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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-NVP-HSP990
NVP-HSP990

Chemical Structure : NVP-HSP990

CAS No.: 934343-74-5

NVP-HSP990 (HSP990)

货号: PC-21200Not For Human Use, Lab Use Only.

NVP-HSP990 (HSP990) is a potent, selective, oral and brain-penetrant Hsp90 inhibitor with IC50 of 0.6, 0.8 and 8.5 nM for Hsp90α, Hsp90β and Grp94, respectively.

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25 mg ¥1880 In stock
50 mg ¥2980 In stock
100 mg ¥4880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NVP-HSP990 (HSP990) is a potent, selective, oral and brain-penetrant Hsp90 inhibitor with IC50 of 0.6, 0.8 and 8.5 nM for Hsp90α, Hsp90β and Grp94, respectively.
NVP-HSP990 inhibits TRAP1 ATPase activity with IC50 of 320 nM, binds to the N-terminal ATP-binding domain of Hsp90.
NVP-HSP990 does not show significant binding or functional activities against a panel of 83 diverse receptors/enzymes involved in major physiologic functions.
NVP-HSP990 induces a signature response of Hsp90 inhibition and inhibits growth of a wide range of tumor cells.
NVP-HSP990 (5 mg/kg twice weekly or 15 mg/kg weekly) demonstrates antitumor efficacy in the GTL-16 gastric cancer model.

物理化学性质&存储条件

分子量 379.40
分子式 C20H18FN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(7R)-2-amino-7-[4-fluoro-2-(6-methoxy-2-pyridinyl)phenyl]-7,8-dihydro-4-methyl-pyrido[4,3-d]pyrimidin-5(6H)-one

参考文献

1. Centenera MM, et al. Clin Cancer Res. 2012 Jul 1;18(13):3562-70.

2. Menezes DL, et al. Mol Cancer Ther. 2012 Mar;11(3):730-9.

3. Jackrel ME, et al. J Clin Invest. 2011 Aug;121(8):2972-5.

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