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Abiraterone Acetate (CB7630)

Name: Abiraterone Acetate (CB7630)
Brand: Selleck Chemicals
SKU: S2246
Rating: 5 (27 reviews)

Catalog No.S2246

For research use only.

Abiraterone Acetate (CB7630) is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor.

Abiraterone Acetate (CB7630) Chemical Structure

CAS No. 154229-18-2

Selleck's Abiraterone Acetate (CB7630) has been cited by 27 publications

Purity & Quality Control

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P450 (e.g. CYP17) Signaling Pathway Map

Biological Activity

Description

Features

Abiraterone is a drug used in castration-resistant prostate cancer.

Targets

CYP17 ^[1]
(Cell-free assay)

72 nM

In vitro

Abiraterone shows a good complexation with the heme iron only in SM1. ^[1] Abiraterone blocks the synthesis of androgens by inhibiting CYP17A1. Abiraterone also blocks 3β-hydroxysteroid dehydrogenase (3βHSD), an enzyme that is absolutely required for the synthesis of biologically active androgens. Abiraterone inhibits conversion of DHEA to Δ⁴-androstenedione. Abiraterone inhibition of 3βHSD blocks DHT synthesis and the androgen receptor response. Abiraterone inhibits the conversion of Δ⁵-androstenediol to testosterone. ^[2] Abiraterone inhibits C_17,20-lyase, with an IC50 of 5.8 nM, in rat testis microsomes. Abiraterone significantly inhibits testosterone secretion (−48%) and in turn increases LH concentration (192%). ^[3] Abiraterone inhibits in vitro proliferation and AR-regulated gene expression of AR-positive prostate cancer cells, which could be explained by AR antagonism in addition to inhibition of steroidogenesis. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

JM109	MmDQSpVv[3Srb36gZZN{[Xl?		NXHsUpZbUW6qaXLpeIlwdiCxZjDDMZRmem2rbnHsJGhqey22YXfn[YQhemWlb33ibY5idnRiaIXtZY4hS1mSMUfBNYRmdHSjMUnIJI12fGGwdDDlfJBz\XO\|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBLVTFyOTDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG\|ZTDpckBxem:pZYP0[ZJwdmViaInkdo95gWyjdHnvckBqdiCycnXz[Y5k\SCxZjDjfZRw[2i{b33lJHA1PTBicnXkeYN1[XOnIHL5JGhRVENvVW[gcYV1cG:mLDDJR\|UxKD1iMD6wNFk1KM7:TT6=	NEOzTIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe5NlcxOyd-Mkm3PVI4ODN:L3G+
P450c17-LNCaP	MlvOSpVv[3Srb36gZZN{[Xl?		M2jheGlvKH[rdILvJIN6fG:laILvcYUhWDR3MDCxO2EyKGmwaHnibZRqd25id3HzJIF{e2G7ZXSgeZNqdmdidHjlJJJieGmmIHHj[ZRq[yCjY3nkJJJmdGWjc3nu[{Bie3OjeTCoRWFTSSluIIX0bYxqgmmwZzDpcpRi[3RiUES1NIMyPy2neIDy[ZN{cW6pIFXzZ4hmemmlaHnhJINwdGlib4KgVFQ2OGNzNz3MUmNiWCClZXzsd{BieyC2aHWg[Y57gW2nIIPveZJk\SxiSVO1NEA:KDBwODFOwG0v	NEjXSo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMke3N\|A{QSd-MUK3O\|MxOzl:L3G+
V79MZh11B1	M3O3cWZ2dmO2aX;uJIF{e2G7		Mon4TY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abFEySjFiY3XscJMtKEmFNUCgQUAyNjZyODFOwG0v	M{LRZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkeyPFY5Lz5zOE[3Nlg3QDxxYU6=
V79MZh11B1	M2nzeWZ2dmO2aX;uJIF{e2G7		M4HpSmlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgR3lROTGEMTDlfJBz\XO\|ZXSgbY4h\XiycnXzd4VlKGmwIG[3PW1bcDFzQkGgZ4VtdHNuIFnDOVAhRSBzLk[wPEDPxE1w	MkPRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{MUGxO\|QoRjF7MkGxNVc1RC:jPh?=
V79MZh	Mn7CSpVv[3Srb36gZZN{[Xl?		MmnITY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abEBk\WyuczygTWM2OCB;IEGuOlEh\|ryPLh?=	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV3MEGxPEc,OjB3NUCxNVg9N2F-
V79MZh	MXXGeY5kfGmxbjDhd5NigQ>?		NVm4UG8zUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{B2e2mwZzDbNUwzNTOKXT2xNU1l\W:6eXPvdpRq[2:\|dHXyc45mKGG\|IIP1ZpN1emG2ZTygTWM2OCB;IEGuOlEh\|ryPLh?=	Mn\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUmxOFkoRjJ\|OEW5NVQ6RC:jPh?=
V79MZh	NHu2OFFHfW6ldHnvckBie3OjeR?=		NYDhOFZ{UW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIzKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{whUUN3MDC9JFEvPzVizszNMi=>	MlSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3NUCxNVgoRjJyNUWwNVE5RC:jPh?=
V79MZh	NV\nZ\|BLTnWwY4Tpc44h[XO\|YYm=		NFTadpdKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppKGOnbHzzJJV{cW6pIGuxMFIuO0ifLUGxMYRmd3i7Y3;yeIlkd3O2ZYLvcoUh[XNic4Xid5Rz[XSnLDDJR\|UxKD1iMT63OUDPxE1w	MmDIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUmxOFkoRjJ\|OEW5NVQ6RC:jPh?=
V79MZh11B2	MUjGeY5kfGmxbjDhd5NigQ>?		M{O5TmlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogyOUJ{IHPlcIx{NCCLQ{WwJF0hOS55NUGg{txONg>?	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDZ5Mki2PEc,OTh4N{K4Olg9N2F-
LNCAP	NVTUbnF2SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	MnnEO\|IhcHK\|	M{\pXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEOuNlkh\|ryPLh?=	NFGyeZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOxNFAzPid-MkmzNVAxOjZ:L3G+
hTERT-BJ	MVzDfZRwfG:6aXPpeJkh[XO\|YYm=	NHWwR401QCCqcoO=	NFn5NlJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBpXEWUVD3CTkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BUWkJiYYPzZZktKEeLNUCgQUA1NjVizszNMi=>	M1e1eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUeyNFgxLz5{OUG3NlA5ODxxYU6=
PC3	NIezcJZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	MkHEO\|IhcHK\|	NV7pVFh6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR\|Mh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEWuPVQh\|ryPLh?=	NXLE[I5iRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzNVAxOjZpPkK5N\|ExODJ4PD;hQi=>
MGC803	NGXHd4dCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	NX\GTW1wPzJiaILz	NW\GVHc5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNS2M5ODNiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFcvPzJizszNMi=>	NUDBVmp7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzNVAxOjZpPkK5N\|ExODJ4PD;hQi=>
HeLa	NV3lVHE{SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	M2T0clQ5KGi{cx?=	Mkf5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZVzhJINmdGy\|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJOVAhRSB5Lkmg{txONg>?	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF5MkC4NEc,OjlzN{KwPFA9N2F-
PC3	NXHRfXJPS3m2b4TvfIlkcXS7IHHzd4F6	M2n3dVQ5KGi{cx?=	NH;6SG9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDlwM{Kg{txONg>?	NWDKTWJoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOFg5OzdpPkK0NVQ5QDN5PD;hQi=>
GES-1	NYX3fYx7SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	M{PsO\|czKGi{cx?=	MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEeHUz2xJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzMz6xNkDPxE1w	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTNzMECyOkc,Ojl\|MUCwNlY9N2F-
T47D	M1ftN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MVK3NkBpenN?	MXvHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDUOFdFKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCxOk46KM7:TT6=	M3vNS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MkC5OVYzLz5{N{KwPVU3OjxxYU6=
MDA-MB-231	M4D6RWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MlLvO\|IhcHK\|	NU\QOoVST3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyIE2gNVkvOiEQvF2u	M{L4UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MkC5OVYzLz5{N{KwPVU3OjxxYU6=
MCF7	Ml\JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MVy3NkBpenN?	MkXNS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyIE2gNVkvOyEQvF2u	MoTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd{MEm1OlIoRjJ5MkC5OVYzRC:jPh?=
MDA-MB-361	MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NXnEPXRGPzJiaILz	M{H6TWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2zOlEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEKwMlQh\|ryPLh?=	NXjG[\|V2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkeyNFk2PjJpPkK3NlA6PTZ{PD;hQi=>
T47D	NGHmXlhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	M{HWdlQ5KGi{cx?=	MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiR1m1NEA:KDJ2IN88UU4>	M17WblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUeyNFgxLz5{OUG3NlA5ODxxYU6=
WiDr	MX;BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	MoXwOFghcHK\|	M1mxT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iV3nEdkBk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxKD1iNEKg{txONg>?	MoLuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzN{KwPFAoRjJ7MUeyNFgxRC:jPh?=

Click to View More Cell Line Experimental Data

In vivo

Following intraperitoneal administration in a rodent model, abiraterone was found to have rapid deacetylation. When administered as its acetate pro-drug (CB 7630), it suppressed circulating testosterone to undetectable levels and markedly decreased the weights of androgen sensitive organs. Abiraterone is well tolerated and the mean elimination half-life of abiraterone in these studies was 27.6 h (thus supporting the use of once-daily dosing)^[5]. Preclinical studies with abiraterone demonstrated reduction in androgen production downstream of CYP17 which resulted in decreased weight of the ventral prostate, testis, and seminal vesicles in mice^[6].

Protocol (from 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 contains 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, test compounds are 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 in our laboratory using a specific antibody against Δ4A and instructions provided by Biogenesis. 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 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 Research: ^[4]	Cell lines: LNCaP and VCaP cells Concentrations: 0 μM -10 μM Incubation Time: 24 hours and 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 Research: ^[2]	Animal Models: Male NOD/SCID mice with LAPC4 cells Dosages: 0.5 mmol/kg/d Administration: Administered via s.c.

References

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Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 5% DMSO+95% Corn oil For best results, use promptly after mixing. Click to purchase: Corn Oil	30 mg/mL

Chemical Information

Molecular Weight	391.55
Formula	C₂₆H₃₃NO₂
CAS No.	154229-18-2
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC(=O)OC1CCC2(C3CCC4(C(C3CC=C2C1)CC=C4C5=CN=CC=C5)C)C

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04587427	Not yet recruiting	Drug: Radium 223 dichloride (Xofigo BAY88-8223)	Metastatic Castration-resistant Prostate Cancer (mCRPC)	Bayer	March 31 2022	--
NCT05177042	Recruiting	Drug: ARV-110 in Combination with Abiraterone	Prostate Cancer Metastatic	Arvinas Androgen Receptor Inc.\|Arvinas Inc.	January 7 2022	Phase 1
NCT04887506	Recruiting	Drug: TAVT-45\|Drug: Zytiga\|Drug: Prednisone	Metastatic Castration-resistant Prostate Cancer\|Metastatic Castration-sensitive Prostate Cancer\|Metastatic Prostate Cancer	Tavanta Therapeutics	April 14 2021	Phase 3
NCT04862091	Recruiting	Drug: Abiraterone Acetate Tablets (I)\|Drug: ZYTIGA®	Metastatic Castration-resistant Prostate Cancer (mCRPC)	Jiangsu HengRui Medicine Co. Ltd.	April 23 2021	Phase 2
NCT04458311	Recruiting	Drug: Abiraterone Acetate\|Drug: Tildrakizumab	Metastatic Castration Resistant Prostate Cancer	Institute of Cancer Research United Kingdom\|Sun Pharmaceutical Industries Limited	December 1 2020	Phase 1\|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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

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