Abiraterone (CB-7598)

Catalog No.S1123

For research use only.

Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.

Abiraterone (CB-7598) Chemical Structure

CAS No. 154229-19-3

Selleck's Abiraterone (CB-7598) has been cited by 33 publications

Purity & Quality Control

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Biological Activity

Description Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.
Features Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.
Targets
CYP17 [1]
(Cell-free assay)
2 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
JM109 NGDyeYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVHncFF4UW6qaXLpeIlwdiCxZjDDMZRmem2rbnHsJGhqey22YXfn[YQhemWlb33ibY5idnRiaIXtZY4hS1mSMUfBNYRmdHSjMUnIJI12fGGwdDDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBLVTFyOTDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBxem:pZYP0[ZJwdmViaInkdo95gWyjdHnvckBqdiCycnXz[Y5k\SCxZjDjfZRw[2i{b33lJHA1PTBicnXkeYN1[XOnIHL5JGhRVENvVW[gcYV1cG:mLDDJR|UxRTBwMEC5OO69VS5? NVOxfJc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3PVI4ODNpPkK5O|kzPzB|PD;hQi=>
P450c17-LNCaP M2HSZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkG4TY4hfmm2cn:gZ5l1d2Oqcn;t[UBRPDVyIEG3RVEhcW6qaXLpeIlwdiC5YYOgZZN{[XmnZDD1d4lv\yC2aHWgdoFxcWRiYXPleIlkKGGlaXSgdoVt\WG|aX7nJIF{e2G7IDjBRXJCMSxidYTpcIl7cW6pIHnueIFkfCCSNEWwZ|E4NWW6cILld5NqdmdiRYPjbIVzcWOqaXGgZ49tcSCxcjDQOFUx[zF5LVzOR4FRKGOnbHzzJIF{KHSqZTDlcpp6dWVic3;1doNmNCCLQ{WwQVAvQM7:TT6= M2P2b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{N{ezNFM6Lz5zMke3N|A{QTxxYU6=
V79MZh11B1 M3vSR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEHVZmRKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlEh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppOTGEMTDj[YxteyxiSVO1NF0yNjZyON88UU4> NH[2S2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[3Nlg3QCd-MUi2O|I5Pjh:L3G+
V79MZh11B1 NIrOe2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\He5h2UW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCneIDy[ZN{\WRiaX6gWlc6VVqqMUHCNUBk\WyuczygTWM2OD1zLk[wPO69VS5? NVXkXIlWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyNVEyPzRpPkG5NlEyOTd2PD;hQi=>
V79MZh MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnnHTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abEBk\WyuczygTWM2OD1zLk[x{txONg>? NW\oUWQ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1OVAyOThpPkKwOVUxOTF6PD;hQi=>
V79MZh NUfZeVk1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXjJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkGg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWroJINmdGy|IIXzbY5oKFtzLEKtN2heNTFzLXTlc5h6[2:{dHnjc5N1\XKxbnWgZZMhe3Wkc4TyZZRmNCCLQ{WwQVEvPjIQvF2u MmLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUmxOFkoRjJ|OEW5NVQ6RC:jPh?=
V79MZh M1vaUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnmzTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abEBk\WyuczygTWM2OD1zLke1{txONg>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV3MEGxPEc,OjB3NUCxNVg9N2F-
V79MZh NVX5U5EyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlPUTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abEBk\WyuczD1d4lv\yCdMTyyMVNJZS1zMT3k[Y95gWOxcoTpZ49{fGW{b37lJIF{KHO3YoP0doF1\SxiSVO1NF0yNjd3zszNMi=> NYC2V4tJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVkyPDlpPkKzPFU6OTR7PD;hQi=>
V79MZh11B2 MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnLITY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abFEySjJiY3XscJMtKEmFNUC9NU44PTIQvF2u MmjOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh4N{K4OlgoRjF6NkeyPFY5RC:jPh?=
LNCAP NWfocHR[SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmXnO|IhcHK| M1u2bGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1|LkK5{txONg>? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTNzMECyOkc,Ojl|MUCwNlY9N2F-
hTERT-BJ M3;m[GN6fG:2b4jpZ4l1gSCjc4PhfS=> M{myO|Q5KGi{cx?= M4i1bmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIhVTVKWLVLKJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJHNTSiCjc4PhfUwhT0l3ME20MlXPxE1w MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF5MkC4NEc,OjlzN{KwPFA9N2F-
PC3 NWi1blNVSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M17TbFczKGi{cx?= M4jTXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS57NN88UU4> M2fs[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{GwNFI3Lz5{OUOxNFAzPjxxYU6=
MGC803 M{nHT2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MnzTO|IhcHK| M4iydWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVfDPFA{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Nz63Nu69VS5? NHH2cpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOxNFAzPid-MkmzNVAxOjZ:L3G+
HeLa NHTVc2xCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MlvkOFghcHK| NHjwZoZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD15LkpOwG0v MnXsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzN{KwPFAoRjJ7MUeyNFgxRC:jPh?=
PC3 MXnDfZRwfG:6aXPpeJkh[XO|YYm= MYe0PEBpenN? M2\tc2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvOzMQvF2u Ml3rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNEi4N|coRjJ2MUS4PFM4RC:jPh?=
GES-1 NEnhcmtCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnfpO|IhcHK| MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEeHUz2xJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTNwMUNOwG0v NVK2d45qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzNVAxOjZpPkK5N|ExODJ4PD;hQi=>
T47D NX2xeJVrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHWxfZA4OiCqcoO= NEPVSpZIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBVPDeGIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NVYvQc7:TT6= M{X6R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MkC5OVYzLz5{N{KwPVU3OjxxYU6=
MDA-MB-231 M4TJR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX;ndZUxPzJiaILz MkfJS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTF7LkNOwG0v MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzJyOUW2Nkc,Ojd{MEm1OlI9N2F-
MCF7 NV33dmNFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIi4ZW44OiCqcoO= NFvkfmhIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NVkvO87:TT6= NFu0VpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{KwPVU3Oid-MkeyNFk2PjJ:L3G+
MDA-MB-361 NHq2VHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYjKfGlYPzJiaILz MoXQS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWRCNU2ELUO2NUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTJyLkVOwG0v NIq0em49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{KwPVU3Oid-MkeyNFk2PjJ:L3G+
T47D MVrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NIHKWWY1QCCqcoO= NFPFOXZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OD1{NN88UU4> NXL0dotiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxO|IxQDBpPkK5NVczODhyPD;hQi=>
WiDr Mnq2RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NF7OW4Y1QCCqcoO= M3rufGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iV3nEdkBk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxRTR{zszNMi=> M1rKUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUeyNFgxLz5{OUG3NlA5ODxxYU6=
Assay
Methods Test Index PMID
Western blot eIF4E / eIF4G / eIF4E / eIF4G / AR ; p-4EBP1 / 4EBP1 22174412
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]

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 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 Research:[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 Research:[5]
  • Animal Models: LAPC-4 xenograft mice
  • Dosages: 0.15 mmol/kg
  • Administration: Administered via s.c.

Solubility (25°C)

In vitro

DMSO 0 mg/mL
(0.0 mM)
Water 0 mg/mL
(0.0 mM)
Ethanol '''0 mg/mL

Chemical Information

Molecular Weight 349.51
Formula

C24H31NO

CAS No. 154229-19-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12CCC(CC1=CCC3C2CCC4(C3CC=C4C5=CN=CC=C5)C)O

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.
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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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