產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 25mg 100mg
CAS	934343-74-5
別名
化學名	(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.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術有限公司

在線咨詢

留言注意事項：

1.遵守中華人民共和國有關法律、法規(guī)，尊重網(wǎng)上道德，承擔一切因您的行為而直接或間接引起的法律責任。

2.請您真實的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對產(chǎn)品有任何疑問,也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個人或團體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細地址*
常用郵箱*
請輸入您對我們的意見或建議*
驗證碼*