中文名 | PT2977 |
英文名 | 3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile |
别名 | 贝组替凡 化合物 T16679 PT2977(贝组替凡) 贝组替凡BELZUTIFANPT2977MK6482 3-[[(1S,2S,3R)-2,3-二氟-2,3-二氢-1-羟基-7-(甲基磺酰基)-1H-茚-4-基]氧基]-5-氟苄腈 |
英文别名 | PT2977 MK-6482 Belzutifan PT2977 (MK-6482) Belzutifan (MK-6482) HY-125840 Belzutifan PT2977 Belzutifan (PT2977, MK-6482) 3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile Benzonitrile, 3-[[(1S,2S,3R)-2,3-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro- |
CAS | 1672668-24-4 |
化学式 | C17H12F3NO4S |
分子量 | 383.34 |
密度 | 1.56±0.1 g/cm3(Predicted) |
沸点 | 505.8±50.0 °C(Predicted) |
溶解度 | 溶于DMSO |
酸度系数 | 11.66±0.60(Predicted) |
存储条件 | -20℃ |
产品用途 | Belzutifan, also known as PT2977 and MK-6482, is HIF-2alpha inhibitor. PT2977 binds to and blocks the function of HIF-2alpha, thereby preventing HIF-2alpha heterodimerization and its subsequent binding to DNA. This results in decreased transcription and expression of HIF-2alpha downstream target genes, many of which regulate hypoxic signaling. This inhibits cell growth and survival of HIF-2alpha-expressing tumor cells. HIF-2alpha, the alpha subunit for the heterodimeric transcription factor HIF-2, is overexpressed in many cancers and promotes tumorigenesis. Belzutifan was approved in 2021 for treatment of von Hippel-Lindau disease under certain conditions。 |
参考资料 展开查看 | 1: Garje R, An JJ, Sanchez K, Greco A, Stolwijk J, Devor E, Rustum Y, Zakharia Y.Current Landscape and the Potential Role of Hypoxia-Inducible Factors andSelenium in Clear Cell Renal Cell Carcinoma Treatment. Int J Mol Sci. 2018 Dec1;19(12). pii: E3834. doi: 10.3390/ijms19123834. Review. PubMed PMID: 30513765. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.609 ml | 13.043 ml | 26.086 ml |
5 mM | 0.522 ml | 2.609 ml | 5.217 ml |
10 mM | 0.261 ml | 1.304 ml | 2.609 ml |
5 mM | 0.052 ml | 0.261 ml | 0.522 ml |
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