| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S81116-5mg |
99.63% | ￥200.00 |
8 | - | - | - | - |
|
S81116-10mg |
≥98% | ￥360.00 |
货期：2-3天 | - | - | - | - |
|
S81116-25mg |
99.63% | ￥850.00 |
2 | - | - | - | - |
|
| 产品描述： | NVP-HSP990 is a potent, selective and orally active Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively. | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | HSP90α：0.6 nM (IC50)；HSP90β：0.8 nM (IC50)；GRP94：8.5 nM (IC50)；TRAP1 ATPase：320 nM (IC50);Apoptosis; HSP | ||||||||||||||||||||
| 体内研究： | NVP-HSP990 (2.5 to 5 mg/kg twice weekly, or 5 to 15 mg/kg weekly, p.o.) causes dose proportional antitumor efficacy, without obvious loss or overt signs of toxicity in a GTL-16 tumor bearing mice. NVP-HSP990 (5 or 10 mg/kg weekly, p.o.) also results in significant inhibition of tumor growth in BT-474 breast cancer model. NVP-HSP990 (5 mg/kg twice weekly or 15 mg/kg weekly, p.o.) inhibits the growth of tumor in the MV4;11 xenograft model. Furthermore, NVP-HSP990 (0.5 mg/kg every day, 14, 5 mg/kg twice weekly, or 15 mg/kg weekly, p.o.) displays antitumor efficacy in H1975 and A549 tumor models. NVP-HSP990 (5, 15 mg/kg, p.o.) shows prolonged suppression of c-Met levels with 30% and 50% reduction and exhibits antitumor activities in GTL-16 tumor xenograft | ||||||||||||||||||||
| 参考文献： | 1. Menezes DL, et al. The novel oral Hsp90 inhibitor NVP-HSP990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo. Mol Cancer Ther. 2012 Mar;11(3):730-9. 2. McBride CM, et al. Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990. J Med Chem. 2014 Nov 13;57(21):9124-9. 3. Lamottke B, et al. The novel, orally bioavailable HSP90 inhibitor NVP-HSP990 induces cell cycle arrest and apoptosis in multiple myeloma cells and acts synergistically with melphalan by increased cleavage of caspases. Eur J Haematol. 2012 May;88(5):406-15. | ||||||||||||||||||||
| 溶解性： | DMSO : ≥ 33 mg/mL (86.98 mM) | ||||||||||||||||||||
| 保存条件： | 2-8℃ | ||||||||||||||||||||
| 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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