| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S85209-5mg促销 |
≥98% | ￥280.00 ￥252.00 |
5 | - | - | - | - |
|
S85209-10mg促销 |
≥98% | ￥376.00 ￥338.00 |
7 | - | - | - | - |
|
S85209-25mg促销 |
≥98% | ￥500.00 ￥450.00 |
6 | - | - | - | - |
|
S85209-50mg促销 |
≥98% | ￥800.00 ￥720.00 |
2 | - | - | - | - |
|
S85209-100mg促销 |
≥98% | ￥1590.00 ￥1430.00 |
1 | - | - | - | - |
|
S85209-250mg促销 |
≥98% | ￥3960.00 ￥3560.00 |
1 | - | - | - | - |
|
| 产品描述： | CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities | ||||||||||||||||||||
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| 靶点： | ErbB2:10 nM (IC50);Apoptosis;EGFR | ||||||||||||||||||||
| 体内研究： | CP-724714 (3.25-100 mg/kg; p.o.; 0.5-8 hours) results in a concentration-dependent reduction of ErbB2 receptor phosphorylation. CP-724714 (6.25-100 mg/kg; p.o.; q.d; for 8 to 40 day) inhibits FRE-erbB2 xenograft growth. CP-724714 (Athymic, female FRE-erbB2 xenograft-bearing mice; 30 or 100 mg/kg; p.o.) treatments results in a time- and dose- dependent induction of apoptosis, which was evident as early as 4 to 8 h after dosing. Approximately 75% more tumor cells exhibited apoptotic changes in the 100 mg/kg treatment group compared with vehicle control group at 8 h after dosing. CP-724714 induces regression of BT-474 tumors and significant inhibition in a number of other human tumor xenografts. Additionally, CP-724714 showed a favorable nonclinical toxicity profile with no apparent effects on cardiac tissue Animal Model: Female athymic mice (bearing FRE-erbB2 xenografts) Dosage: 3.25-100 mg/kg Administration: P.o.; 0.5-8 hours Result: Produced a reduction of erbB2 tyrosine phosphorylation in FRE-erbB2 xenografts. | ||||||||||||||||||||
| 参考文献： | 1. Jani JP, et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res, 2007, 67(20), 9887-9893. 2. Feng B, et al. Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicol Sci, 2009, 108(2), 492-500. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 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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