產(chǎn)品目錄

規(guī)格	1mg
CAS	558640-51-0
別名
化學(xué)名	3-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide
分子式	C19H18ClN3O4
分子量	387.82
溶解度	Soluble 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：

VER-49009 is a potent and selective inhibitor of HSP90 with IC50 value of 47 nM for HSP90β [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.

VER-49009 is a potent HSP90 inhibitor. VER-49009 inhibited recombinant yeast Hsp90 ATPase activity with IC50 value of 167 nM at 400 μM ATP and inhibited recombinant human HSP90β with IC50 value of 1033 nM in the presence of the activator AHA1. Also, VER-49009 bound to recombinant human HSP90β with Kd value of 78.0 nM. In human cancer cells, VER-49009 exhibited antiproliferative activity with mean GI50 value of 685 nM. In HT29 cells, VER-49009 exhibited extensive glucuronidation and increased glucuronide levels by 230-fold, which were responsible for the resistance. In CH1doxR cells that were resistant to doxorubicin, VER-49009 exhibited similar cellular GI50 value compared with CH1 cells. In HCT116 colon cancer cells, VER-49009 caused G1 and G2-M block [1].

In athymic mice bearing OVCAR3 human ovarian ascites tumors, VER-49009 completely inhibited ERBB2 [1].

特別提醒：

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

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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