AB521 free base · Synonyms: Castadifan | Casdatifanum

Casdatifan is an orally active HIF-2α inhibitor.

For research use only. Not for human or veterinary use.

Target HIF/HIF Prolyl-Hydroxylase VEGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

AB521 structure

CAS No.: 2709069-30-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 mg	USD 1,500.00	BP-00909-1mg	In stock	Get quote
5 mg	USD 4,300.00	BP-00909-5mg	In stock	Get quote
10 mg	USD 6,900.00	BP-00909-10mg	In stock	Get quote
25 mg	Inquire	BP-00909-25mg	In stock	Inquire

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Description

Casdatifan (AB521) is an orally active HIF-2α (hypoxia-inducible factor 2α) inhibitor. Casdatifan demonstrated significant antitumor activity and favorable pharmacokinetics in ccRCC (clear cell renal cell carcinoma) models.

Biological activity

In Vitro Casdatifan (2-10 μM; 24 h) reduces HIF-2α protein levels in 786-O and A-498 clear cell renal cell carcinoma (ccRCC) cells under normoxic conditions. Casdatifan potently inhibits VEGF secretion in 786-O ccRCC cells, with an IC50 of 28.9 nM. Casdatifan (0.001-10 μM; 21 days) inhibits the anchorage-independent growth of 786-O ccRCC cells in a concentration-dependent manner. Casdatifan (1 μM; 20 h) inhibits HIF-2α-dependent gene transcription in hypoxically induced primary human M2-polarized macrophages. Casdatifan (3 days) reduces HIF-2α protein levels in activated hypoxic primary human CD8+ T cells without impairing T cell proliferation or cytokine secretion. In Vivo Casdatifan (3-100 mg/kg; p.o.; once daily; until study endpoint) dose-dependently inhibits HIF-2α-mediated transcription and significantly suppresses tumor growth in nude mice bearing 786-O and A-498 xenograft models. Casdatifan (30 mg/kg; p.o.; once daily; until study endpoint) significantly enhances the antitumor efficacy in the NSG-MHC I/II DKO humanized PBMC A-498 ccRCC xenograft model when administered in combination with Zimberelimab.

Identifiers

SMILES: CS(C(C1=C2C[C@@H](F)[C@H]1O)=CC=C2[C@](C[C@H](F)[C@@H]3F)([H])C4=C3C=C(F)C=C4C#N)(=O)=O
InChIKey: KHBHHNNBNHHGPE-QCCZFBHPSA-N

Specifications

MW (average): 439.4230
Formula: C₂₁H₁₇F₄NO₃S
CAS No.: 2709069-30-5
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years, 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO, >100mg/mL

Documents

References

[1]. Schweickert PG, et al. Casdatifan (AB521) is a novel and potent allosteric small molecule inhibitor of protumourigenic HIF-2α dependent transcription. Br J Pharmacol. 2025;182(17):4147-4167.

Same target

Search HIF/HIF Prolyl-Hydroxylase

Same research area

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