[CAS NO. 1672668-24-4] Belzutifan

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PRODUCTS SPECIFICATIONS [1672668-24-4]

Catalog

HY-125840

Brand

MCE

CAS

1672668-24-4

DESCRIPTION [1672668-24-4]

Overview

MDL	MFCD32197212
Molecular Weight	383.34
Molecular Formula	C17H12F3NO4S
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

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC ₅₀ of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) ^[1] .

IC50 & Target

IC50: 9 nM (HIF-2α) ^[1]

In Vitro

Belzutifan (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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04995484	Merck Sharp & Dohme LLC	Moderate Hepatic Impairment	June 24, 2022	Phase 1
NCT04195750	Merck Sharp & Dohme LLC	Carcinoma, Renal Cell	February 27, 2020	Phase 3
NCT04586231	Merck Sharp & Dohme LLC\|Eisai Inc.	Carcinoma, Renal Cell	February 25, 2021	Phase 3
NCT04627064	Dana-Farber Cancer Institute\|Eli Lilly and Company	Clear Cell Renal Cell Carcinoma	December 31, 2020	Phase 1
NCT03634540	Peloton Therapeutics, Inc.	Renal Cell Carcinoma (RCC)\|Clear Cell Renal Cell Carcinoma (ccRCC)\|Kidney Cancer\|Renal Cancer\|Renal Cell Carcinoma\|Renal Cell Cancer Metastatic\|Renal Cell Carcinoma Recurrent\|Renal Cell Cancer, Recurrent\|Kidney	September 27, 2018	Phase 2
NCT04846920	Merck Sharp & Dohme LLC	Carcinoma, Renal Cell	June 14, 2021	Phase 1
NCT05030506	Merck Sharp & Dohme LLC	Renal Cell Carcinoma	October 13, 2021	Phase 1
NCT04924075	Merck Sharp & Dohme LLC	Pheochromocytoma+Paraganglioma\|Pancreatic Neuroendocrine Tumor\|Von Hippel-Lindau Disease	August 12, 2021	Phase 2
NCT04489771	Merck Sharp & Dohme LLC	Carcinoma, Renal Cell	September 13, 2020	Phase 2
NCT04626518	Merck Sharp & Dohme LLC	Carcinoma, Renal Cell	December 17, 2020	Phase 1\|Phase 2
NCT04976634	Merck Sharp & Dohme LLC	Carcinoma, Hepatocellular\|Colorectal Neoplasms\|Pancreatic Ductal Adenocarcinoma\|Biliary Tract Neoplasms\|Endometrial Neoplasms\|Esophageal Neoplasms	August 18, 2021	Phase 2
NCT02974738	Peloton Therapeutics, Inc.	Advanced Solid Tumors\|Solid Tumor\|Solid Carcinoma\|Solid Tumor, Adult\|ccRCC\|RCC, Clear Cell Adenocarcinoma\|RCC\|Kidney Cancer\|Clear Cell Renal Cell Carcinoma\|Renal Cell Carcinoma, Metastatic\|Renal Cell Carcinoma Recurrent\|Renal Cell Carcinoma, Clear Cell Adenocarcinoma\|Glioblastoma\|Glioblastoma, Adult\|GBM\|Glioblastoma Multiforme	December 7, 2016	Phase 1
NCT03445169	Peloton Therapeutics, Inc.	Healthy	February 23, 2018	Phase 1
NCT04994522	Merck Sharp & Dohme LLC	End Stage Renal Disease\|Renal Impairment	July 12, 2022	Phase 1
NCT05468697	Merck Sharp & Dohme LLC	Renal Cell Carcinoma	August 10, 2022	Phase 1\|Phase 2
NCT03401788	Peloton Therapeutics, Inc.	VHL - Von Hippel-Lindau Syndrome\|VHL Gene Mutation\|VHL Syndrome\|VHL Gene Inactivation\|VHL-Associated Renal Cell Carcinoma\|VHL-Associated Clear Cell Renal Cell Carcinoma	May 2, 2018	Phase 2
NCT04736706	Merck Sharp & Dohme LLC\|Eisai Inc.	Carcinoma, Renal Cell	April 14, 2021	Phase 3
NCT04626479	Merck Sharp & Dohme LLC	Carcinoma, Renal Cell	December 16, 2020	Phase 1\|Phase 2
NCT05239728	Merck Sharp & Dohme LLC	Clear Cell Renal Cell Carcinoma	March 15, 2022	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 130.43 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6087 mL	13.0433 mL	26.0865 mL
5 mM	0.5217 mL	2.6087 mL	5.2173 mL
10 mM	0.2609 mL	1.3043 mL	2.6087 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
4.

Add each solvent one by one: 1% DMSO >> 99% saline

Solubility: ≥ 0.5 mg/mL (1.30 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[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.