PT2399 (Standard)
PT2399 (Standard) is the analytical standard of PT2399 (HY-108697). This product is intended for research and analytical applications. PT2399 is a selective and orally active HIF-2α antagonist (IC50 < 5 nM) that binds the PAS-B domain and disrupts HIF-2α-ARNT heterodimerization. PT2399 inhibits HIF-2α-driven transcription, destabilizes HIF-2α, and suppresses HIF target genes without inhibiting HIF1α. PT2399 reduces tumor cell proliferation, vessel area, circulating tumor-derived VEGFA/VEGF, and lactate while increasing pyruvate. PT2399 can be used for research on clear cell renal cell carcinoma and chronic myeloid leukemia (CML).
For research use only. We do not sell to patients.
- CAS No.: 1672662-14-4
- Formula: C17H10F5NO4S
- Molecular Weight:419.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Product Information
Information
Application
The compound is the grade of analytical standard, which is the reference standard supplied assay. It is commonly used in qualitative, quantitative and methodological research experiments in HPLC, GC and MS.
Chemical Information
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CAS No. 1672662-14-4
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Molecular Weight 419.32
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Formula C17H10F5NO4S
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SMILES
N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C(F)F)=O)C3=C2CC(F)(F)[C@H]3O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Chen W, et al. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539(7627):112-117. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)