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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-HIF/HIF Prolyl-hydroxylase-Belzutifan
Belzutifan

Chemical Structure : Belzutifan

CAS No.: 1672668-24-4

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Belzutifan (PT2977, MK-6482, MK6482, PT-2977)

货号: PC-72737Not For Human Use, Lab Use Only.

Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay).

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5 mg ￥1280 In stock
10 mg ￥1880 In stock
25 mg ￥3280 In stock
50 mg ￥5280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay).
PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells.
PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model
In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.

物理化学性质&存储条件

分子量 383.341
分子式 C17H12F3NO4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

100 mM in DMSO (38.2 mg/mL)
Chemical Name/SMILES

3-(((1S,2S,3R)-2,3-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile

参考文献

1. Choueiri TK, et al. Nat Med. 2021 May;27(5):802-805.

2. Xu R, et al. J Med Chem. 2019 Aug 8;62(15):6876-6893.

3. Jonasch E, et al. N Engl J Med. 2021 Nov 25;385(22):2036-2046.

4. Kamihara J, et al. N Engl J Med. 2021 Nov 25;385(22):2059-2065.

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