Chemical Structure : AB521
CAS No.:
2709069-30-5
AB521
(Casdatifan, AB-521)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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439.42
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Formula
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C21H17F4NO3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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)-
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References
1. Schweickert PG, et al. Br J Pharmacol. 2025 May 21. doi: 10.1111/bph.70075.
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