
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