Bicalutamide (ICI-176334)

For research use only.

Catalog No.S1190

36 publications

Bicalutamide (ICI-176334) Chemical Structure

CAS No. 90357-06-5

Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.

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Selleck's Bicalutamide (ICI-176334) has been cited by 36 publications

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Choose Selective Androgen Receptor Inhibitors

Biological Activity

Description Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Targets
Androgen Receptor [1]
(LNCaP/AR(cs) cells)
0.16 μM
In vitro

Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. Bicalutamide treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 results in altered gene expression consistent with its well-documented agonist activity in context of AR overexpression. Bicalutamide induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. Bicalutamide treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. Bicalutamide exhibits partial agonist activity as evidenced by induction of DNA binding at AR target genes and incomplete antagonism of the effects of R1881. In absence of R1881, Bicalutamide partially activates VP16-AR–mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrates AR-driven luciferase reporter construct. In the presence of R1881, Bicalutamide shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. [1] Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. [2] Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-bicalutamide combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-453 cells NYrnemZETnWwY4Tpc44h[XO|YYm= MUfEbZNxdGGlZX3lcpQhd2ZiW{PIYXIyQDhzIH\yc40hSVJiaX6gbJVu[W5iTVTBMW1DNTR3MzDj[YxteyxiRVO1NF0{OSCwTR?= NEHZXXYzOzdzM{W2Oy=>
LNCaP cells MUDGeY5kfGmxbjDhd5NigQ>? MVXJcohq[mm2aX;uJI9nKFt|SG2tSGhVKGKrbnTpcochfG9iVEi3O2Eh[W6mcn;n[Y4hemWlZYD0c5Ihd2ZiTF7DZXAh[2WubIOsJGtqRTN3IH7N M3v5WFE2PjB|OU[w
Freestyle293F cells MW\GeY5kfGmxbjDhd5NigQ>? NV3adIJEUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgRY5lem:pZX6gdoVk\XC2b4KgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hTnKnZYP0fYxmOjl|RjDj[YxteyxiSVO1NF0xNjB3NDFOwG0> NYj5cIR[OjNzOUm0O|c>
HEK293 cells M2HyZ2Z2dmO2aX;uJIF{e2G7 NXfVTW1GOyCq MVTEbZNxdGGlZX3lcpQhd2ZiW{G3MYFteGijLX3leIh6dC1|SG3tbYJwdGW{b37lJIZzd21iYX7kdo9o\W5icnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjZoTldkA{KGi{czygTWM2OD13NDDuUS=> MYeyNlM6OTB|Mx?=
MDA453 cells MkHpSpVv[3Srb36gZZN{[Xl? M13VNWRqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgbY4hVUSDNEWzJINmdGy|LDDLbV03PCCwTR?= NWCwXGVkOTh{OUG2OFQ>
human MDA-MB-453 cells M2rHRWZ2dmO2aX;uJIF{e2G7 MkLkSIl{eGyjY3Xt[Y51KG:oIGuzTH1FUFRiZoLvcUBCWiCrbjDoeY1idiCPRFGtUWIuPDV|IHPlcIx{NCCLQ{WwQVY1KG6P MoHwNlA2QDR4MUC=
COS1 cells NWnyR|ExTnWwY4Tpc44h[XO|YYm= M3TUWmFvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBxW0d3LYTh[4dm\CCqdX3hckBidmS{b3flckBz\WOncITvdkBmgHC{ZYPz[YQhcW5iQ1;TNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icnXj[ZB1d3JvbXXkbYF1\WRidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGK7IFHSMZJm\3WuYYTl[EBz[XRicILvZoF{cW5icILvcY91\XJiZoLh[41mdnRiZILpeoVvKG[rcnXmcJkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCjc4PhfUwhUUN3ME2wMlA5PjlizszN MlLlNlU3PDZ4NEm=
HeLa cells MkjFSpVv[3Srb36gZZN{[Xl? NW\UbIVFSW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCjbnTyc4dmdiC{ZXPldJRweiCneIDy[ZN{\WRiaX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIRqcHmmcn;0[ZN1d3O2ZYLvcoUhcW6mdXPl[EB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgZpkhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF0xNjF2IN88US=> NH3ZPGMyPzhyNEKyPS=>
CV1 cells NYfSOYVlTnWwY4Tpc44h[XO|YYm= M4X6N2JqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEOYMTDj[YxteyxiS3m9NE4yPTFizszN MYqxO|I2Pzh|OB?=
monkey COS7 cells NVS5PIo6TnWwY4Tpc44h[XO|YYm= M1\YO2JqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKG2xbnvlfUBEV1N5IHPlcIx{KGK7IIfoc4xmKGOnbHygZolv\GmwZzDhd5NigSxiS3m9NE4yPTFizszN MVSxPFQ1OjlzMh?=
COS7 cells MXrGeY5kfGmxbjDhd5NigQ>? M4LPNWFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgW|c1OUNibYX0ZY51KGW6cILld5Nm\CCrbjDDU3M4KGOnbHzzJIF{e2W|c3XkJIF{KGy3Y3nm[ZJie2ViYXP0bZZqfHliYX\0[ZIhOjRiaILzJIJ6KHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5zODFOwG0> NYP2UIpFOjJyOUSyO|k>
CHO-K1 cells MoPjSpVv[3Srb36gZZN{[Xl? NIm0WWgzKGh? MonWSIl{eGyjY3Xt[Y51KG:oIGuzTH1ucWKxbHXyc45mKG[{b32gbJVu[W5iQWKg[ZhxemW|c3XkJIlvKEOKTz3LNUBk\WyuczDh[pRmeiB{IHjyd{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyPUCuNkDPxE1? MYOyNFM5OTN4MR?=
human HT-3 cell M2DCfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFe4ZXNKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc{OTN2IN88US=> MYLTRW5ITVJ?
human LNCAP cells NYTUbXBYWHKxbHnm[ZJifGmxbjDhd5NigQ>? NH;LT|U{KGSjeYO= MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{whUUN3ME2wMlc{OjdizszN NELSSIczPjB2NkOxNy=>
human PC3 cells NWDTXVF[TnWwY4Tpc44h[XO|YYm= MYPEbZNxdGGlZX3lcpQhd2ZiW{PIYXIyQDhzIH\yc40h[W6mcn;n[Y4hemWlZYD0c5IhcW5iaIXtZY4hWEN|IHPlcIx{NCCHQ{WwQVQvOyEQvF2= NYLVWGt{OjV3OUGwOlY>
human 22Rv1 cells NUXh[IJmTnWwY4Tpc44h[XO|YYm= M2LCRlMh\GG7cx?= NFfjT4xCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHHu[JJw\2WwIILlZ4VxfG:{IFi4O|R[KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCqdX3hckAzOlK4MTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKESKVD3pcoR2[2WmIHPlcIwh\3Kxd4ToJIFnfGW{IEOg[IF6eyCkeTDXV3QuQCCjc4PhfUwhUUN3ME20MlYh|ryP MUWyOFkxODV6OB?=
human CCF-STTG1 cell MljWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPhPItsUW6qaXLpeIlwdiCxZjDoeY1idiCFQ1[tV3RVTzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3Ojef-8kEBKSzVyPUSuPVI6OjlizszN NHT1e|NUSU6JRWK=
human SCC-25 cell NV\TbpNDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIH0W3hKdmirYnn0bY9vKG:oIHj1cYFvKFOFQz2yOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvODh4NU[g{txO MlH4V2FPT0WU
human MKN45 cell NFmy[YlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUjsVWs2UW6qaXLpeIlwdiCxZjDoeY1idiCPS160OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvQTZyNTFOwG0> NX\nb252W0GQR1XS
human ES5 cell NYXlfVhxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;WTY5pcWKrdHnvckBw\iCqdX3hckBGWzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16Lk[xNVU1KM7:TR?= M37ocXNCVkeHUh?=
human SK-MEL-3 cell MmmwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYSzc49nUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFyLkC5OlQh|ryP M1PZTHNCVkeHUh?=
human PC-3 cell NHnUW3BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX7JV3h1UW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvOjd7MTFOwG0> NX3PPZF1W0GQR1XS
human NOS-1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYfJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUGuNlkyPyEQvF2= NGmyXFFUSU6JRWK=
human LB1047-RCC cell NFL4VZZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX72c5MzUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuNlU{KM7:TR?= NXXYOmxlW0GQR1XS
human CAMA-1 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGNCVUFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlM6OjZizszN MX\TRW5ITVJ?
human SAS cell NUn2PVBMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXvJcohq[mm2aX;uJI9nKGi3bXHuJHNCWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkOwPFEh|ryP MlfXV2FPT0WU
human NCI-H2228 cell NFvrNVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Moe4TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyNlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy55NUOxJO69VQ>? MXrTRW5ITVJ?
human NCI-H187 cell NEHWV4pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUjle5hNUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4Lk[2NVYh|ryP M{TseHNCVkeHUh?=
human BFTC-905 cell NUHKZm5mT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXXlTpZMUW6qaXLpeIlwdiCxZjDoeY1idiCERmTDMVkxPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF5LkS4OVch|ryP MoK0V2FPT0WU
human G-361 cell NESyTIlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoDrTY5pcWKrdHnvckBw\iCqdX3hckBINTN4MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG3MlgzPiEQvF2= M2HzXXNCVkeHUh?=
human DU145 cells MVrDfZRwfG:6aXRCpIF{e2G7 MVK3NkBp M3;3eWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEWUYXzwbIEu\GWoaXPp[Y51KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiRWLi[ZRiKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OThizszN MkHRV2FPT0WU
human SW780 cell NV\SdYJ5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlT3TY5pcWKrdHnvckBw\iCqdX3hckBUXzd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5 MWHTRW5ITVJ?
human BB49-HNC cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWXaXoNEUW6qaXLpeIlwdiCxZjDoeY1idiCEQkS5MWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF6Lkm1N|Ih|ryP MWjTRW5ITVJ?
human KALS-1 cell NHXTV|lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoDtTY5pcWKrdHnvckBw\iCqdX3hckBMSUyVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU43PjN3IN88US=> MlLVV2FPT0WU
human AU565 cell M1zlb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoTTTY5pcWKrdHnvckBw\iCqdX3hckBCXTV4NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5Mlc1ODJizszN MUTTRW5ITVJ?
human NCI-H2087 cell M2DsUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4nGWGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFg4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwMEW5NUDPxE1? NWTN[5djW0GQR1XS
human RVH-421 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJHJXUC12MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU42Pzl3IN88US=> MnXvV2FPT0WU
human SK-CO-1 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHi4ZXFKdmirYnn0bY9vKG:oIHj1cYFvKFONLVPPMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS56OEeyJO69VQ>? MonNV2FPT0WU
human KU-19-19 cell NX:4SIFsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnrkTY5pcWKrdHnvckBw\iCqdX3hckBMXS1zOT2xPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIzNjB{NEKg{txO NEXWcVlUSU6JRWK=
human NB6 cell NFXwNYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1XVZ2lvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkKuPVE{PSEQvF2= MVHTRW5ITVJ?
human RO82-W-1 cell MlHmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXrJcohq[mm2aX;uJI9nKGi3bXHuJHJQQDJvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvOTNzODFOwG0> MUfTRW5ITVJ?
human LNCAP cells NH3pOoxEgXSxdH;4bYPDqGG|c3H5 MmTaNkBl[Xm| NXf4[pZQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhOiCmYYnzJIJ6KGOnbHygZ492dnSrbnegcYV1cG:mLDDJR|UxRTJ|Lke5JO69VQ>? NHO3PIkzOzd{N{C0OC=>
human CTB-1 cell NXL6fXY2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnPlTY5pcWKrdHnvckBw\iCqdX3hckBEXEJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlU2OzZizszN NYH0b5NUW0GQR1XS
human SW48 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIjnfmRKdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE43PTR4IN88US=> M1vS[XNCVkeHUh?=
human TCCSUP cell NXTGdFJyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHRES1OXUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlczOzJizszN NITFS4tUSU6JRWK=
human DK-MG cell M3LZUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M33iXWlvcGmkaYTpc44hd2ZiaIXtZY4hTEtvTVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE45QTF5IN88US=> NF\EbpJUSU6JRWK=
human ST486 cell M3\2Z2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGfTUJFKdmirYnn0bY9vKG:oIHj1cYFvKFOWNEi2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvPzR4NDFOwG0> M3OxW3NCVkeHUh?=
human H4 cell NEXhUGdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUPsV4Q3UW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK2Mlk1PThizszN NVK5OngzW0GQR1XS
human SBC-1 cell NIHRSpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHXvbFVKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvOzVyNzFOwG0> NYjyTohlW0GQR1XS
human CAS-1 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M120c2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE43Ojl2IN88US=> NFvuPGhUSU6JRWK=
human OAW-42 cell M{n0NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnXUTY5pcWKrdHnvckBw\iCqdX3hckBQSVdvNEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE44OTl3IN88US=> MWPTRW5ITVJ?
human HCC1954 cell NYXGXmlvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvYTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzOUW0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzV{NTFOwG0> MVrTRW5ITVJ?
human MDA-MB-453 cell NF75XFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2\KfGlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQ2OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ7LkmwO{DPxE1? MWjTRW5ITVJ?
human MCF7 cell NXu3O3JUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHzCUHRKdmirYnn0bY9vKG:oIHj1cYFvKE2FRkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPU4{ODFizszN NYHnV5JrW0GQR1XS
human PC3 cells MYnGeY5kfGmxbjDhd5NigQ>? MnTCNVAx64DCzszN MmDKOFghcA>? M13JemlvcGmkaYTpc44hd2ZiYXP0bY4h[mG|ZXSgdJNmfWSxcH;kbYEh\m:{bXH0bY9vKGmwIHHu[JJw\2WwLXTldIVv\GWwdDDoeY1idiCSQ{OgZ4VtdHNiYYSgNVAxKHWPIHHmeIVzKDR6IHjyd{BjgSCGQWDJJJN1[WmwaX7nJIJie2WmIH\seY9z\XOlZX7j[UBucWO{b4Pjc5B6KGG|c3H5 NECweFkzOjZ5Mkm4OC=>
human PC3 cells NHT5W4VHfW6ldHnvckBie3OjeR?= MojyNE4yNTFizszN NIX6PZFC\2:waYP0JIFkfGm4aYT5JIF1KGGwZILv[4VvKHKnY3XweI9zKFd5NEHDJI12fGGwdDDlfJBz\XO|ZXSgbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KHO2aX31cIF1cW:wIH;mJJJm[2WydH;yJJRz[W6|YXP0bZZifGmxbjDheEAxNjFidH:gNUB2VSCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> NXryNXlZOjJzN{W2PVQ>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cytosolic AR / Nuclear AR ; 

PubMed: 30833616     


The representative expressions and the quantifications of proteins regarding the bicalutamide-induced apoptosis. (a) downregulation of nuclear androgen receptor (nAR).

30833616
Growth inhibition assay
Cell viability; 

PubMed: 27994514     


MDA-MB-231 and HCC1937 cells were treated with 10 μM bicalutamide and 10μM ABT-888 alone or in combination for 24h, 48h, 72h, and cell viability was determined by MTT assay.

27994514
In vivo Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice. [3]

Protocol

Kinase Assay:[1]
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Whole-cell competitive binding assays:

Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (harbors a mixture of exogenous wild-type AR and endogenous mutant AR (T877A)) and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum, or during the assay with 10% charcoal-stripped, dextran-treated fetal bovine serum (CSS). Cells are pre-incubated with 18F-FDHT, increasing concentrations (1pM to 1μM) of cold Bicalutamide are added, and the assay is performed to measure specific uptake of 18F-FDHT (4). IC50 values are determined using a one site binding model with least squares curve fitting and R2 > 0.99.
Cell Research:[3]
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  • Cell lines: C4-2 cell
  • Concentrations: 0-1 μM
  • Incubation Time: 72 hours
  • Method: Exponentially growing C4-2 cells are plated into two 96-well plates and incubated overnight at 37 ˚C. Twenty-four hours later one plate is aspirated and stored at -80 ˚C and the other treated with 10-fold serial concentrations of ridaforolimus (1000 nM to 0.0001 nM) or vehicle (ethanol). Following 72 hours culture at 37 ˚C, the plates are assessed simultaneously for cell growth using the Cy qUANT Cell Proliferation Assay kit. Bicalutamide and Ridaforolimus combination proliferation assays are performed similarly except cell growth is determined as the change in cell number between vehicle control and compound treated cells after 72 hours in culture.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: Male nude mice bearing C4-2 cells
  • Dosages: 10 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (199.82 mM)
Water Insoluble
Ethanol '5 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 430.37
Formula

C18H14F4N2O4S

CAS No. 90357-06-5
Storage powder
in solvent
Synonyms N/A
Smiles CC(CS(=O)(=O)C1=CC=C(C=C1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

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

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02910050 Unknown status Drug: Bicalutamide|Drug: Aromatase Inhibitor Breast Cancer Xu fei|Sun Yat-sen University January 2016 Phase 2
NCT02614859 Active not recruiting Drug: Bicalutamide|Drug: Metformin and Bicalutamide Cancer of Prostate Fox Chase Cancer Center|National Cancer Institute (NCI) December 1 2015 Phase 2
NCT02146937 Withdrawn Drug: Bicalutamide plus Finasteride- Combination therapy Detectable Prostate Nodules Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins March 2014 Phase 2
NCT01415778 Completed Drug: ICI176334-1|Drug: Casodex 80 mg tablet Healthy AstraZeneca August 2011 Phase 1
NCT01416883 Terminated Drug: ICI176334-1 Healthy AstraZeneca July 2010 Phase 1

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID