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Chemical Structure : PT2385
CAS No.: 1672665-49-4
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $128 | In stock | |
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 383.3417 | |
| Formula | C17H12F3NO4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Benzonitrile, 3-[[(1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro- |
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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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