Belzutifan | HIF2α inhibitor | Probechem Biochemicals

Chemical Structure : Belzutifan

CAS No.: 1672668-24-4

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

Catalog No.: 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).

Packing	Price	Stock
5 mg	$128	In stock
10 mg	$188	In stock
25 mg	$328	In stock
50 mg	$528	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	383.341
Formula	C17H12F3NO4S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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

References

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.

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

Biological Activity

Physicochemical Properties

References

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