化学性质:
规格 | 1mg |
CAS | 558640-51-0 |
别名 |
|
化学名 | 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 |
储存条件 | 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 |
产品描述:
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].
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
标签:VER-49009
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