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angelhunte铁杆木虫 (正式写手)
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[求助]
辉瑞新上市的新药crizotinib的ALK酶抑制率是多少，如果有文献会追加100金币
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辉瑞新上市的新药crizotinib的ALK酶抑制率是多少，如果有文献会追加100金币 |
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- FDA批准辉瑞的XALKORI(Crizotinib)
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4楼2012-09-18 16:41:24
songxiangen
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痴夷子皮: 金币+1, 谢谢交流，欢迎常来哦。 2012-09-20 08:32:53
感谢参与，应助指数 +1
痴夷子皮: 金币+1, 谢谢交流，欢迎常来哦。 2012-09-20 08:32:53
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Crizotinib (PF-02341066) 的生物活性 Inhibitor of the catalytic activity of c-Met kinase and the NPM-ALK(nucleophosmin-anaplastic lymphoma kinase) fusion protein.[1] A t(2;5) chromosomal translocation resulting in expression of an oncogenic kinase fusion protein known as NPM-ALK has been implicated in the pathogenesis of anaplastic large-cell lymphoma (ALCL). [2] After incubation with Crizotinib (PF-02341066), cells were washed once with HBSS supplemented with 1 mmol/L Na3VO4 and protein lysates were generated. Subsequently, phosphorylation of ALK was assessed by a sandwich ELISA method using an immobilized anti–total-ALK antibody and an anti–phospho-ALK antibody (pY1604) as a detec ion antibody. Crizotinib (PF-02341066) inhibited NPM-ALKphosphorylation in Karpas299 or SU-DHL-1 ALCL cells (mean IC50 value=24 nM). Crizotinib (PF-02341066) potently inhibited cell proliferation, which was associated with G1-S–phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells (IC50 values=30 nM) but not ALK-negative lymphoma cells. The induction of apoptosis was confirmed using terminal deoxyribonucleotide transferase–mediated nick-end labeling and Annexin V staining (IC50 values=25–50 nM). [3] Crizotinib (PF-02341066) 参考文献 [1] Blood 2005;105: 2640-2653 [2] Oncogene 2001;20:5623-5637 [3] Mol Cancer Ther 2007;6:3314-3322 不知道对楼主有没有用 |
2楼2012-09-18 11:35:33
angelhunte
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细胞活性，我要的是酶活性，有报道说小于1nM,但不知道具体数据 3楼2012-09-18 15:02:27
5楼2012-09-18 16:49:33
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