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Abiraterone (CB-7598)

Name: Abiraterone (CB-7598)
Brand: Selleck Chemicals
SKU: S1123
Rating: 5 (33 reviews)

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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P450 (e.g. CYP17) Signaling Pathway Map

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=

Click to View More Cell Line Experimental Data

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]	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 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.

References

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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
Storage	2 years	-80°C	in solvent
Smiles	CC12CCC(CC1=CCC3C2CCC4(C3CC=C4C5=CN=CC=C5)C)O

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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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