General
Preferred name
belzutifan
Synonyms
PT2977 ()
MK-6482 ()
CS-0101119MK-6482PT-2977PT2977 ()
Pt 2977 ()
PT-2977 ()
MK6482 ()
Welireg ()
PT 2977 ()
WELIREG ()
P&D ID
PD126131
CAS
1672668-24-4
Tags
available
drug
Approved by
FDA
First approval
2021
Drug indication
Renal cell carcinoma
Von hippel-lindau disease
clear cell renal carcinoma
Solid tumour/cancer
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Belzutifan (PT2977) is an orally active and selective HIF-2¦Á inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2¦Á inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC)[1].
PRICE 193
DESCRIPTION Belzutifan (MK-6482) is a potential treatment for clear cell renal cell carcinoma (ccRCC). Belzutifan is an orally active and selective HIF-2?? inhibitor (IC50: 9 nM). Belzutifan , as a second-generation HIF-2?? inhibitor, increases potency and improves pharmacokinetic profile.
DESCRIPTION Belzutifan (previously PT2977 and MK-6482) binds to and inhibits HIF-2α function, and has been developed as a novel cancer therapeutic . HIF-2α is a transcription factor component that is established as an oncogneic driver of ccRCC, via loss of its interaction with the tumour suppressor von Hippel-Lindau (VHL), which results in disrupted proteasomal degradation and thereby accumulation of HIF-2α. Elevated HIF-2α promotes increased expression of hypoxia-responsive genes which regulate processes including angiogenesis, proliferation, migration, and immune evasion. (GtoPdb)
DESCRIPTION Belzutifan (MK-6482) is a potential treatment for clear cell renal cell carcinoma (ccRCC). Belzutifan is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). Belzutifan , as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. (TargetMol Bioactive Compound Library)
Compound Sets
14
Cayman Chemical Bioactives
39652
ChEMBL Approved Drugs
CHEMBL4585668
ChEMBL Drugs
CHEMBL4585668
DrugBank
DB15463
DrugBank Approved Drugs
DB15463
DrugCentral
5469
DrugCentral Approved Drugs
5469
DrugMAP
DML1KTO
EUbOPEN Chemogenomics Library
EUB0002639
Guide to Pharmacology
11251
MedChem Express Bioactive Compound Library
HY-125840
NIH Approved Oncology Drugs
440799301
ReFrame library
TargetMol Bioactive Compound Library
T16679
External IDs
24
Properties
(calculated by RDKit )
Molecular Weight
383.04
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
3
Aromatic Ring Count
2
cLogP
3.29
TPSA
87.39
Fraction CSP3
0.24
Chiral centers
3.0
Largest ring
6.0
QED
0.88
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
HIF-2α
HIF/HIF Prolyl-Hydroxylase
Pathway
Angiogenesis
Chromatin/Epigenetic
Metabolic Enzyme/Protease
Recommended Cell Concentration
None
Source data