An active metabolite of abiraterone; androgen receptor antagonist (IC50 = 5.3 nM); reduces expression of androgen receptor target genes in LNCaP

Δ4-Abiraterone – 5 mg

Brand:
Cayman
CAS:
154229-21-7
Storage:
-20
UN-No:
Non-Hazardous - /

Δ4-Abiraterone (D4A) is an active metabolite of the CYP17A1 inhibitor abiraterone (Item No. 9002768).{47328} D4A is an androgen receptor antagonist (IC50 = 5.3 nM) that reduces expression of the androgen receptor target genes PSA, TMPRSS2, and FKBP5 in LNCaP, LAPC4, and C4-2 cell lines. It inhibits the cytochrome P450 (CYP) isoform CYP17A1 by 66.5% when used at a concentration of 1 nM. D4A (10 μM) also blocks SRD5A conversion of Δ4-androstenedione to 5α-androstanedione in LAPC4 cells. In vivo, D4A delays tumor progression in a VCaP mouse xenograft model and increases progression-free survival in a C4-2 mouse xenograft model.  

 

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SKU: 27594 - 5 mg Category:

Description

An active metabolite of abiraterone; androgen receptor antagonist (IC50 = 5.3 nM); reduces expression of androgen receptor target genes in LNCaP, LAPC4, and C4-2 cell lines; inhibits CYP17A1 at 1 nM; blocks SRD5A conversion of Δ4-androstenedione to 5α-androstanedione in LAPC4 cells at 10 μM; delays tumor progression in a VCaP mouse xenograft model; increases progression-free survival in a C4-2 mouse xenograft model

Formal name: 17-(3-pyridinyl)-androsta-4,16-dien-3-one

Synonyms:  CB 7627|D4A

Molecular weight: 347.5

CAS: 154229-21-7

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Cancer||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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