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PT2399

Chemical Structure : PT2399

CAS No.: 1672662-14-4

PT2399 (PT 2399, PT-2399)

Catalog No.: PC-60317Not For Human Use, Lab Use Only.

PT2399 (PT 2399, PT-2399) is a selective, potent HIF-2α antagonist that binds directly to the HIF2α PAS B domain.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PT2399 (PT 2399, PT-2399) is a selective, potent HIF-2α antagonist that binds directly to the HIF2α PAS B domain.
PT2399 minimally affects a panel of 68 receptors, ion channels, and enzymes.
PT2399 specifically disassembles HIF-2 but not HIF-1 complexes, reduces the expression of HIF-2 target genes (VEGF, SERPINE1, IGFBP3, CCND1, TGFA, and SLC2A1), but not HIF-1 targets (CA9, PGK1, and LDHA).
PT2399 exhibits tumor growth inhibition in selected VHL-deficient clear-cell renal cell carcinoma (ccRCC) models.

Physicochemical Properties

M.Wt 419.32
Formula C17H10F5NO4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[(1S)-7-(difluoromethylsulfonyl)-2,2-difluoro-1-hydroxy-indan-4-yl]oxy-5-fluoro-benzonitrile

References

1. Chen W, et al. Nature. 2016 Nov 3;539(7627):112-117.

2. Cho H, et al. Nature. 2016 Nov 3;539(7627):107-111.

3. Ricketts CJ, et al. Cancer Cell. 2016 Oct 10;30(4):515-517.

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