Bicalutamide (ICI-176334)

Catalog No.S1190

For research use only.

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

Bicalutamide (ICI-176334) Chemical Structure

CAS No. 90357-06-5

Selleck's Bicalutamide (ICI-176334) has been cited by 39 publications

Purity & Quality Control

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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 NEXjO45HfW6ldHnvckBie3OjeR?= NUjlSZBWTGm|cHzhZ4Vu\W62IH;mJHs{UF2UMUi4NUBnem:vIFHSJIlvKGi3bXHuJG1FSS2PQj20OVMh[2WubIOsJGVEPTB;M{Ggcm0> M{DnSFI{PzF|NU[3
LNCaP cells MY\GeY5kfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKFt|SG2tSGhVKGKrbnTpcochfG9iVEi3O2Eh[W6mcn;n[Y4hemWlZYD0c5Ihd2ZiTF7DZXAh[2WubIOsJGtqRTN3IH7N NUXNRoxiOTV4MEO5OlA>
Freestyle293F cells Mn\FSpVv[3Srb36gZZN{[Xl? M2\oXWlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFHu[JJw\2WwIILlZ4VxfG:{IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGZz\WW|dIns[VI6O0ZiY3XscJMtKEmFNUC9NE4xPTRizszN MkW0NlMyQTl2N{e=
HEK293 cells NGDNUllHfW6ldHnvckBie3OjeR?= NYrLbHhmOyCq MnXtSIl{eGyjY3Xt[Y51KG:oIGuxO{1idHCqYT3t[ZRpgWxvM1jdcYljd2yncn;u[UBnem:vIHHu[JJw\2WwIILlZ4VxfG:{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOyCqcoOsJGlEPTB;NUSgcm0> M{DkPFIzOzlzMEOz
MDA453 cells NWDXXoFiTnWwY4Tpc44h[XO|YYm= M3XremRqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgbY4hVUSDNEWzJINmdGy|LDDLbV03PCCwTR?= Mn[3NVgzQTF4NES=
human MDA-MB-453 cells NUezRm1wTnWwY4Tpc44h[XO|YYm= M3XXOWRqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hSVJiaX6gbJVu[W5iTVTBMW1DNTR3MzDj[YxteyxiSVO1NF03PCCwTR?= MkjNNlA2QDR4MUC=
COS1 cells NVm2[ohHTnWwY4Tpc44h[XO|YYm= NIn3[XdCdnSjZ3;ubZN1KGGldHn2bZR6KGGpYXnud5QheFOJNT30ZYdo\WRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPPV|Eh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIILlZ4VxfG:{LX3l[IlifGWmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCkeTDBVk1z\We3bHH0[YQhemG2IIDyc4Jie2mwIIDyc41wfGW{IH\yZYdu\W62IHTybZZmdiCoaYLl[ox6KGy3Y3nm[ZJie2VicnXwc5J1\XJiYYPzZZktKEmFNUC9NE4xQDZ7IN88US=> MoX3NlU3PDZ4NEm=
HeLa cells MXTGeY5kfGmxbjDhd5NigQ>? NEXNRlZCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKGGwZILv[4VvKHKnY3XweI9zKGW6cILld5Nm\CCrbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[g[IlpgWS{b4Tld5Rwe3Sncn;u[UBqdmS3Y3XkJJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eTDifUBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVAvOTRizszN NETCNXEyPzhyNEKyPS=>
CV1 cells MnTGSpVv[3Srb36gZZN{[Xl? Ml36Rolv\GmwZzDh[oZqdmm2eTD0c{BpfW2jbjDhcoRzd2enbjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hS1ZzIHPlcIx{NCCNaU2wMlE2OSEQvF2= MX:xO|I2Pzh|OB?=
monkey COS7 cells NFfIfnpHfW6ldHnvckBie3OjeR?= NXzGUVlySmmwZHnu[{Bi\m[rbnn0fUB1dyCqdX3hckBidmS{b3flckBz\WOncITvdkBmgHC{ZYPz[YQhcW5ibX;ub4V6KEORU{egZ4VtdHNiYomge4hwdGViY3XscEBjcW6maX7nJIF{e2G7LDDLbV0xNjF3MTFOwG0> MnHHNVg1PDJ7MUK=
COS7 cells MYTGeY5kfGmxbjDhd5NigQ>? MV;B[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IGe3OFFEKG23dHHueEBmgHC{ZYPz[YQhcW5iQ1;TO{Bk\WyuczDhd5Nme3OnZDDhd{BtfWOrZnXyZZNmKGGldHn2bZR6KGGodHXyJFI1KGi{czDifUBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvOThizszN M1SwWFIzODl2Mke5
CHO-K1 cells NXjINYcyTnWwY4Tpc44h[XO|YYm= NYfwNoF4OiCq MVfEbZNxdGGlZX3lcpQhd2ZiW{PIYY1q[m:uZYLvcoUh\nKxbTDoeY1idiCDUjDlfJBz\XO|ZXSgbY4hS0iRLVuxJINmdGy|IHHmeIVzKDJiaILzJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTB;MD6yJO69VQ>? NWDoVXNJOjB|OEGzOlE>
human HT-3 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFrNco9KdmirYnn0bY9vKG:oIHj1cYFvKEiWLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc{OTN2IN88US=> M{G0VXNCVkeHUh?=
human LNCAP cells Ml\pVJJwdGmoZYLheIlwdiCjc4PhfS=> MmTWN{Bl[Xm| M{TIOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiMzDkZZl{NCCLQ{WwQVAvPzN{NzFOwG0> MWWyOlA1PjNzMx?=
human PC3 cells MlzxSpVv[3Srb36gZZN{[Xl? NVSw[nZsTGm|cHzhZ4Vu\W62IH;mJHs{UF2UMUi4NUBnem:vIHHu[JJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIGDDN{Bk\WyuczygSWM2OD12LkOg{txO NIXDNGEzPTV7MUC2Oi=>
human 22Rv1 cells MkTmSpVv[3Srb36gZZN{[Xl? MVizJIRigXN? NGLnWnJCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHHu[JJw\2WwIILlZ4VxfG:{IFi4O|R[KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCqdX3hckAzOlK4MTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKESKVD3pcoR2[2WmIHPlcIwh\3Kxd4ToJIFnfGW{IEOg[IF6eyCkeTDXV3QuQCCjc4PhfUwhUUN3ME20MlYh|ryP NWLDboozOjR7MEC1PFg>
human CCF-STTG1 cell MnnPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFyxZWdKdmirYnn0bY9vKG:oIHj1cYFvKEOFRj3TWHRIOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;ND65NlkzQSEQvF2= MVLTRW5ITVJ?
human SCC-25 cell M17GSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVrEPXk5UW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtNlUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjB6NkW2JO69VQ>? MofLV2FPT0WU
human MKN45 cell M3nPPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJG1MVjR3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj65OlA2KM7:TR?= MVHTRW5ITVJ?
human ES5 cell M3fjUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkLHTY5pcWKrdHnvckBw\iCqdX3hckBGWzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16Lk[xNVU1KM7:TR?= NH;2PHNUSU6JRWK=
human SK-MEL-3 cell NVflfZd[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEjJeFBKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBwMEm2OEDPxE1? NVq3VXFqW0GQR1XS
human PC-3 cell M1v1b2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmHxTY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNlc6OSEQvF2= NXntTmdYW0GQR1XS
human NOS-1 cell Mnf0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH7Fd3pKdmirYnn0bY9vKG:oIHj1cYFvKE6RUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvOjlzNzFOwG0> MXHTRW5ITVJ?
human LB1047-RCC cell MmjSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUXJcohq[mm2aX;uJI9nKGi3bXHuJGxDOTB2Nz3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5{NUOg{txO NGTGNGxUSU6JRWK=
human CAMA-1 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGjRSJpKdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjN7Mk[g{txO M4fiT3NCVkeHUh?=
human SAS cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnL6TY5pcWKrdHnvckBw\iCqdX3hckBUSVNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6zNFgyKM7:TR?= Ml\OV2FPT0WU
human NCI-H2228 cell M{Lwd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlrVTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyNlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy55NUOxJO69VQ>? NGGwR3NUSU6JRWK=
human NCI-H187 cell NWXBWmRiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUi3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvPjZzNjFOwG0> NHLnNnZUSU6JRWK=
human BFTC-905 cell NVPnRm5zT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUfJcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvPDh3NzFOwG0> NWLhbXBZW0GQR1XS
human G-361 cell NF36UZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3jxb2lvcGmkaYTpc44hd2ZiaIXtZY4hTy1|NkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xO{45OjZizszN MmjhV2FPT0WU
human DU145 cells MWPDfZRwfG:6aXRCpIF{e2G7 NH7lUYY4OiCq M3;2PGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEWUYXzwbIEu\GWoaXPp[Y51KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiRWLi[ZRiKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OThizszN NUXwdGhNW0GQR1XS
human SW780 cell NX;od4NxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= M4HHTXNCVkeHUh?=
human BB49-HNC cell MnPmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYT1dXdpUW6qaXLpeIlwdiCxZjDoeY1idiCEQkS5MWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF6Lkm1N|Ih|ryP Mn:2V2FPT0WU
human KALS-1 cell MoD1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHvEb5BKdmirYnn0bY9vKG:oIHj1cYFvKEuDTGOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6NjZ4M{Wg{txO M1\wZnNCVkeHUh?=
human AU565 cell NUX5ZnJpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTvb2ZKdmirYnn0bY9vKG:oIHj1cYFvKEGXNU[1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPzRyMjFOwG0> M2LGRnNCVkeHUh?=
human NCI-H2087 cell NFj5d49Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Moi5TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS5yNUmxJO69VQ>? MkHmV2FPT0WU
human RVH-421 cell NUW1boRsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXL1UXdvUW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwNUe5OUDPxE1? MlPGV2FPT0WU
human SK-CO-1 cell MnnVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWPyT4xqUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3DU{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwOEi3NkDPxE1? MUnTRW5ITVJ?
human KU-19-19 cell MlnkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIPFbI1KdmirYnn0bY9vKG:oIHj1cYFvKEuXLUG5MVE6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjJwMEK0NkDPxE1? M1vFZnNCVkeHUh?=
human NB6 cell NXrmW|ByT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXfXN282UW6qaXLpeIlwdiCxZjDoeY1idiCQQk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNk46OTN3IN88US=> M4O1bXNCVkeHUh?=
human RO82-W-1 cell M{WyUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVjIRpFrUW6qaXLpeIlwdiCxZjDoeY1idiCUT{iyMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ|LkGzNVgh|ryP NU\xN3djW0GQR1XS
human LNCAP cells MkTKR5l1d3SxeHnjxsBie3OjeR?= MUSyJIRigXN? NVnLSII4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhOiCmYYnzJIJ6KGOnbHygZ492dnSrbnegcYV1cG:mLDDJR|UxRTJ|Lke5JO69VQ>? MkPDNlM4OjdyNES=
human CTB-1 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuOVU{PiEQvF2= NFqwSZpUSU6JRWK=
human SW48 cell MkTNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3rHZWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d2ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlY2PDZizszN MVLTRW5ITVJ?
human TCCSUP cell M{LReWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3G4VmlvcGmkaYTpc44hd2ZiaIXtZY4hXEOFU2XQJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPzJ|MjFOwG0> MV3TRW5ITVJ?
human DK-MG cell NUnOUo03T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGHjXplKdmirYnn0bY9vKG:oIHj1cYFvKESNLV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvQDlzNzFOwG0> NXvaZmpYW0GQR1XS
human ST486 cell Ml\lS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1PrPWlvcGmkaYTpc44hd2ZiaIXtZY4hW1R2OE[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOU44PDZ2IN88US=> MVXTRW5ITVJ?
human H4 cell M3L2Wmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFT4XXNKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mk[uPVQ2QCEQvF2= MnXlV2FPT0WU
human SBC-1 cell MorRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWHJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkiuN|UxPyEQvF2= MX3TRW5ITVJ?
human CAS-1 cell NYrKO5pIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmPoTY5pcWKrdHnvckBw\iCqdX3hckBESVNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlYzQTRizszN NFPDOXVUSU6JRWK=
human OAW-42 cell NFLyTW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1zhWWlvcGmkaYTpc44hd2ZiaIXtZY4hV0GZLUSyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzF7NTFOwG0> MkDFV2FPT0WU
human HCC1954 cell NHX4WmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4fVcWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUm1OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5Njd3MkWg{txO M1;ESnNCVkeHUh?=
human MDA-MB-453 cell NF31XZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXHJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20OVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQS57MEeg{txO MlzrV2FPT0WU
human MCF7 cell MnLWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILhcWhKdmirYnn0bY9vKG:oIHj1cYFvKE2FRkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPU4{ODFizszN MmXXV2FPT0WU
human PC3 cells NWjKbFdoTnWwY4Tpc44h[XO|YYm= MWOxNFDkiIEQvF2= NXPBW2Y6PDhiaB?= MljxTY5pcWKrdHnvckBw\iCjY4TpckBj[XOnZDDwd4V2\G:yb3TpZUBnd3KvYYTpc44hcW5iYX7kdo9o\W5vZHXw[Y5l\W62IHj1cYFvKFCFMzDj[YxteyCjdDCxNFAhfU1iYX\0[ZIhPDhiaILzJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJI1q[3Kxc3PvdJkh[XO|YYm= M3\DTVIzPjd{OUi0
human PC3 cells Ml\LSpVv[3Srb36gZZN{[Xl? M3zPVlAvOS1zIN88US=> NFjY[G5C\2:waYP0JIFkfGm4aYT5JIF1KGGwZILv[4VvKHKnY3XweI9zKFd5NEHDJI12fGGwdDDlfJBz\XO|ZXSgbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KHO2aX31cIF1cW:wIH;mJJJm[2WydH;yJJRz[W6|YXP0bZZifGmxbjDheEAxNjFidH:gNUB2VSCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> NGe5VmIzOjF5NU[5OC=>
Assay
Methods Test Index PMID
Western blot Cytosolic AR / Nuclear AR 30833616
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • 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 3 years -20°C powder
2 years -80°C in solvent
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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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
NCT04573231 Recruiting Drug: 18F-DCFPyL Breast Cancer|HER2-negative Breast Cancer|Metastatic Breast Cancer University of Wisconsin Madison May 24 2021 Phase 2
NCT04443062 Recruiting Drug: 177Lu-PSMA-617 Prostate Cancer Radboud University|Prostaatkankerstichting|Advanced Accelerator Applications July 20 2020 Phase 2
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

(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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