Abiraterone (Synonyms: 阿比特龍; CB-7598)

目錄號(hào): HY-70013 純度: 99.88%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Abiraterone 是一種有效的不可逆的 CYP17A1 抑制劑，具有抗雄激素活性，抑制細(xì)胞色素 p450 酶 CYP17 的 17α-羥化酶和 17,20-裂合酶活性，IC₅₀ 值分別為 2.5 nM 和 15 nM.

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Abiraterone Chemical Structure

CAS No. : 154229-19-3

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規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in Ethanol	￥264	In-stock
1 mg	￥171	In-stock
5 mg	￥343	In-stock
10 mg	￥550	In-stock
25 mg	￥1000	In-stock
50 mg	￥1500	In-stock
100 mg	￥2260	In-stock
200 mg	￥3000	In-stock
500 mg	￥5500	In-stock
1 g	現(xiàn)貨	詢(xún)價(jià)
5 g		詢(xún)價(jià)
10 g		詢(xún)價(jià)

or 大包裝詢(xún)價(jià)

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Customer Review

Other Forms of Abiraterone:

Abiraterone-d₄ In-stock
Abiraterone acetate In-stock
Abiraterone (Standard) 詢(xún)價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 19 篇科研文獻(xiàn)

•Cell Res. 2020 Oct;30(10):833-853. [Abstract]
•Cell Res. 2020 Oct;30(10):833-853. [Abstract]
•Nature. 2012 Jan 22;482(7383):116-9. [Abstract]
•Eur Urol. 2015 Aug;68(2):228-35. [Abstract]
•Cell Death Dis. 2022 Dec 12;13(12):1034. [Abstract]
•Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
•Anal Chem. 2016 Oct 4;88(19):9347-9350. [Abstract]
•Prostate Cancer Prostatic Dis. 2023 Aug 26. [Abstract]
•Cancers (Basel). 2023 Aug 15, 15(16), 4115.
•J Immunol. 2022 Dec 21;ji2200696. [Abstract]
•Cells. 2020 Oct 19;9(10):2323. [Abstract]
•Sci Rep. 2017 Mar 15;7:44409. [Abstract]

•J Cancer. 2023 Jul 16;14(12):2236-2245. [Abstract]
•Prostate. 2017 Dec;77(16):1550-1562. [Abstract]
•biorxiv. 2024 Jun 9.
•Research Square Preprint. 2023 Nov 25.
•Biochemistry and Molecular Biology. 2020 Jul.
•Bionanoscience. 01 February 2017.
•Oncotarget. 2016 Sep 13;7(37):59781-59794. [Abstract]

Abiraterone 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Cytochrome P450 亞型特異性產(chǎn)品:

查看所有亞型

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

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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

細(xì)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]

體外研究
(In Vitro)

已證實(shí) Abiraterone 劑量 ≥5 μM 可顯著抑制 AR 陽(yáng)性前列腺癌細(xì)胞系 LNCaP 和 VCaP 的增殖^[2]。Abiraterone 對(duì) 17,20-裂解酶和 17α-羥化酶的 IC₅₀ 值分別為 15 nM 和 2.5 nM（CYP17 是一種具有 17α-羥化酶和 17,20-裂解酶活性的雙功能酶）。Abiraterone 抑制人類(lèi) 17,20-裂解酶和 17α-羥化酶的 IC₅₀ 值分別為 27 和 30 nM^[3]。Abiraterone 抑制重組人類(lèi) 3βHSD1 和 3βHSD2 活性，競(jìng)爭(zhēng)性 K_i 值分別為 2.1 和 8.8 μM。 10 μM Abiraterone 足以完全阻斷兩種細(xì)胞系中 5α-二酮和 DHT 的合成。使用 abi 治療可顯著抑制強(qiáng)勁增長(zhǎng)亞群中的 CRPC 進(jìn)展，有效地在 4 周的治療中限制腫瘤生長(zhǎng) (P<0.00001)。Abiraterone 可抑制 LNCaP 中的 [³H]-脫氫表雄酮 (DHEA) 耗竭和 Δ⁴-雄烯二酮 (AD) 積累，IC₅₀ 值 <1 μM^[4]。

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

體內(nèi)研究
(In Vivo)

先前研究表明，0.5 mmol/kg/d Abiraterone 處理劑量可產(chǎn)生約 0.5 至 1 μM 的血清濃度。對(duì)照組異種移植腫瘤生長(zhǎng)差異很大，一些腫瘤生長(zhǎng)緩慢，只有一小部分腫瘤表現(xiàn)出強(qiáng)勁生長(zhǎng)^[4]。靜脈注射（5 mg/kg）后，清除率 (Cl) 和分布容積 (V_d) 值分別為 31.2 mL/min/kg 和 1.97 L/kg。AUC_0-∞（從零時(shí)間點(diǎn)到無(wú)窮大時(shí)間點(diǎn)的血漿濃度-時(shí)間曲線下面積）值為 2675 ng*h/mL。終末半衰期 (t_1/2) 值為 0.73 小時(shí)。由于清除率高，Abiraterone (ART) 僅在靜脈注射后 2 小時(shí)內(nèi)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 號(hào)

154229-19-3

性狀

固體

顏色

White to off-white

中文名稱(chēng)

阿比特龍；坦度酮羅；阿比特倫

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

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

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

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

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

DMSO 中的溶解度 : 2.5 mg/mL (7.15 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

純度 & 產(chǎn)品資料

純度: 99.88%

選擇批次：

Data Sheet (637 KB) SDS (700 KB)

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

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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.
參考文獻(xiàn)	[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 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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

Help & FAQs

Do most proteins show cross-species activity?
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阿比特龍坦度酮羅阿比特倫CB7598CB 7598Cytochrome P450CYPsInhibitorinhibitorinhibit

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Abiraterone (Synonyms: 阿比特龍; CB-7598)

Customer Review

Other Forms of Abiraterone:

MCE 顧客使用本產(chǎn)品發(fā)表的 19 篇科研文獻(xiàn)

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摩爾計(jì)算器

稀釋計(jì)算器

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Abiraterone (Synonyms: 阿比特龍; CB-7598)

Customer Review

Other Forms of Abiraterone:

Abiraterone 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 19 篇科研文獻(xiàn)

Abiraterone 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Cytochrome P450 亞型特異性產(chǎn)品:

生物活性

實(shí)驗(yàn)參考方法

純度 & 產(chǎn)品資料

參考文獻(xiàn)

Abiraterone 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

Abiraterone 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

Keywords:

您最近查看的產(chǎn)品:

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