General
Preferred name
PT2399
Synonyms
(s)-10f ()
PT-2399 ()
P&D ID
PD121874
CAS
1672662-14-4
Tags
available
probe
Probe info
Probe type
experimental probe
Probe sources
Chemical Probes.org
High-quality chemical probes
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT Off-target activity is suggested based on the anti-proliferative activity in cells lacking HIF-2α. It would be helpful if an off-target (e.g. GPCR/kinase panel) was performed. Sep 24 2020 - 9:52am
DESCRIPTION PT2399 is a potent and selective HIF-2¦Á antagonist, which directly binds to HIF-2¦Á PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo[1][2][3].
PRICE 331
DESCRIPTION PT2399 is a first-in-class, orally available, small molecule inhibitor of HIF-2 that selectively disrupts the heterodimerization of HIF-2?? with HIF-1??. PT2399 displays potent antitumor activity in vivo
MOA Antagonist (Chemical Probes.org)
DESCRIPTION PT2399 is a first-in-class, orally available, small molecule inhibitor of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. PT2399 displays potent antitumor activity in vivo (TargetMol Bioactive Compound Library)
Compound Sets
7
Chemical Probes.org
pt2399
High-quality chemical probes
PD121874
Mcule NIBR MoA Box Subset
MCULE-1475829713
MedChem Express Bioactive Compound Library
HY-108697
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
pt2399
TargetMol Bioactive Compound Library
T12675L
External IDs
12
Properties
(calculated by RDKit )
Molecular Weight
419.03
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
2
cLogP
3.71
TPSA
87.39
Fraction CSP3
0.24
Chiral centers
1.0
Largest ring
6.0
QED
0.76
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
HIF-2α
HIF/HIF Prolyl-Hydroxylase
HIF
EPAS1
Member status
member
MOA
HIF2A/EPAS1 inhibitor
Orthogonal probe
PT2385
Pathway
Metabolic Enzyme/Protease
Angiogenesis
Chromatin/Epigenetic
Metabolism
Target class
Transcription factor
Target subclass
Hypoxia-Inducible Factor
Source data