PT2399
PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo[1][2][3].
Product Specifications
CAS Number
1672662-14-4
UNSPSC
12352005
Target
HIF/HIF Prolyl-Hydroxylase
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/pt2399.html
Purity
99.96
Solubility
DMSO : ≥ 200 mg/mL
Smiles
N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C(F)F)=O)C3=C2CC(F)(F)[C@H]3O)=C1
Molecular Formula
C17H10F5NO4S
Molecular Weight
419.32
References & Citations
[1]Chen W, et al. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539 (7627) :112-117.|[2]Cho H, et al. On-Target Efficacy of a HIF2α Antagonist in Preclinical Kidney Cancer Models. Nature. Nature. 2016 Nov 3;539 (7627) :107-111.|[3]Wehn PM, et al. Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S) -3- ((2,2-Difluoro-1-hydroxy-7- (methylsulfonyl) -2,3-dihydro-1 H-inden-4-yl) oxy) -5-fluorobenzonitrile (PT2385) . J Med Chem. 2018 Nov 8;61 (21) :9691-9721.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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