色瑞替尼

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本试剂(色瑞替尼)
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简介：
货 号：LC2-C-2086
名 称：色瑞替尼
别 名：Ceritinib Free Base
C A S ：1032900-25-6
分子量：558.14
分子式：C28H36ClN5O3S
纯 度：HPLC/TLC:>99%
说 明：
文 献：Ceritinib, also known as LDK-378, is a very selective anaplastic lymphoma kinase (ALK) inhibitor. It inhibits ALK with an IC50 of 200 pM. It inhibits kinases IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively and other kinases tested with IC50s of >100 nM. In vivo it displayed efficacy in anaplastic large cell lymphoma (ALCL) and non-small-cell lung cancer (NSCLC) cancer xenograft models at well-tolerated doses. Marsilje T.H., et al. "Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials." J. Med. Chem. 56: 5675-5690 (2013). Non-small-cell lung cancers (NSCLC) harboring ALK gene rearrangements always develop resistance to the ALK tyrosine kinase inhibitor crizotinib. Ceritinib effectively inhibited crizotinib-resistant ALK with L1196M, G1269A, I1171T and S1206Y mutations. However, ceritinib did not overcome two crizotinib-resistant ALK mutations, G1202R and F1174C. Friboulet L., et al. "The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer." Cancer Discov. 4: 662-673 (2014). A phase 1 clinical trial showed ceritinib was highly active in patients with advanced, ALK-rearranged NSCLC. Certinib was also active in patients who had had disease progression during crizotinib treatment regardless of the presence of resistance mutations in ALK. Shaw A.T., et al. "Ceritinib in ALK-rearranged non-small-cell lung cancer." N. Engl. J. Med. 370: 1189-1197 (2014).