Abiraterone (Synonyms: CB-7598)

Name: Abiraterone
Brand: MedChemExpress
SKU: HY-70013
Rating: 5.0 (19 reviews)

Cat. No.: HY-70013 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Abiraterone Chemical Structure

CAS No. : 154229-19-3

Size	Price	Stock	Quantity
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 81	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
1 g	USD 198	In-stock	Estimated Time of Arrival: December 31
2 g	USD 317	In-stock	Estimated Time of Arrival: December 31
5 g	USD 581	In-stock	Estimated Time of Arrival: December 31
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Based on 19 publication(s) in Google Scholar

Other Forms of Abiraterone:

19 Publications Citing Use of MCE Abiraterone

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View All Cytochrome P450 Isoform Specific Products:

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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CYP17

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]

In Vitro

Significant inhibition of proliferation of the AR-positive prostate cancer cell lines LNCaP and VCaP with doses of Abiraterone ≥5 μM is confirmed^[2]. Abiraterone shows IC₅₀ values of 15 nM and 2.5 nM for the 17,20-lyase and 17α-hydroxylase (CYP17 is a bifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activity). Abiraterone inhibits human 17,20-lyase and 17α-hydroxylase with IC₅₀ of 27 and 30 nM respectively^[3]. Abiraterone inhibits recombinant human 3βHSD1 and 3βHSD2 activity with competitive K_i values of 2.1 and 8.8 μM. 10 μM Abiraterone is sufficient to completely block synthesis of 5α-dione and DHT in both cell lines.Treatment with abi significantly inhibited CRPC progression in the robustly growing subset, effectively putting a ceiling on tumor growth over 4 weeks of treatment (P<0.00001). [³H]-dehydroepiandrosterone (DHEA) depletion and Δ⁴-androstenedione (AD) accumulation are inhibited by Abiraterone in LNCaP, with an IC₅₀<1 μM^[4].

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

In Vivo

The 0.5 mmol/kg/d Abiraterone treatment dose is previously shown to yield serum concentrations of about 0.5 to 1 μM. Xenograft tumor growth in the control group is widely variable, with some tumors growing slowly and only a subset of tumors exhibiting robust growth^[4]. Following i.v. administration (5 mg/kg) the clearance (Cl) and volume of distribution (V_d) are found to be 31.2 mL/min/kg and 1.97 L/kg, respectively. The AUC_0-∞ (area under the plasma concentration-time curve from time zero to infinity time point) is found to be 2675 ng*h/mL. The terminal half-life (t_1/2) is 0.73 h. Because of high clearance, Abiraterone (ART) is quantifiable only until 2 h following i.v. administration^[5].

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

Clinical Trial

Molecular Weight

349.51

Formula

C₂₄H₃₁NO

CAS No.

154229-19-3

Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12C(C3=CN=CC=C3)=CC[C@]1([C@@]4(CC=C5[C@@](C)([C@]4(CC2)[H])CC[C@@H](C5)O)[H])[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMF : 5 mg/mL (14.31 mM; ultrasonic and warming and heat to 60°C)

Ethanol : 5 mg/mL (14.31 mM; ultrasonic and warming and heat to 60°C)

DMSO : 2.5 mg/mL (7.15 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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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

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.88%

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Data Sheet (285 KB) SDS (700 KB)

COA (254 KB) RP-HPLC (146 KB)

Handling Instructions (2659 KB)

References

[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.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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

Abiraterone Related Classifications

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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-7598CB7598CB 7598Cytochrome P450CYPsInhibitorinhibitorinhibit

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Abiraterone (Synonyms: CB-7598)

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Other Forms of Abiraterone:

Abiraterone Related Antibodies

19 Publications Citing Use of MCE Abiraterone

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