| 货号 | 12076-5mg |
| 描述 | The HER family of receptor tyrosine kinases, EGFR, HER2, HER3, and HER4, mediate proliferation, migration, adhesion, differentiation, and survival in many different cell types and have been implicated in the development and progression of a variety of human tumors.1 Canertinib is an irreversible quinazoline-based HER family tyrosine kinase inhibitor with IC50 values of 0.8, 19, and 7 nM for blocking in vitro activity of EGFR, HER2, and HER4, respectively.1 As a broadly applicable anti-cancer agent, it has been used to suppress proliferation of malignant peripheral nerve sheath tumor cells (effective concentration of 250-500 nM), to inhibit growth and induce dose-dependent apoptosis in a panel of neuroblastoma cell lines (IC50s = 0.94-2.45 μM), and to reduce proliferation of acute myeloid leukemia cells (IC50 = 0.27 μM).2,3,4 Canertinib also displays anti-neoplastic activity towards T98G glioblastoma cells, HCT8 colorectal carcinoma cells, and cells expressing the breast cancer resistance protein.5 |
| 别名 | CI-1033;PD 183805; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Arkin, M., and Moasser, M.M. HER2 directed small molecule antagonists. Curr.Opin.Investig.Drugs 9(12), 1264-1276 (2008). 2.Dilworth, J.T.,Wojtkowiak, J.W.,Mathieu, P., et al. Suppression of proliferation of two independent NF1 malignant peripheral nerve sheath tumor cell lines by the pan-ErbB inhibitor Cl-1033. Cancer Biology and Therapy 7(12), 1938-1946 (2008). 3.Richards, K.N.,Zweidler-McKay, P.A.,Van Roy, N., et al. Signaling of ERBB receptor tyrosine kinases promotes neuroblastoma growth in vitro and in vivo. Cancer 116(13), 3233-3243 (2010). 4.Nordigården, A.,Zetterblad, J.,Trinks, C., et al. Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice. British Journal of Haematology 155, 198-208 (2011). 5.Erlichman, C.,Boerner, S.A.,Hallgren, C.G., et al. The HER tyrosine kinase inhibitor CI1033 enhances cytotoxicity of 7-ethyl-10-hydroxycamptothecin and topotecan by inhibiting breast cancer resistance protein-mediated drug efflux. Cancer Research 61, 739-748 (2001). | |
| 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 | 558.9 |
| 分子式 | C24C25ClFN5O3 • 2HCl |
| CAS号 | 289499-45-2 |
| 稳定性 | ≥ 2 years |
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