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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-HIF/HIF Prolyl-hydroxylase-AB521
AB521

Chemical Structure : AB521

CAS No.: 2709069-30-5

AB521 (Casdatifan, AB-521)

货号: PC-24655Not For Human Use, Lab Use Only.

AB521 (Casdatifan) is a potent, allosteric small molecule inhibitor of protumourigenic HIF-2α, potently and selectively inhibits HIF-2α-mediated transcription with IC50 of 28.9 nM in 786-O ccRCC cells (VEGF secretion inhibition).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AB521 (Casdatifan) is a potent, allosteric small molecule inhibitor of protumourigenic HIF-2α, potently and selectively inhibits HIF-2α-mediated transcription with IC50 of 28.9 nM in 786-O ccRCC cells (VEGF secretion inhibition).
AB521 binds the PAS-B domain of HIF-2α, effectively inhibiting HIF-2α-ARNT complex formation and HIF-2α-mediated transcription.
AB521 selectively inhibits HIF-2α and not HIF-1α.
AB521 inhibits HIF-2α-dependent gene expression in primary human macrophages and endothelial cells.
AB521 blocks HIF-2α-mediated gene transcription in vivo and inhibits tumour growth.

物理化学性质&存储条件

分子量 439.42
分子式 C21H17F4NO3S
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

1-Naphthalenecarbonitrile, 3,5,6-trifluoro-8-[(1S,2R)-2-fluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]-5,6,7,8-tetrahydro-, (5R,6S,8R)-

参考文献

1. Schweickert PG, et al. Br J Pharmacol. 2025 May 21. doi: 10.1111/bph.70075.

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