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Abiraterone acetate

CAS No. : 154229-18-2

MCE 国际站：Abiraterone acetate

产品活性：Abiraterone acetate (CB7630) 是一种口服、有效、选择性和不可逆的 CYP17A1 抑制剂，具有抗雄激素活性。Abiraterone acetate是 Abiraterone (CB7598) 的前药形式。

研究领域：Metabolic Enzyme/Protease

作用靶点：Cytochrome P450

In Vitro: Abiraterone (Abi) acetate is an ester prodrug of the anticancer agent Abiraterone, which shows IC₅₀ values of 15 nM and 2.5 nM for the 17,20-lyase and 17α-hydroxylase (CYP17 is a bifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activity). Abiraterone inhibits human 17,20-lyase and 17α-hydroxylase with IC₅₀ of 27 and 30 nM respectively. Significant inhibition of proliferation of the AR-positive prostate cancer cell lines LNCaP and VCaP with doses of Abiraterone ≥5 µM is confirmed. Abiraterone inhibits recombinant human 3βHSD1 and 3βHSD2 activity with competitive K_i values of 2.1 and 8.8 µM. 10 µM Abiraterone is sufficient to completely block synthesis of 5α-dione and DHT in both cell lines.Treatment with Abiraterone significantly inhibited CRPC progression in the robustly growing subset, effectively putting a ceiling on tumor growth over 4 weeks of treatment (P<0.00001).

In Vivo: Abiraterone (Abi) acetate prolongs survival in castration-resistant prostate cancer (CRPC). [³H]-dehydroepiandrosterone (DHEA) depletion and Δ⁴-androstenedione (AD) accumulation are inhibited by Abiraterone in LNCaP, with an IC₅₀<1 µM. The 0.5 mmol/kg/d Abiraterone treatment dose is previously shown to yield serum concentrations of about 0.5 to 1 µM. Xenograft tumor growth in the control group is widely variable, with some tumors growing slowly and only a subset of tumors exhibiting robust growth.

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