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D4-abiraterone is the active metabolite of abiraterone produced by 3β-HSD and is further metabolised by SRD5A.Δ4-Abiraterone is an inhibitor of CYP17A1, 3β-HSD and SRD5A, and an antagonist of the androgen receptor.
Description | D4-abiraterone is the active metabolite of abiraterone produced by 3β-HSD and is further metabolised by SRD5A.Δ4-Abiraterone is an inhibitor of CYP17A1, 3β-HSD and SRD5A, and an antagonist of the androgen receptor. |
Targets&IC50 | Androgen receptor:5.3-7.9 nM |
In vitro | D4-abiraterone (10 μM) nearly fully blocks AD conversion to 5α-androgens. D4-abiraterone binds AR more strongly (IC₅₀ = 5.3-7.9 nM) than abiraterone (IC₅₀ = 418-500+ nM), and more effectively suppresses AR target genes like PSA[1]. |
In vivo | In LNCaP and VCaP mouse tumors, D4-abiraterone was 10× stronger than abiraterone. At 0.1 μM, D4-abiraterone matched 1 μM abiraterone in blocking AD formation and delayed tumor growth within 48 h[1]. |
Alias | Δ4-Abiraterone, Delta4-Abiraterone, CB-7627, CB7627, Abiraterone D4A metabolite |
Molecular Weight | 347.49 |
Formula | C24H29NO |
Cas No. | 154229-21-7 |
Smiles | C[C@@]12[C@]([C@]3([C@@]([C@]4(C)C(CC3)=CC(=O)CC4)(CC1)[H])[H])(CC=C2C=5C=CC=NC5)[H] |
Relative Density. | 1.14 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (115.11 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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