MCE 的所有產(chǎn)品僅用作科學研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務。

Abiraterone acetate

CAS No. : 154229-18-2

MCE 國際站：Abiraterone acetate

產(chǎn)品活性：Abiraterone acetate (CB7630) 是一種口服、有效、選擇性和不可逆的 CYP17A1 抑制劑，具有抗雄激素活性。Abiraterone acetate是 Abiraterone (CB7598) 的前體形式。

研究領域：Metabolic Enzyme/Protease

作用靶點：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.

相關產(chǎn)品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Antioxidant Compound Library  |  Oxygen Sensing Compound Library  |  NMPA-Approved Drug Library  |  FDA Approved & Pharmacopeial Drug Library  |  Targeted Therapy Drug Library   |  Mitochondria-Targeted Compound Library  |  Children’s Drug Library  |  FDA-Approved Anticancer Drug Library  |  Anti-Prostate Cancer Compound Library  |  Heterocyclic Compound Library  |  Off-patent Drug Library  |  Highly Selective Inhibitors Library  |  PC945  |  Mephenytoin-d₅  |  AMG-208  |  Doxepin-d₃ hydrochloride  |  Hypericin  |  EMT inhibitor-2  |  Atazanavir  |  Galeterone  |  CYP1B1-IN-2  |  Bergapten  |  Fadrozole hydrochloride  |  Ginsenoside Rd  |  ML252  |  Ezutromid  |  Seviteronel  |  4-(Trifluoromethyl)umbelliferone  |  Chlorpromazine hydrochloride  |  BVT948  |  Nonsteroidal aromatase inhibitor 1  |  Anticancer agent 111  |  CYP121A1-IN-1  |  Fenofibrate (Standard)  |  TMS  |  SOS1-IN-16  |  CYP3A4-IN-1  |  Furafylline  |  Eriodictyol chalcone  |  Linderane  |  Thermopsoside

熱門產(chǎn)品線：重組蛋白  |  化合物庫  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標記物  |  寡核苷酸  |  抗體  |  點擊化學

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry