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PT2399

Catalog No. T12675L   CAS 1672662-14-4

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

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PT2399 Chemical Structure
PT2399, CAS 1672662-14-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 121.00
5 mg In stock $ 297.00
10 mg In stock $ 396.00
25 mg In stock $ 837.00
50 mg In stock $ 1,160.00
100 mg In stock $ 1,560.00
1 mL * 10 mM (in DMSO) In stock $ 336.00
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Purity: 99.07%
Purity: 98.8%
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Biological Description
Chemical Properties
Storage & Solubility Information
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
Targets&IC50 HIF-2α:6 nM
In vitro PT2399, a selective HIF-2 antagonist that was identified using a structure-based design approach.?PT2399 dissociated HIF-2 (an obligatory heterodimer of HIF-2α-HIF-1β) in human ccRCC cells and suppressed tumorigenesis in 56% (10 out of 18) of such lines[1].PT2399 ?inhibits HIF-2α (IC50: 6 nM).?PT2399 represses various HIF target genes in 786-O VHL?/? ccRCC cells, does not suppress HIF-1α-specific targets such as BNIP3.?PT2399 can cripple HIF-2α’s ability to bind to Aryl hydrocarbon receptor nuclear translocator (ARNT).?PT2399 (20 μM) induces off-target toxicity because it inhibits the proliferation of HIF-2α ?/? 786-O cells and other cancer cell lines with undetectable HIF-2α.?PT2399 (0.2–2 μM;?0-21 days) inhibits 786-O cells soft agar growth[2][3].
In vivo PT2399) that directly inhibits HIF-2α causes tumour regression in preclinical mouse models of primary and metastatic pVHL-defective clear cell renal cell carcinoma in an on-target fashion[2].PT2399 inhibits tumor cell proliferation 3.5 fold in renal cell carcinoma (RCC) bearing mice.?PT2399 directly inhibits HIF-2α causes tumor regression in preclinical models of primary and metastatic pVHL-defective ccRCC in an on-target fashion.?PT2399 reduces tumor cell density and increases fibrosis in RCC bearing mice.?PT2399 (100 mg/kg;?oral gavage;?every 12 hours) is more active than SU 11248 and inhibits tumor growth in several SU 11248-resistant tumors in RCC bearing mice [1][2].
Molecular Weight 419.32
Formula C17H10F5NO4S
CAS No. 1672662-14-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 200 mg/mL (476.96 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Epigenetics Compound Library Bioactive Compound Library Anti-Cancer Compound Library Anti-Pancreatic Cancer Compound Library Transcription Factor-Targeted Compound Library NO PAINS Compound Library Glycolysis Compound Library HIF-1 Signaling Pathway Compound Library Angiogenesis related Compound Library

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Keywords

PT2399 1672662-14-4 Angiogenesis Chromatin/Epigenetic Metabolism HIF/HIF Prolyl-Hydroxylase HIF Hypoxia-inducible factors Inhibitor PT-2399 inhibit HIF-PH HIFs PT 2399 inhibitor

 

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