Buy Abiraterone (CB-7598) | P450 (e.g. CYP17) Inhibitors | Price | IC50

Validation & Quality Control

Product Citations(2)

Chem Res Toxicol, 2012, 25(8), 1720-1731

J Pharm Biomed Anal, 2013, 74:77-82

Quality Control & MSDS

Related Compound Libraries

Abiraterone (CB-7598) is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) FDA Approved Drug Library (96-well)

Product Information

Compare P450 (e.g. CYP17) Inhibitors

Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1250	MDV3100 (Enzalutamide)	<1 mg/mL	93 mg/mL	3 mg/mL
S2246	Abiraterone Acetate (CB7630)	<1 mg/mL	<1 mg/mL	28 mg/mL
S1190	Bicalutamide (Casodex)	<1 mg/mL	86 mg/mL	7 mg/mL
S1123	Abiraterone (CB-7598)	<1 mg/mL	0.33 mg/mL	<1 mg/mL
S2187	Avasimibe(CI-1011)	<1 mg/mL	100 mg/mL	8 mg/mL
S1442	Voriconazole	<1 mg/mL	70 mg/mL	20 mg/mL
S1353	Ketoconazole	<1 mg/mL	16 mg/mL	10 mg/mL
S1908	Flutamide (Eulexin)	<1 mg/mL	55 mg/mL	55 mg/mL
S2555	Clarithromycin (Biaxin, Klacid)	<1 mg/mL	18 mg/mL	<1 mg/mL
S2042	Cyproterone acetate	<1 mg/mL	≥83 mg/mL	≥10 mg/mL
S2803	Galeterone (TOK-001)	<1 mg/mL	24 mg/mL	40 mg/mL
S1195	TAK-700 (Orteronel)	<1 mg/mL	61 mg/mL	8 mg/mL
S2526	Alizarin	<1 mg/mL	48 mg/mL	<1 mg/mL
S2046	Pioglitazone HCl (Actos)	<1 mg/mL	79 mg/mL	4 mg/mL
S2921	PF-4981517	<1 mg/mL	91 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Product Citations Tech Support & FAQs

Biological Activity

Description	Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM.
Targets	CYP17
IC50	2 nM ^[1]
In vitro	Abiraterone binds and inhibits wild-type and mutant androgen receptor (AR). Abiraterone inhibits in vitro proliferation and androgen receptor-regulated gene expression of androgen receptor-positive prostate cancer cells, which could be explained by androgen receptor antagonism in addition to inhibition of steroidogenesis. In fact, activation of mutant androgen receptor by eplerenone is inhibited by greater concentrations of Abiraterone. Abiraterone displaces ligand from both WT-AR and T877A with EC50 of 13.4 μM and 7.9 μM, respectively. ^[2]Abiraterone inhibits lyase activity with an IC50 of 5.8 nM in rat testis microsomes. Abiraterone acetate significantly inhibits T secretion (−48%) and in turn increased LH concentration (192%).^[3]
In vivo	Abiraterone inhibits CYP17 with an IC50 of 72 nM, in human testicular microsomes. ^[4] Abiraterone fails to significantly reduce the size of any of the organs. ^[5] Abiraterone reduces the testosterone levels strongly, almost reaching the level of the orchiectomy control. The testosterone levels are reduced by Abiraterone for more than 95% compared to the control group. ^[6]
Clinical Trials	Abiraterone acetate plus prednisone has entered in a phase II clinical trial in the treatment of prostate cancer.
Features	Abiraterone has been approved for the treatment of docetaxel-treated castration-resistant prostate cancer (CRPC).

Protocol(Only for Reference)

Kinase Assay: ^[3]

C_17,20-lyase activity assay	Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contained 0.25 M sucrose, 20 mM Tris–HCl (pH 7.4), 10 mM G6P and 1.2 IU/mL G6PDH. After equilibration at 37 °C for 10 minutes, the reaction is initiated by addition of βNADP to obtain a final concentration of 0.6 mM. Prior to the distribution of 600 μL of the reaction mixture in each tube, Abiraterone is evaporated to dryness under a stream of nitrogen and then are incubated at 37 °C for 10 minutes. After incubation with Abiraterone, 500 μL of the reaction mixture is transferred to tubes containing 1 μM of the enzyme substrate, 17OHP. After a further 10 minutes incubation, tubes are placed on ice and the reaction is stopped by addition of 0.1 ml NaOH 1N. Tubes are deep-frozen and stored at −20 °C until assayed for Δ4A levels. A Δ4A RIA is developed and automated on a microplate format using a specific antibody against Δ4A. The separation of free and bound antigen is achieved with a dextran-coated charcoal suspension. After centrifugation, aliquots of the clear supernatant are counted in duplicates in a 1450 MicrobetaPlus liquid scintillation counter. The Δ4A concentrations of unknown samples are determined from the standard curve. The detection limit is 0.5 ng/mL and the within and between assay coefficients of variation are 10.7 and 17.6%, respectively at an assay value of 13 ng/mL. The rate of enzymatic reaction is expressed as pmol of Δ4A formed per 10 minutes and per mg of protein. The value of maximum activity without inhibitor (control) is set at 100%. The IC50 values are calculated using non-linear analysis from the plot of enzyme activity (%) against log of inhibitor concentration.

C_17,20-lyase activity assay

Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contained 0.25 M sucrose, 20 mM Tris–HCl (pH 7.4), 10 mM G6P and 1.2 IU/mL G6PDH. After equilibration at 37 °C for 10 minutes, the reaction is initiated by addition of βNADP to obtain a final concentration of 0.6 mM. Prior to the distribution of 600 μL of the reaction mixture in each tube, Abiraterone is evaporated to dryness under a stream of nitrogen and then are incubated at 37 °C for 10 minutes. After incubation with Abiraterone, 500 μL of the reaction mixture is transferred to tubes containing 1 μM of the enzyme substrate, 17OHP. After a further 10 minutes incubation, tubes are placed on ice and the reaction is stopped by addition of 0.1 ml NaOH 1N. Tubes are deep-frozen and stored at −20 °C until assayed for Δ4A levels. A Δ4A RIA is developed and automated on a microplate format using a specific antibody against Δ4A. The separation of free and bound antigen is achieved with a dextran-coated charcoal suspension. After centrifugation, aliquots of the clear supernatant are counted in duplicates in a 1450 MicrobetaPlus liquid scintillation counter. The Δ4A concentrations of unknown samples are determined from the standard curve. The detection limit is 0.5 ng/mL and the within and between assay coefficients of variation are 10.7 and 17.6%, respectively at an assay value of 13 ng/mL. The rate of enzymatic reaction is expressed as pmol of Δ4A formed per 10 minutes and per mg of protein. The value of maximum activity without inhibitor (control) is set at 100%. The IC50 values are calculated using non-linear analysis from the plot of enzyme activity (%) against log of inhibitor concentration.

Cell Assay: ^[2]

Cell lines	LNCaP and VCaP cells
Concentrations	0.1-5 μM
Incubation Time	24 hours or 96 hours
Method	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 at 24 hours and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence.

Animal Study: ^[5]

Animal Models	LAPC-4 xenograft mice
Formulation	0.3% hydroxypropyl cellulose
Dosages	0.15 mmol/kg
Administration	Administered via s.c.

1

References

Chemical Information

Download Abiraterone (CB-7598) SDF

Molecular Weight (MW)	349.51
Formula	C₂₄H₃₁NO
CAS No.	154229-19-3
Synonyms	N/A

Solubility (25°C) DMSO 0.33 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Product Citations (2)

Screening for modulatory effects on steroidogenesis using the human H295R adrenocortical cell line: a metabolomics approach. [Rijk JC, et al. Chem Res Toxicol 2012;25(8), 1720-1731]
PubMed: 22768806
Analysis of abiraterone stress degradation behavior using liquid chromatography coupled to ultraviolet detection and electrospray ionization mass spectrometry. [Khedr A, et al. J Pharm Biomed Anal 2013;74:77-82]
PubMed: 23245237

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related P450 (e.g. CYP17) Inhibitors

TAK-700 (Orteronel)
TAK-700 (Orteronel) is a potent and highly selective rat and human 17,20-lyase inhibitor with IC50 of 54 nM and 38 nM, respectively.
Cyproterone acetate
Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM.
Avasimibe(CI-1011)
Avasimibe inhibits ACAT and CYP2C9 with IC50 of 3.3 μM and 2.9 μM, respectively.
Alizarin
Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2 μM, 10.0 μM and 2.7 μM, respectively.
TH-302
TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM.
Galeterone (TOK-001)
Galeterone (TOK-001, VN/124-1) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively.
PF-4981517
PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM.
Varespladib (LY315920)
LY315920 (Varespladib) is a potent and selective secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM.
MK-8245
MK-8245 is an inhibitor of stearoyl-CoA desaturase (SCD) which targets the liver with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1.
Tipifarnib (Zarnestra)
Tipifarnib (Zarnestra, R115777) is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM.

Choose Your Country or Region

Product Categories

Abiraterone (CB-7598)

Validation & Quality Control

Product Citations(2)

Quality Control & MSDS

Related Compound Libraries

Abiraterone (CB-7598) is available in the following compound libraries:

Product Information

Compare P450 (e.g. CYP17) Inhibitors

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: ^[3]

Cell Assay: ^[2]

Animal Study: ^[5]

References

Chemical Information

Research Area

Product Citations (2)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related P450 (e.g. CYP17) Inhibitors

Recently Viewed Items

Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1250	MDV3100 (Enzalutamide)	<1 mg/mL	93 mg/mL	3 mg/mL
S2246	Abiraterone Acetate (CB7630)	<1 mg/mL	<1 mg/mL	28 mg/mL
S1190	Bicalutamide (Casodex)	<1 mg/mL	86 mg/mL	7 mg/mL
S1123	Abiraterone (CB-7598)	<1 mg/mL	0.33 mg/mL	<1 mg/mL
S2187	Avasimibe(CI-1011)	<1 mg/mL	100 mg/mL	8 mg/mL
S1442	Voriconazole	<1 mg/mL	70 mg/mL	20 mg/mL
S1353	Ketoconazole	<1 mg/mL	16 mg/mL	10 mg/mL
S1908	Flutamide (Eulexin)	<1 mg/mL	55 mg/mL	55 mg/mL
S2555	Clarithromycin (Biaxin, Klacid)	<1 mg/mL	18 mg/mL	<1 mg/mL
S2042	Cyproterone acetate	<1 mg/mL	≥83 mg/mL	≥10 mg/mL
S2803	Galeterone (TOK-001)	<1 mg/mL	24 mg/mL	40 mg/mL
S1195	TAK-700 (Orteronel)	<1 mg/mL	61 mg/mL	8 mg/mL
S2526	Alizarin	<1 mg/mL	48 mg/mL	<1 mg/mL
S2046	Pioglitazone HCl (Actos)	<1 mg/mL	79 mg/mL	4 mg/mL
S2921	PF-4981517	<1 mg/mL	91 mg/mL	<1 mg/mL

Choose Your Country or Region

Product Categories

Abiraterone (CB-7598)

Validation & Quality Control

Product Citations(2)

Quality Control & MSDS

Related Compound Libraries

Abiraterone (CB-7598) is available in the following compound libraries:

Product Information

Compare P450 (e.g. CYP17) Inhibitors

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: [3]

Cell Assay: [2]

Animal Study: [5]

References

Chemical Information

Research Area

Product Citations (2)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related P450 (e.g. CYP17) Inhibitors

Recently Viewed Items

E-newsletter

Kinase Assay: ^[3]

Cell Assay: ^[2]

Animal Study: ^[5]