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PT2385

Chemical Structure : PT2385

CAS No.: 1672665-49-4

PT2385 (PT-2385)

Catalog No.: PC-43267Not For Human Use, Lab Use Only.

PT2385 (PT-2385) is a potent, selective, and orally active antagonist of HIF2α, binds to HIF2α PAS-B domain (Kd=50 nM) and disrupts HIF2α/ARNT dimer formation.

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Biological Activity

PT2385 (PT-2385) is a potent, selective, and orally active antagonist of HIF2α, binds to HIF2α PAS-B domain (Kd=50 nM) and disrupts HIF2α/ARNT dimer formation; allosterically blocks HIF2α dimerization with the HIF1α/2α transcriptional dimerization partner ARNT/HIF1β, disrupts HIF2α, but not HIF1α, heterodimerization with ARNT in Hep3B cells; inhibits the expression of HIF2α-dependent genes, including VEGF-A, PAI-1, and cyclin D1 in ccRCC cell lines and tumor xenografts, also reduces HIF2α mRNA and protein levels in xenograft tumors.

Kidney Cancer

Phase 2 Clinical

Physicochemical Properties

M.Wt 383.3417
Formula C17H12F3NO4S
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

Benzonitrile, 3-[[(1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro-

References

1. Wallace EM, et al. Cancer Res. 2016 Sep 15;76(18):5491-500.

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

3. Courtney KD, et al. J Clin Oncol. 2018 Mar 20;36(9):867-874.

4. Xie C, et al. Nat Med. 2017 Nov;23(11):1298-1308.

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