| 查看: 1526 | 回复: 8 | ||
| 当前只显示满足指定条件的回帖，点击这里查看本话题的所有回帖 | ||
angelhunte铁杆木虫 (正式写手)
菜鸟
|
[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
|
|
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 |
回复此楼» 猜你喜欢
多聚组氨酸，大分子量
已经有657人回复
-
胰岛素的实验室表达
已经有0人回复
-
药理学论文润色/翻译怎么收费?
已经有144人回复
-
胰岛素的实验室表达
已经有0人回复
-
胰岛素的实验室表达
已经有0人回复
-
胰岛素的实验室表达
已经有1人回复
-
胰岛素的实验室表达
已经有0人回复
-
胰岛素的实验室表达
已经有0人回复
-
求助电子版：晶型药物研发理论与应用
已经有0人回复
-
北京大学药学院诚招药物化学/有机化学方向博士后
已经有5人回复
» 本主题相关价值贴推荐，对您同样有帮助:
- FDA批准辉瑞的XALKORI(Crizotinib)
已经有5人回复
angelhunte
铁杆木虫 (正式写手)
菜鸟
- 应助: 2 (幼儿园)
- 金币: 6867.1
- 散金: 10
- 红花: 3
- 帖子: 382
- 在线: 70.7小时
- 虫号: 763601
- 注册: 2009-05-05
- 专业: 药物化学
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
songxiangen
金虫 (小有名气)
- 应助: 2 (幼儿园)
- 金币: 1041.8
- 帖子: 147
- 在线: 43.8小时
- 虫号: 329792
- 注册: 2007-03-23
- 性别: GG
- 专业: 有机合成
【答案】应助回帖
★
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
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
|
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
4楼2012-09-18 16:41:24
5楼2012-09-18 16:49:33
