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 26 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 NFHGR2VHfW6ldHnvckBie3OjeR?= MlrCTY5pcWKrdHnvckBw\iCFLYTldo1qdmGuIFjpd{11[WepZXSgdoVkd22kaX7hcpQhcHWvYX6gR3lROTeDMXTlcJRiOTmKIH31eIFvfCCneIDy[ZN{\WRiaX6gSZNkcGW{aXPobYEh[2:uaTDKUVExQSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDwdo9o\XO2ZYLvcoUhcHmmcn;4fYxifGmxbjDpckBxemW|ZX7j[UBw\iCleYTvZ4hzd22nIGC0OVAhemWmdXP0ZZNmKGK7IFjQUGMuXVZibXX0bI9lNCCLQ{WwJF0hOC5yMEm0JO69VS5? NVfySYtJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3PVI4ODNpPkK5O|kzPzB|PD;hQi=>
P450c17-LNCaP NWjKZ4FPTnWwY4Tpc44h[XO|YYm= NXOzUndpUW5idnn0do8h[3m2b3Podo9u\SCSNEWwJFE4STFiaX7obYJqfGmxbjD3ZZMh[XO|YYnl[EB2e2mwZzD0bIUhemGyaXSgZYNmfGmlIHHjbYQhemWuZXHzbY5oKGG|c3H5JEhCSVKDKTygeZRqdGm8aX7nJIlvfGGldDDQOFUx[zF5LXX4dJJme3OrbnegSZNkcGW{aXPobYEh[2:uaTDvdkBRPDVyY{G3MWxPS2GSIHPlcIx{KGG|IITo[UBmdnq7bXWgd492emOnLDDJR|UxKD1iMD64JO69VS5? MlW5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJ5N{OwN|koRjF{N{ezNFM6RC:jPh?=
V79MZh11B1 NELoSIZHfW6ldHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkGg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWroNVFDOSClZXzsd{whUUN3MDC9JFEvPjB6IN88UU4> MoLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh4N{K4OlgoRjF6NkeyPFY5RC:jPh?=
V79MZh11B1 MXnGeY5kfGmxbjDhd5NigQ>? NVXBcWN5UW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCneIDy[ZN{\WRiaX6gWlc6VVqqMUHCNUBk\WyuczygTWM2OCB;IEGuOlA5KM7:TT6= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJzMUG3OEc,OTl{MUGxO|Q9N2F-
V79MZh NHfQRotHfW6ldHnvckBie3OjeR?= NYO3ZlN4UW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{whUUN3MDC9JFEvPjFizszNMi=> MnP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3NUCxNVgoRjJyNUWwNVE5RC:jPh?=
V79MZh NIKzdG1HfW6ldHnvckBie3OjeR?= NXTTO2ZPUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{B2e2mwZzDbNUwzNTOKXT2xNU1l\W:6eXPvdpRq[2:|dHXyc45mKGG|IIP1ZpN1emG2ZTygTWM2OCB;IEGuOlEh|ryPLh?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3OUG0PUc,OjN6NUmxOFk9N2F-
V79MZh MVvGeY5kfGmxbjDhd5NigQ>? NHiwcJRKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppKGOnbHzzMEBKSzVyIE2gNU44PSEQvF2u MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV3MEGxPEc,OjB3NUCxNVg9N2F-
V79MZh MnLCSpVv[3Srb36gZZN{[Xl? NGC4Zm9KdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppKGOnbHzzJJV{cW6pIGuxMFIuO0ifLUGxMYRmd3i7Y3;yeIlkd3O2ZYLvcoUh[XNic4Xid5Rz[XSnLDDJR|UxKD1iMT63OUDPxE1w MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3OUG0PUc,OjN6NUmxOFk9N2F-
V79MZh11B2 NW\aTWFKTnWwY4Tpc44h[XO|YYm= MofGTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abFEySjJiY3XscJMtKEmFNUCgQUAyNjd3MTFOwG0v M{fJRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkeyPFY5Lz5zOE[3Nlg3QDxxYU6=
LNCAP M{HvUmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M2fqUlczKGi{cx?= MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB|LkK5JO69VS5? M2O0bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{GwNFI3Lz5{OUOxNFAzPjxxYU6=
hTERT-BJ NHPzRYREgXSxdH;4bYNqfHliYYPzZZk> MV20PEBpenN? M37hPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIhVTVKWLVLKJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJHNTSiCjc4PhfUwhT0l3MDC9JFQvPSEQvF2u MljjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzN{KwPFAoRjJ7MUeyNFgxRC:jPh?=
PC3 M2LKZ2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVPGZW1QPzJiaILz MofHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDVwOUSg{txONg>? NF3Idmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOxNFAzPid-MkmzNVAxOjZ:L3G+
MGC803 MmfyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NVHIO3hQPzJiaILz MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2JQ{iwN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iNz63NkDPxE1w NWjrVXJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzNVAxOjZpPkK5N|ExODJ4PD;hQi=>
HeLa M2m5bWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mn3ROFghcHK| MmLDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJOVAhRSB5Lkmg{txONg>? MmPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzN{KwPFAoRjJ7MUeyNFgxRC:jPh?=
PC3 MUPDfZRwfG:6aXPpeJkh[XO|YYm= Ml72OFghcHK| NXTBb5JNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB7LkOyJO69VS5? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF2OEizO{c,OjRzNEi4N|c9N2F-
GES-1 M3HjTmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXLHb5J{PzJiaILz MnLMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCJRWOtNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMUOuNVIh|ryPLh?= NIfVbnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOxNFAzPid-MkmzNVAxOjZ:L3G+
T47D M4LDe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFfqcpM4OiCqcoO= MnPKS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gWFQ4TCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVYvQSEQvF2u MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzJyOUW2Nkc,Ojd{MEm1OlI9N2F-
MDA-MB-231 MkC1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mlz2O|IhcHK| NYPob4U3T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVkvOiEQvF2u M13ud|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MkC5OVYzLz5{N{KwPVU3OjxxYU6=
MCF7 MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3XW[FczKGi{cx?= NFKwRo5Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAyQS5|IN88UU4> NYnpRVZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkeyNFk2PjJpPkK3NlA6PTZ{PD;hQi=>
MDA-MB-361 M2frO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NILUepg4OiCqcoO= NIHGZ41Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtN|YyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCyNE41KM7:TT6= M1:0N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MkC5OVYzLz5{N{KwPVU3OjxxYU6=
T47D MX7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NH3sTnU1QCCqcoO= NF2xelFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OCB;IEK0JO69VS5? M{LrZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUeyNFgxLz5{OUG3NlA5ODxxYU6=
WiDr MWTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1LYZlQ5KGi{cx?= M1;xc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iV3nEdkBk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxKD1iNEKg{txONg>? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF5MkC4NEc,OjlzN{KwPFA9N2F-
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.

  • (Only for Reference)
Animal Research:

[2]

  • Animal Models: Male NOD/SCID mice with LAPC4 cells
  • Dosages: 0.5 mmol/kg/d
  • Administration: Administered via s.c.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO Insoluble
Water Insoluble
Ethanol ''''28 mg/mL

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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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