Abiraterone (Synonyms: 阿比特龙; CB-7598)

目录号: HY-70013 纯度: 99.88%: FAQs
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摩尔计算器

Abiraterone 是一种有效的不可逆的 CYP17A1 抑制剂，具有抗雄激素活性，抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶和 17,20-裂合酶活性，IC₅₀ 值分别为 2.5 nM 和 15 nM.

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Abiraterone Chemical Structure

CAS No. : 154229-19-3

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MCE 顾客使用本产品发表的 19 篇科研文献

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC₅₀s of 2.5 nM and 15 nM, respectively.

IC₅₀ & Target

CYP17

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	35.8 nM Compound: ABT	Inhibition of recombinant human CYP17 expressed in human A549 cell membranes using 17-alpha hydroxyprogesterone as substrate and NADPH as cofactor pretreated for 5 mins followed by substrate and cofactor addition after 60 mins by LC/MS analysis Inhibition of recombinant human CYP17 expressed in human A549 cell membranes using 17-alpha hydroxyprogesterone as substrate and NADPH as cofactor pretreated for 5 mins followed by substrate and cofactor addition after 60 mins by LC/MS analysis	[PMID: 28350999]
A549	GI₅₀	95 μM Compound: Abiraterone	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay Antiproliferative activity against human A549 cells after 48 hrs by SRB assay	[PMID: 29172080]
DU-145	GI₅₀	> 10 μM Compound: abiraterone	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
ECa-109 cell line	IC₅₀	> 32 μM Compound: Abiraterone	Antiproliferative activity against human EC109 cells after 72 hrs by MTT assay Antiproliferative activity against human EC109 cells after 72 hrs by MTT assay	[PMID: 29310026]
GES1	IC₅₀	13.12 μM Compound: Abiraterone	Antiproliferative activity against human GES-1 cells after 72 hrs by MTT assay Antiproliferative activity against human GES-1 cells after 72 hrs by MTT assay	[PMID: 29310026]
HBL-100	GI₅₀	> 100 μM Compound: Abiraterone	Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay	[PMID: 29172080]
HEK-293T	IC₅₀	> 100 μM Compound: Abiraterone	Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36455509]
HeLa	IC₅₀	16.9 μM Compound: Abiraterone	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36455509]
HeLa	GI₅₀	7.9 μM Compound: Abiraterone	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay	[PMID: 29172080]
HepG2	IC₅₀	59.8 μM Compound: Abiraterone	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36455509]
hTERT-BJ	GI₅₀	4.5 μM Compound: Abiraterone	Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay	[PMID: 29172080]
LNCaP	IC₅₀	2706 nM Compound: Abiraterone	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay	[PMID: 36070471]
LNCaP	IC₅₀	3.29 μM Compound: Abiraterone	Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay	[PMID: 29310026]
LNCaP	IC₅₀	800 nM Compound: Abiraterone	In vitro cytochrome P450 17A1 inhibition was assayed using the rapid acetic acid releasing assay (AARA), utilizing intact P450c17-expressing Escherichia coli or P450c17-LNCaP cells as the enzyme source. In vitro cytochrome P450 17A1 inhibition was assayed using the rapid acetic acid releasing assay (AARA), utilizing intact P450c17-expressing Escherichia coli or P450c17-LNCaP cells as the enzyme source.	[PMID: 12773039]
MCF7	IC₅₀	19.3 μM Compound: Abiraterone	Growth inhibition of human MCF7 cells after 72 hrs by MTT assay Growth inhibition of human MCF7 cells after 72 hrs by MTT assay	[PMID: 27209562]
MCF7	IC₅₀	38.2 μM Compound: Abiraterone	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36455509]
MDA-MB-231	IC₅₀	19.2 μM Compound: Abiraterone	Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27209562]
MDA-MB-361	IC₅₀	20.4 μM Compound: Abiraterone	Growth inhibition of human MDA-MB-361 cells after 72 hrs by MTT assay Growth inhibition of human MDA-MB-361 cells after 72 hrs by MTT assay	[PMID: 27209562]
MGC-803	IC₅₀	7.72 μM Compound: Abiraterone	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 29310026]
PC-3	GI₅₀	> 10 μM Compound: abiraterone	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
PC-3	IC₅₀	5.94 μM Compound: Abiraterone	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 29310026]
PC-3	IC₅₀	9.32 μM Compound: Abiraterone	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24148837]
SK-OV-3	IC₅₀	59.5 μM Compound: Abiraterone	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36455509]
SW1573	GI₅₀	85 μM Compound: Abiraterone	Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay	[PMID: 29172080]
T47D	IC₅₀	16.9 μM Compound: Abiraterone	Growth inhibition of human T47D cells after 72 hrs by MTT assay Growth inhibition of human T47D cells after 72 hrs by MTT assay	[PMID: 27209562]
T47D	GI₅₀	24 μM Compound: Abiraterone	Antiproliferative activity against human T47D cells after 48 hrs by SRB assay Antiproliferative activity against human T47D cells after 48 hrs by SRB assay	[PMID: 29172080]
T47D	IC₅₀	34.7 μM Compound: Abiraterone	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36455509]
WiDr	GI₅₀	42 μM Compound: Abiraterone	Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay	[PMID: 29172080]

体外研究
(In Vitro)

已证实 Abiraterone 剂量 ≥5 μM 可显著抑制 AR 阳性前列腺癌细胞系 LNCaP 和 VCaP 的增殖^[2]。Abiraterone 对 17,20-裂解酶和 17α-羟化酶的 IC₅₀ 值分别为 15 nM 和 2.5 nM（CYP17 是一种具有 17α-羟化酶和 17,20-裂解酶活性的双功能酶）。Abiraterone 抑制人类 17,20-裂解酶和 17α-羟化酶的 IC₅₀ 值分别为 27 和 30 nM^[3]。Abiraterone 抑制重组人类 3βHSD1 和 3βHSD2 活性，竞争性 K_i 值分别为 2.1 和 8.8 μM。 10 μM Abiraterone 足以完全阻断两种细胞系中 5α-二酮和 DHT 的合成。使用 abi 治疗可显著抑制强劲增长亚群中的 CRPC 进展，有效地在 4 周的治疗中限制肿瘤生长 (P<0.00001)。Abiraterone 可抑制 LNCaP 中的 [³H]-脱氢表雄酮 (DHEA) 耗竭和 Δ⁴-雄烯二酮 (AD) 积累，IC₅₀ 值 <1 μM^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

先前研究表明，0.5 mmol/kg/d Abiraterone 处理剂量可产生约 0.5 至 1 μM 的血清浓度。对照组异种移植肿瘤生长差异很大，一些肿瘤生长缓慢，只有一小部分肿瘤表现出强劲生长^[4]。静脉注射（5 mg/kg）后，清除率 (Cl) 和分布容积 (V_d) 值分别为 31.2 mL/min/kg 和 1.97 L/kg。AUC_0-∞（从零时间点到无穷大时间点的血浆浓度-时间曲线下面积）值为 2675 ng*h/mL。终末半衰期 (t_1/2) 值为 0.73 小时。由于清除率高，Abiraterone (ART) 仅在静脉注射后 2 小时内可量化^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

349.51

Formula

C₂₄H₃₁NO

CAS 号

154229-19-3

性状

固体

颜色

White to off-white

中文名称

阿比特龙；坦度酮罗；阿比特伦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

Ethanol 中的溶解度 : 5 mg/mL (14.31 mM; 超声助溶 (<60°C))

DMF 中的溶解度 : 5 mg/mL (14.31 mM; 超声助溶 (<60°C))

DMSO 中的溶解度 : 2.5 mg/mL (7.15 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8611 mL	14.3057 mL	28.6115 mL
5 mM	0.5722 mL	2.8611 mL	5.7223 mL
10 mM	0.2861 mL	1.4306 mL	2.8611 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

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纯度 & 产品资料

纯度: 99.88%

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Data Sheet (637 KB) SDS (700 KB)

COA (292 KB) RP-HPLC (146 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Attard G, et al. Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms that castration-resistant prostate cancer commonly remains hormone driven. J Clin Oncol. 2008 Oct 1;26(28):4563-71. [Content Brief]

[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. [Content Brief]

[3]. 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. [Content Brief]

[4]. 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. [Content Brief]

[5]. Kumar SV, et al. Validated RP-HPLC/UV method for the quantitation of abiraterone in rat plasma and its application to a pharmacokinetic study in rats. Biomed Chromatogr. 2013 Feb;27(2):203-7. [Content Brief]

[6]. 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. [Content Brief]

Cell Assay ^[2]	LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days. Cells are treated with Abiraterone (5 μM and 10 μM) at 24 and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]^[5]	Mice^[4] Male NOD/SCID mice 6 to 8 weeks of age are surgically orchiectomized and implanted with a 5 mg 90-day sustained release DHEA pellet to mimic CRPC with human adrenal physiology. Two days later, 7×10⁶ LAPC4 cells are injected subcutaneously with Matrigel. Tumor dimensions are measured 2 to 3 times per week, and volume is calculated as length×width×height×0.52. Once tumors reach 300 mm³, mice are randomly assigned to vehicle or Abiraterone treatment groups. Mice in the Abiraterone group are treated with 5 mL/kg intraperitoneal injections of 0.5 mmol/kg/d (0.1 mL 5% benzyl alcohol and 95% safflower oil solution) and control mice with vehicle only, once daily for 5 days per week over a duration of 4 weeks (n=8 mice per treatment). Statistical significance between Abiraterone and vehicle treatment groups is assessed by ANOVA based on a mixed-effect model. Rats^[5] Male Sprague-Dawley rats (n=8, 240-260 g) are used. Blood samples (450 µL) are obtained following an i.v. 5 mg/kg dose of ART into polypropylene tubes containing Na₂-EDTA solution as an anticoagulant and at pre-dose, 0.12, 0.25, 0.5, 1, 2, 4, 6, 8 and 24 h (a sparse sampling protocol is adopted during blood collection and at each time point blood is collected from four animals). Plasma is harvested by centrifuging the blood using a Biofuge at 1760g for 5 min and stored frozen at -80±10°C until analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Attard G, et al. Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms that castration-resistant prostate cancer commonly remains hormone driven. J Clin Oncol. 2008 Oct 1;26(28):4563-71. [Content Brief] [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. [Content Brief] [3]. 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. [Content Brief] [4]. 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. [Content Brief] [5]. Kumar SV, et al. Validated RP-HPLC/UV method for the quantitation of abiraterone in rat plasma and its application to a pharmacokinetic study in rats. Biomed Chromatogr. 2013 Feb;27(2):203-7. [Content Brief] [6]. 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. [Content Brief]

Abiraterone 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol / DMF	1 mM	2.8611 mL	14.3057 mL	28.6115 mL	71.5287 mL
DMSO / Ethanol / DMF	5 mM	0.5722 mL	2.8611 mL	5.7223 mL	14.3057 mL
Ethanol / DMF	10 mM	0.2861 mL	1.4306 mL	2.8611 mL	7.1529 mL

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Abiraterone154229-19-3CB-7598阿比特龙坦度酮罗阿比特伦CB7598CB 7598Cytochrome P450CYPsInhibitorinhibitorinhibit

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Abiraterone (Synonyms: 阿比特龙; CB-7598)

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MCE 顾客使用本产品发表的 19 篇科研文献

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Abiraterone (Synonyms: 阿比特龙; CB-7598)

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Abiraterone 相关抗体

MCE 顾客使用本产品发表的 19 篇科研文献

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