上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
CEP-28122
CEP-28122是一种高度有效的选择性ALK抑制剂, IC50值为1.9 ± 0.5 nM。
CEP-28122 Chemical Structure
CAS No. : 1022958-60-6
规格 | 是否有货 | ||
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100 mg | 询价 | ||
250 mg | 询价 | ||
500 mg | 询价 |
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CEP-28122 的其他形式现货产品:
生物活性 |
CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay. IC50 value: 1.9 ± 0.5 nM Target: ALK in vitro: CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 with IC50 of 46 ±10 nM. CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells. [1] in vivo: CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher. [1] |
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分子量 |
539.07 |
Formula |
C28H35ClN6O3 |
CAS 号 |
1022958-60-6 |
运输条件 |
Room temperature in continental US; may vary elsewhere. |
储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
参考文献 |
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