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D4-abiraterone

(Synonyms: Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite)

目录号: PL01805 纯度: ≥99%

D4-abiraterone 是阿比特龙的主要代谢产物。D4-abiraterone 是 CYP17A1, 3β-羟基类固醇脱氢酶 (3 βHSD) 和类固醇-5α-还原酶 ( SRD5A ) 的抑制剂，也是雄激素受体的拮抗剂。

CAS No. :154229-21-7

商品编号	规格	价格	会员价
PL01805-5mg	5mg	¥1145.00	请登录
PL01805-10mg	10mg	¥1845.00	请登录
PL01805-25mg	25mg	¥3975.00	请登录
PL01805-50mg	50mg	¥5665.00	请登录
PL01805-100mg	100mg	¥7675.00	请登录
PL01805-1 mL x 10 mM (in DMSO)	1 mL x 10 mM (in DMSO)	¥1255.00	请登录

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中文名称	D4-abiraterone
英文名称	D4-abiraterone
英文别名	Androsta-4,16-dien-3-one,17-(3-pyridinyl)- (9CI);17-(3-Pyridinyl)-androsta-4,16-dien-3-one;17-(3-Pyridyl)androsta-5,16-dien-3-one;17-(pyridin-3-yl)androsta-4,16-dien-3-one;Androsta-4,16-dien-3-one, 17-(3-pyridinyl)-;CB 7627;CB-7627;Δ4-abiraterone;Abiraterone ketone analog;D4-abiraterone;D4A;D4-abiraterone (CB-7627);7-(3-pyridyl)androsta-5,16-dien-3-one;17-(3-pyridinyl)-androsta-4,16-diene-3-one
Cas No.	154229-21-7
分子式	C₂₄H₂₉NO
分子量	347.49
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
详情描述	D4-abiraterone 是阿比特龙的主要代谢产物。D4-abiraterone 是 CYP17A1, 3β-羟基类固醇脱氢酶 (3 βHSD) 和类固醇-5α-还原酶 ( SRD5A ) 的抑制剂，也是雄激素受体的拮抗剂。

产品详情	D4-abiraterone 是阿比特龙的主要代谢产物。D4-abiraterone 是 CYP17A1, 3β-羟基类固醇脱氢酶 (3 βHSD) 和类固醇-5α-还原酶 ( SRD5A ) 的抑制剂，也是雄激素受体的拮抗剂。
生物活性	D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
性状	Solid
IC50 & Target[1][2]	CYP17A1, 3βHSD, SRD5A, androgen receptor
体外研究(In Vitro)	D4-abiraterone (D4A ) (10 mM) nearly completely blocks conversion from D4-androstenedione (AD) to 5α-androstanedione and other 5α-reduced androgens. The affinity of D4-abiraterone for mutant (expressed in LNCaP, half-maximum inhibitory concentration (IC50=5.3 nM)) and wild type (expressed in LAPC4, IC50=7.9 nM) androgen receptor (AR) is greater than that of abiraterone (Abi) (IC50=418 and >500 nM, respectively). Compare with Abi, D4-abiraterone clearly better suppresses PSA, TMPRSS2 and FKBP5 expression in LNCAP, LAPC4 and C4-2 cell lines. D4-abiraterone also inhibits AR target gene expression in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	D4-abiraterone (D4A) is tenfold more potent than abiraterone (Abi) in blocking conversion from dehydroepiandrosterone (DHEA) by 3β-hydroxysteroid dehydrogenase (3βHSD) to D4-androstenedione (AD) in LNCaP and VCaP xenografts. 0.1 μM D4-abiraterone is equivalent to 1 μM Abi for blocking AD accumulation at 48 h in both LNCaP and VCaP xenografts. Progression is significantly delayed in the D4-abiraterone group compare with the Abi acetate group (P=0.011). D4-abiraterone treatment increases progression-free survival compare with Abi acetate. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献	[1]. Li Z, et al. Conversion of abiraterone to D4A drives anti-tumour activity in prostate cancer. Nature. 2015 Jul 16;523(7560):347-51.

溶解度数据	In Vitro: DMSO : 50 mg/mL (143.89 mM; Need ultrasonic)配制储备液

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[1]. Li Z, et al. Conversion of abiraterone to D4A drives anti-tumour activity in prostate cancer. Nature. 2015 Jul 16;523(7560):347-51.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

D4-abiraterone

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