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

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.
PT2385 allosterically blocks HIF2α dimerization with the HIF1α/2α transcriptional dimerization partner ARNT/HIF1β, disrupts HIF2α, but not HIF1α, heterodimerization with ARNT in Hep3B cells.
PT2385 inhibits the expression of HIF2α-dependent genes, including VEGF-A, PAI-1, and cyclin D1 in ccRCC cell lines and tumor xenografts.
PT2385 also reduces HIF2α mRNA and protein levels in xenograft tumors.

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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