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乙酸阿比特龙酯

更新时间:2024-01-02 12:56:38

乙酸阿比特龙酯结构式
乙酸阿比特龙酯结构式
品牌特惠专场
常用名 乙酸阿比特龙酯 英文名 Abiraterone Acetate
CAS号 154229-18-2 分子量 391.546
密度 1.1±0.1 g/cm3 沸点 506.7±50.0 °C at 760 mmHg
分子式 C26H33NO2 熔点 127-130°C
MSDS 中文版 美版 闪点 260.2±30.1 °C
符号 GHS08
GHS08
信号词 Danger

 乙酸阿比特龙酯用途


Abiraterone acetate是口服,有效,选择性和不可逆的 CYP17 抑制剂。

 乙酸阿比特龙酯名称

中文名 乙酸阿比特龙酯
英文名 abiraterone acetate
中文别名 醋酸阿比特龙 | (3BETA)-17-(3-吡啶基)-雄甾-5,16-二烯-3-乙酸酯 | 阿比特龙乙酸盐 | 醋酸阿比特龙酯
英文别名 更多

 乙酸阿比特龙酯生物活性

描述 Abiraterone acetate是口服,有效,选择性和不可逆的 CYP17 抑制剂。
相关类别
靶点

CYP17[1]

体外研究 阿比特龙(Abi)乙酸酯是抗癌剂阿比特龙的酯前药,对于17,20-裂解酶和17α-羟化酶显示IC 50值为15 nM和2.5 nM(CYP17是具有17α-羟化酶和17的双功能酶, 20-裂解酶活性)。阿比特龙抑制人17,20-裂解酶和17α-羟化酶,IC50分别为27和30 nM [1]。用阿齐拉酮≥5μM剂量显着抑制AR阳性前列腺癌细胞系LNCaP和VCaP的增殖[2]。阿比特龙抑制重组人3βHSD1和3βHSD2活性,竞争性Ki值为2.1和8.8μM。 10μM阿比特龙足以完全阻断两种细胞系中5α-二酮和DHT的合成。阿比特龙的治疗显着抑制稳健生长子集中的CRPC进展,有效地使治疗4周内肿瘤生长达到上限(P <0.00001) [3]。
体内研究 阿比特龙(Abi)乙酸盐可延长去势抵抗性前列腺癌(CRPC)的存活率。 LNCaP中阿比特龙抑制[3H] -脱氢表雄酮(DHEA)消耗和Δ4-雄烯二酮(AD)积累,IC50 <1μM。先前显示0.5mmol/kg/d阿比特龙治疗剂量产生约0.5至1μM的血清浓度。对照组的异种移植肿瘤生长变化很大,一些肿瘤生长缓慢,只有一部分肿瘤表现出强劲的生长[3]。
细胞实验 将LNCaP和VCaP细胞接种在96孔板中,并在补充CSS的无酚红或FBS补充的培养基中生长7天。在接种后24和96小时,用阿比特龙(5μM和10μM)处理细胞,并通过添加CellTiter Glo并测量发光在第7天测定细胞活力[2]。
动物实验 小鼠[3]通过手术切除睾丸切除6至8周龄的雄性NOD / SCID小鼠,并植入5mg 90天持续释放DHEA小丸以模拟具有人肾上腺生理学的CRPC。两天后,用Matrigel皮下注射7×106个LAPC4细胞。肿瘤尺寸每周测量2至3次,体积计算为长×宽×高×0.52。一旦肿瘤达到300mm 3,将小鼠随机分配到载体或阿比特龙治疗组。阿比特龙组小鼠用5 mL / kg腹腔注射0.5 mmol / kg / d(0.1 mL 5%苄醇和95%红花油溶液)和对照小鼠仅用载体治疗,每日一次,每周5天以上持续4周(每次治疗n = 8只小鼠)。基于混合效应模型,通过ANOVA评估阿比特龙和媒介物治疗组之间的统计学显着性。
参考文献

[1]. Stein MN, et al. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16(3):387-400.

[2]. Richards J, et al. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72(9):2176-82.

[3]. Li R, et al. Abiraterone inhibits 3β-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistant prostate cancer. Clin Cancer Res. 2012 Jul 1;18(13):3571-9.

[4]. Lee GT, et al. Intracrine androgen biosynthesis in renal cell carcinoma. Br J Cancer. 2017 Mar 28;116(7):937-943.

 乙酸阿比特龙酯物理化学性质

密度 1.1±0.1 g/cm3
沸点 506.7±50.0 °C at 760 mmHg
熔点 127-130°C
分子式 C26H33NO2
分子量 391.546
闪点 260.2±30.1 °C
精确质量 391.251129
PSA 39.19000
LogP 6.55
外观性状 固体;White to Light yellow to Light orange powder to crystal
蒸汽压 0.0±1.3 mmHg at 25°C
折射率 1.584
储存条件 -20°C Freezer

 乙酸阿比特龙酯安全信息

符号 GHS08
GHS08
信号词 Danger
危害声明 H360-H372
警示性声明 P201-P260-P280-P308 + P313
靶器官 Endocrine system
危害码 (欧洲) Xi
危险品运输编码 NONH for all modes of transport
RTECS号 BV7992100
海关编码 2933399090

 乙酸阿比特龙酯海关

海关编码 2933399090
中文概述 2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素 品名, 成分含量, 用途, 乌洛托品请注明外观, 6-己内酰胺请注明外观, 签约日期
Summary 2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 乙酸阿比特龙酯文献7

更多文献
Phase I clinical trial of the CYP17 inhibitor abiraterone acetate demonstrating clinical activity in patients with castration-resistant prostate cancer who received prior ketoconazole therapy.

J. Clin. Oncol. 28(9) , 1481-8, (2010)

Abiraterone acetate is a prodrug of abiraterone, a selective inhibitor of CYP17, the enzyme catalyst for two essential steps in androgen biosynthesis. In castration-resistant prostate cancers (CRPCs),...

Significant and sustained antitumor activity in post-docetaxel, castration-resistant prostate cancer with the CYP17 inhibitor abiraterone acetate.

J. Clin. Oncol. 28(9) , 1489-95, (2010)

The principal objective of this trial was to evaluate the antitumor activity of abiraterone acetate, an oral, specific, irreversible inhibitor of CYP17 in docetaxel-treated patients with castration-re...

Phase II multicenter study of abiraterone acetate plus prednisone therapy in patients with docetaxel-treated castration-resistant prostate cancer.

J. Clin. Oncol. 28(9) , 1496-501, (2010)

Persistence of ligand-mediated androgen receptor signaling has been documented in castration-resistant prostate cancers (CRPCs). Abiraterone acetate (AA) is a potent and selective inhibitor of CYP17, ...

 乙酸阿比特龙酯英文别名

17-(3-pyridyl)-5,16-androstadien-3beta-acetate
Abiraterone acetate
Androsta-5,16-dien-3-ol, 17-(3-pyridinyl)-, acetate (ester), (3β)-
Zytiga
(3β)-17-(3-Pyridinyl)androsta-5,16-dien-3-yl acetate
(3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-yl acetate
Abiraterone (acetate)
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