產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號(hào) | 型號(hào) |
HSP990 (NVP-HSP990) | 10mM (in 1mL DMSO) 5mg 25mg 100mg | 934343-74-5 | EY-Y0164718 |
Cas No.934343-74-5
別名
化學(xué)名 (7R)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one
分子式 C20H18FN5O2
分子量 379.39
溶解度 ≥ 12.3mg/mL in DMSO
儲(chǔ)存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
HSP990 (NVP-HSP990) is a potent and selective inhibitor of HSP90 with IC50 values of 0.6, 0.8 and 8.5 nM for Hsp90α, Hsp90β and Grp94, respectively [1].
Heat shock protein 90 (HSP90) is a chaperone protein that stabilizes proteins against heat stress, assists proteins to fold properly and aids in protein degradation. Also, HSP90 stabilizes proteins required for tumor growth.
HSP990 (NVP-HSP990) is a potent and selective HSP90 inhibitor. NVP-HSP990 bound to the N-terminal ATP-binding domain of Hsp90. NVP-HSP990 inhibited TRAP1 ATPase activity by 90% with IC50 value of 320 nM. In GTL-16 cells, NVP-HSP990 destabilized the Hsp90-p23 complex in a concentration- and time-dependent way. Also, NVP-HSP990 decreased c-Met with EC50 value of 37 nM and induced Hsp70 with EC50 value of 20 nM. NVP-HSP990 inhibited ERK and AKT phosphorylation with EC50 values of 11 and 6 nM respectively and thus inhibited ERK and AKT activation. In five human tumor cell lines, NVP-HSP990 inhibited cell growth with GI50 values of 4-40 nM [1]. In glioma tumor-initiating cells, NVP-HSP990 inhibited cell growth with IC50 value of 10-500 nM in a dose-dependent way and reduced CDK2 and CDK4, thus disrupting cell-cycle control [2].
In the GTL-16 gastric cancer mice model, NVP-HSP990 exhibited antitumor efficacy [1].
References:
[1]. Menezes DL, Taverna P, Jensen MR, 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, 11(3): 730-739.
[2]. Fu J, Koul D, Yao J, et al. Novel HSP90 inhibitor NVP-HSP990 targets cell-cycle regulators to ablate Olig2-positive glioma tumor-initiating cells. Cancer Res, 2013, 73(10): 3062-3074.
關(guān)鍵字： 934343-74-5;C20H18FN5O2;HSP990 (NVP-HSP990);
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來，秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念，立足生物科技領(lǐng)域，運(yùn)用生物技術(shù)和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機(jī)構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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