PT2385 (PT-2385)

Chemical Structure : PT2385

CAS No.: 1672665-49-4

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货号: 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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5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3280	In stock
50 mg	￥5280	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	383.3417
分子式	C17H12F3NO4S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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-

参考文献

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.

PT2385 (PT-2385)

生物&药学活性

物理化学性质&存储条件

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PT2385 (PT-2385)

生物&药学活性

物理化学性质&存储条件

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