| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S80335-5mg |
≥98% | ￥332.00 |
10 | - | - | - | - |
|
S80335-25mg |
≥98% | ￥550.00 |
4 | - | - | - | - |
|
S80335-50mg |
≥98% | ￥832.00 |
1 | - | 2 | - | - |
|
S80335-100mg |
≥98% | ￥1540.00 |
货期：3-5天 | - | - | - | - |
|
| 产品描述： | Crizotinib (PF-02341066) hydrochloride (Xalkori) 可抑制 c-Met 和核磷脂(NPM)-anaplastic lymphoma kinase (ALK) 的酪氨酸磷酸化，对应基于细胞的测定中的IC50值分别为 11 nM 和 24 nM。Crizotinib hydrochloride 也是一种有效的 ROS1 的抑制剂，Ki值小于0.025 nM。Crizotinib 可通过抑制多种肺癌细胞系中的STAT3途径诱导自噬 | ||||||||||||||||||||
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| 靶点： | ROS1(Cell-free assay):<0.025 nM(Ki); c-Met(Cell-based assay):11 nM;NPM-ALK(Cell-based assay):24 nM;c-Met/HGFR;ROS;ALK;Autophagy;ROSKinase | ||||||||||||||||||||
| 体内研究： | In the GTL-16 model, PF-2341066 reveals the ability to cause marked regression of large established tumors (>600 mm3) in both the 50 mg/kg/day and 75 mg/kg/day treatment cohorts, with a 60% decrease in mean tumor volume over the 43-day administration schedule. In an another study, PF-2341066 displays the ability to completely inhibits GTL-16 tumor growth for >3 months, with only 1 of 12 mice exhibiting a significant increase in tumor growth over the 3-month treatment schedule at 50 mg/kg/day. In the NCI-H441 NSCLC model, a 43% decrease in mean tumor volume is observed at 50 mg/kg/day during the 38-day PF-2341066 administration cycle. In the Caki-1 RCC model, a 53% decrease in mean tumor volume is observed to be associated with decreased volume of each tumor by at least 30% at 50 mg/kg/day during the 33-day PF-2341066 administration cycle. PF-2341066 also reveals near-complete prevention of the growth of established tumors at 50 mg/kg/day in the U87MG glioblastoma or PC-3 prostate carcinoma xenograft models, with 97% or 84% inhibition on the final study day, respectively. In contrast, PF-2341066 p.o. given at 50 mg/kg/day does not significantly inhibit tumor growth in the MDA-MB-231 breast carcinoma model, or the DLD-1 colon carcinoma model. A significant dose-dependent reduction of CD31–positive endothelial cells is observed at 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day in GTL-16 tumors, indicating that inhibition of MVD shows a dose-dependent correlation to antitumor efficacy. PF-2341066 displa | ||||||||||||||||||||
| 细胞实验： | Cell lines: GTL-16 gastric carcinoma cells and T47D breast carcinoma cells Concentrations: 0-256 nM Incubation Time: 1 h Method: Cells including GTL-16 gastric carcinoma cells and T47D breast carcinoma cells are seeded in 96-well plates in media supplemented with 10% fetal bovine serum (FBS) and transferred to serum-free media [with 0.04% bovine serum albumin (BSA)] after 24 hours. In experiments investigating ligand-dependent RTK phosphorylation, corresponding growth factors are added for up to 20 minutes. After incubation of cells with PF-2341066 for 1 hour and/or appropriate ligands for the designated times, cells are washed once with HBSS supplemented with 1 mM Na3VO4, and protein lysates are generated from cells. Subsequently, phosphorylation of selected protein kinases is assessed by a sandwich ELISA method using specific capture antibodies used to coat 96-well plates and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates are (a) incubated in the presence of p | ||||||||||||||||||||
| 动物实验： | Animal Models: Female or male nu/nu mice bearing NCI-H441,or DLD-1, or MDA-MB-231 Dosages: 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day Administration: p.o. | ||||||||||||||||||||
| 参考文献： | 1. Helen Y Zou, et al. Cancer Res. 2007 May 1;67(9):4408-17. 2. Helen Y Zou, et al. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8. 3. Liangkun You, et al. Oncotarget. 2015 Nov 24;6(37):40268-82. 4. Zou HY, et al. Cancer Res. 2007, 67(9), 4408-4417. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO、Ethanol、H2O | ||||||||||||||||||||
| 保存条件： | -20°C;充氩 | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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