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PT-2385
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PT-2385图片
CAS NO: 1672665-49-4
包装与价格:
包装 价格(元)
10mM (in 1mL DMSO) 电议
2mg 电议
5mg 电议
10mg 电议
50mg 电议
100mg 电议

半岛bd体育手机客户端 介绍
PT-2385是选择性HIF-2α拮抗剂,Ki值小于50nM。
Cas No. 1672665-49-4
Canonical SMILES N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C)=O)C3=C2CC(F)(F)[C@H]3O)=C1
分子式 C17H12F3NO4S
分子量 383.34
溶解度 DMSO : ≥ 50 mg/mL (130.43 mM)
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
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

PT-2385 is a selective HIF-2α antagonist with a Ki of less than 50 nM.

PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α[1].

PT-2385 (PT2385) inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT-2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT-2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT-2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31)[1].

[1]. Eli Wallace, Ph.D. PT2385: HIF-2α Antagonist for the Treatment of VHL Mutant ccRCC. 12th International VHL Medical Symposium April 8, 2016. [2]. Xie C, et al. Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis. Nat Med. 2017 Nov;23(11):1298-1308.

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