CAS NO: | 1672668-24-4 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 1672668-24-4 |
别名 | PT2977; MK-6482 |
Canonical SMILES | N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C)=O)C3=C2[C@@H](F)[C@@H](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, stored under nitrogen |
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 |
产品描述 | PT2977 is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for Clear cell renal cell carcinoma (ccRCC) and von Hippel-Lindau (VHL) disease[1]. IC50: 9 nM (HIF-2α)[1] PT2977 potently and dose-dependently reduces mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, and leads to rapid and dose-dependent reduction in EPO expression[1]. [1]. Xu R, et al. 3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma. J Med Chem. 2019 Aug 8;62(15):6876-6893. |