Abiraterone Acetate (CB7630)

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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Biological Activity

Description 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.
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 C17,20-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?=
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]

  • C17,20-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.

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.

30 mg/mL

Chemical Information

Molecular Weight 391.55
Formula

C26H33NO2

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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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