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D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor.
D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor.
规格 | 价格 | 库存 | 数量 |
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2 mg | ¥ 1,480 | 5日内发货 |
产品描述 | D4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid 5a-reductase (SRD5A), the main metabolite of abiraterone. D4-Abiraterone is also an antagonist of androgen receptor. |
体外活性 | D4-Abiraterone (D4A) (10 mM) almost completely prevented the conversion of D4-androstenedione (AD) to 5α-androstanedione and other 5α-reducing androgens. D4-Abiraterone has greater affinity for androgen receptor (AR) than mutant (expressed in LNCaP, half maximum inhibitory concentration (IC50 = 5.3 nM)) and wild type (expressed in LAPC4, IC50 = 7.9 nM) Abiron (IC50 = 418 and> 500 nM, respectively). Compared with Abi, D4-abiraterone significantly inhibited the expression of PSA, TMPRSS2 and FKBP5 in LNCAP, LAPC4 and C4-2 cell lines. D4-Abiraterone also suppressed AR target gene expression in a dose-dependent manner. |
体内活性 | In preventing the conversion of 3β-hydroxysteroid dehydrogenase (3βHSD) from dehydroepiandrosterone (DHEA) to D4-androstenedione (AD) in LNCaP and VCaP xenografts, D4-Abiraterone (D4A) The effect is ten times higher than that of Abiron. In LNCaP and VCaP xenografts, AD accumulation was blocked at 48 h, and 0.1 μMD4-Abiraterone was equivalent to 1 μMAbi. Compared with the Abirate acetate group, the progress of the D4-Abiraterone group was significantly delayed (P = 0.011). Compared with abirate acetate, D4-Abiraterone treatment can increase progression-free survival . |
别名 | Abiraterone D4A metabolite, CB-7627, Δ4-Abiraterone |
分子量 | 347.49 |
分子式 | C24H29NO |
CAS No. | 154229-21-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (143.89 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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DMSO
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