Bicalutamide

Catalog No.S1190 Synonyms: ICI-176334

Bicalutamide Chemical Structure

Molecular Weight(MW): 430.37

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

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Cited by 10 Publications

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  • Cancer Res, 2018, doi:10.1158/0008-5472.CAN-17-3728. Bicalutamide purchased from Selleck.

    Immunohistochemical staining of Ki67 was performed to determine cell proliferation in the tumors. Each tissue section was counted manually in three different areas to assess the Ki67-positive cell index. Data were then presented as number of Ki67-positive cells per x 400 microscope field. Results are presented as the means s.d. **P < 0.001 by Student 's t-test, compared with control.

    Oncogene 2014 10.1038/onc.2014.302. Bicalutamide purchased from Selleck.

  • When Tramp-C1 and PTENCaP8 cells were cocultured with macrophages and treated with BMP-6 and dihydrotestosterone simultaneously for 48 h, AR antagonists bicalutamide (Bical) and MDV3100 blocked the androgen hypersensitivity.

    Cancer Sci 2013 104(8), 1027-32. Bicalutamide purchased from Selleck.

    (D) Cell apoptosis measured by flow cytometry analysis after cells were exposed to 10μM bicalutamide and 10μM ABT-888 alone or in combination for 48h in MDA-MB-231 and HCC1937. Data are the mean of three independent experiments. *P<0.05, **P<0.01, #P>0.05.

    Int J Biol Sci, 2016, 12(12):1500-1510. Bicalutamide purchased from Selleck.

  • CX4945 resensitizes CRPC cells to anti-androgen therapy. a, b 22Rv1 and VCaP cells were treated with indicated concentration of bicalutamide (Bic) without CX4945. c, d 22Rv1 and VCaP cells were treated with indicated concentration of bicalutamide (Bic) with a subdose of CX4945 (3 or 5 μM). CCK8 assay was performed at 72 h to measure the cell viability. **P < 0.01, ***P < 0.001

    World J Urol, 2017, 35(8):1213-1221. Bicalutamide purchased from Selleck.

Purity & Quality Control

Choose Selective Androgen Receptor Inhibitors

Biological Activity

Description Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.
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 NYK1TGw1TnWwY4Tpc44h[XO|YYm= NELqZnBFcXOybHHj[Y1mdnRib3[gX|NJZVJzOEixJIZzd21iQWKgbY4hcHWvYX6gUWRCNU2ELUS1N{Bk\WyuczygSWM2OD1|MTDuUS=> M2P3flI{PzF|NU[3
LNCaP cells NGe2To5HfW6ldHnvckBie3OjeR?= MmD0TY5pcWKrdHnvckBw\iCdM1jdMWRJXCCkaX7kbY5oKHSxIGS4O|dCKGGwZILv[4VvKHKnY3XweI9zKG:oIFzOR4FRKGOnbHzzMEBMcT1|NTDuUS=> MXmxOVYxOzl4MB?=
Freestyle293F cells NXzB[FJFTnWwY4Tpc44h[XO|YYm= NH3uNmJKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDBcoRzd2enbjDy[YNmeHSxcjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBHemWnc4T5cIUzQTOIIHPlcIx{NCCLQ{WwQVAvODV2IN88US=> MXmyN|E6QTR5Nx?=
HEK293 cells NVHXNpdoTnWwY4Tpc44h[XO|YYm= MmPwN{Bp NVn6ZnVETGm|cHzhZ4Vu\W62IH;mJHsyPy2jbIDoZU1u\XSqeXytN2hedWmkb3zldo9v\SCocn;tJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZYZ1\XJiMzDodpMtKEmFNUC9OVQhdk1? MX:yNlM6OTB|Mx?=
MDA453 cells Mm\RSpVv[3Srb36gZZN{[Xl? MXjEbZNxdGGlZX3lcpQhd2ZiW{PIYWRJXCCocn;tJIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IHnuJG1FSTR3MzDj[YxteyxiS3m9OlQhdk1? MX:xPFI6OTZ2NB?=
human MDA-MB-453 cells M1u3c2Z2dmO2aX;uJIF{e2G7 MUXEbZNxdGGlZX3lcpQhd2ZiW{PIYWRJXCCocn;tJGFTKGmwIHj1cYFvKE2GQT3NRk01PTNiY3XscJMtKEmFNUC9OlQhdk1? NIC0XYQzODV6NE[xNC=>
COS1 cells NVezV4drTnWwY4Tpc44h[XO|YYm= NYC2e4ZrSW62YXfvcol{fCCjY4Tpeol1gSCjZ3HpcpN1KHCVR{WteIFo\2WmIHj1cYFvKGGwZILv[4VvKHKnY3XweI9zKGW6cILld5Nm\CCrbjDDU3MyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDy[YNmeHSxcj3t[YRq[XSnZDD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliYomgRXIuemWpdXzheIVlKHKjdDDwdo9j[XOrbjDwdo9ud3SncjDmdoFodWWwdDDkdol3\W5iZnny[YZtgSCudXPp[oVz[XOnIILldI9zfGW{IHHzd4F6NCCLQ{WwQVAvODh4OTFOwG0> NGjDc|AzPTZ2Nk[0PS=>
HeLa cells M12yW2Z2dmO2aX;uJIF{e2G7 M1Ll[WFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDkbYh6\HKxdHXzeI9{fGW{b37lJIlv\HWlZXSgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHL5JJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NE4yPCEQvF2= NF7CNVMyPzhyNEKyPS=>
CV1 cells NFfiV3FHfW6ldHnvckBie3OjeR?= NELpTGVDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCFVkGgZ4VtdHNuIFvpQVAvOTVzIN88US=> MmLuNVczPTd6M{i=
monkey COS7 cells M{ni[mZ2dmO2aX;uJIF{e2G7 NFzCOGtDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCvb37r[ZkhS0:VNzDj[YxteyCkeTD3bI9t\SClZXzsJIJqdmSrbnegZZN{[XluIFvpQVAvOTVzIN88US=> MX:xPFQ1OjlzMh?=
COS7 cells MnjJSpVv[3Srb36gZZN{[Xl? NGPZWG9C\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJHc4PDGFIH31eIFvfCCneIDy[ZN{\WRiaX6gR29UPyClZXzsd{Bie3Onc4Pl[EBieyCudXPp[oVz[XOnIHHjeIl3cXS7IHHmeIVzKDJ2IHjyd{BjgSC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMUig{txO MWSyNlA6PDJ5OR?=
CHO-K1 cells MXPGeY5kfGmxbjDhd5NigQ>? NXvoXFJ{OiCq MXrEbZNxdGGlZX3lcpQhd2ZiW{PIYY1q[m:uZYLvcoUh\nKxbTDoeY1idiCDUjDlfJBz\XO|ZXSgbY4hS0iRLVuxJINmdGy|IHHmeIVzKDJiaILzJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTB;MD6yJO69VQ>? M3v4UFIxOzhzM{[x
human HT-3 cell M322Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHHTY5pcWKrdHnvckBw\iCqdX3hckBJXC1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63N|E{PCEQvF2= NXHqOVNyW0GQR1XS
human LNCAP cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 NWPv[GNvOyCmYYnz NX7RTVRLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNuIFnDOVA:OC55M{K3JO69VQ>? NXHjOXByOjZyNE[zNVM>
human PC3 cells MY\GeY5kfGmxbjDhd5NigQ>? NF3j[HVFcXOybHHj[Y1mdnRib3[gX|NJZVJzOEixJIZzd21iYX7kdo9o\W5icnXj[ZB1d3JiaX6gbJVu[W5iUFOzJINmdGy|LDDFR|UxRTRwMzFOwG0> Ml:4NlU2QTFyNk[=
human 22Rv1 cells NHXldIRHfW6ldHnvckBie3OjeR?= MlXIN{Bl[Xm| NYLwcmo5SW62YXfvcol{fCCjY4Tpeol1gSCjdDDhcoRzd2enbjDy[YNmeHSxcjDIPFc1YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hOjKUdkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCGSGStbY5lfWOnZDDj[YxtKGe{b4f0bEBi\nSncjCzJIRigXNiYomgW3NVNThiYYPzZZktKEmFNUC9OE43KM7:TR?= NVvS[|RqOjR7MEC1PFg>
human CCF-STTG1 cell M3zhNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2DMRWlvcGmkaYTpc44hd2ZiaIXtZY4hS0OILWPUWGcyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD12LkmyPVI6KM7:TR?= M3nmOXNCVkeHUh?=
human SCC-25 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{DtW2lvcGmkaYTpc44hd2ZiaIXtZY4hW0OFLUK1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4xQDZ3NjFOwG0> NHX0SG1USU6JRWK=
human MKN45 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVrJcohq[mm2aX;uJI9nKGi3bXHuJG1MVjR3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj65OlA2KM7:TR?= Mon4V2FPT0WU
human ES5 cell MnvmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWWzb21ZUW6qaXLpeIlwdiCxZjDoeY1idiCHU{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlYyOTV2IN88US=> MV;TRW5ITVJ?
human SK-MEL-3 cell MkLjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvODl4NDFOwG0> MYTTRW5ITVJ?
human PC-3 cell MkL3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUi2fnNJUW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvOjd7MTFOwG0> NF7nSIVUSU6JRWK=
human NOS-1 cell MkD2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\aTY5pcWKrdHnvckBw\iCqdX3hckBPV1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlI6OTdizszN NVHwd2ZOW0GQR1XS
human LB1047-RCC cell NUDMbmNpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV6we|JkUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuNlU{KM7:TR?= MoDBV2FPT0WU
human CAMA-1 cell NGO3[pdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1jOdmlvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvOzl{NjFOwG0> MV7TRW5ITVJ?
human SAS cell NXnteFhXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{SwSGlvcGmkaYTpc44hd2ZiaIXtZY4hW0GVIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuN|A5OSEQvF2= NID4TIlUSU6JRWK=
human NCI-H2228 cell MlzVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYPsW|hmUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzOjhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz63OVMyKM7:TR?= NF6yOWtUSU6JRWK=
human NCI-H187 cell Mmn6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXvhWmsyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4Lk[2NVYh|ryP Ml:zV2FPT0WU
human BFTC-905 cell NWHWSJpMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGPl[VFKdmirYnn0bY9vKG:oIHj1cYFvKEKIVFOtPVA2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTdwNEi1O{DPxE1? MVnTRW5ITVJ?
human G-361 cell NYPO[VU{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlf4TY5pcWKrdHnvckBw\iCqdX3hckBINTN4MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG3MlgzPiEQvF2= MkXGV2FPT0WU
human DU145 cells MmXJR5l1d3SxeHnjxsBie3OjeR?= M{\OV|czKGh? MmX2R5l1d3SxeHnjbZR6KGGpYXnud5QhTVKjbIDoZU1l\W[rY3nlcpQhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCHUnLleIEh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yQCEQvF2= NGfPRlJUSU6JRWK=
human SW780 cell M4LLXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= MUjTRW5ITVJ?
human BB49-HNC cell MoXDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3ztNWlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ2OT3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQC57NUOyJO69VQ>? MXHTRW5ITVJ?
human KALS-1 cell NUDidncxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{TnWmlvcGmkaYTpc44hd2ZiaIXtZY4hU0GOUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPjZ|NTFOwG0> MUDTRW5ITVJ?
human AU565 cell MnXvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEXFXWlKdmirYnn0bY9vKG:oIHj1cYFvKEGXNU[1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPzRyMjFOwG0> MlPsV2FPT0WU
human NCI-H2087 cell NWrtPW1UT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rqcmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFg4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwMEW5NUDPxE1? M{\OdnNCVkeHUh?=
human RVH-421 cell NEW3WlBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mo\mTY5pcWKrdHnvckBw\iCqdX3hckBTXkhvNEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTd7NTFOwG0> M2[yXnNCVkeHUh?=
human SK-CO-1 cell NGPofI1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNUORLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU45QDd{IN88US=> MXTTRW5ITVJ?
human KU-19-19 cell M4frSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYLoeVJQUW6qaXLpeIlwdiCxZjDoeY1idiCNVT2xPU0yQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ{LkCyOFIh|ryP M{nNcnNCVkeHUh?=
human NB6 cell MlXmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEOwcXhKdmirYnn0bY9vKG:oIHj1cYFvKE6ENjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlkyOzVizszN MU\TRW5ITVJ?
human RO82-W-1 cell NVvxNFBrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmW0TY5pcWKrdHnvckBw\iCqdX3hckBTVzh{LWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjF|MUig{txO MV7TRW5ITVJ?
human LNCAP cells MYPDfZRwfG:6aXRCpIF{e2G7 M{S2WVIh\GG7cx?= M17xUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxPS0GSIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFIh\GG7czDifUBk\WyuIHPveY51cW6pIH3leIhw\CxiSVO1NF0zOy55OTFOwG0> NETrb|IzOzd{N{C0OC=>
human CTB-1 cell M4nKUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuOVU{PiEQvF2= MXvTRW5ITVJ?
human SW48 cell M13BOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWLwU2t6UW6qaXLpeIlwdiCxZjDoeY1idiCVV{S4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPjV2NjFOwG0> MV3TRW5ITVJ?
human TCCSUP cell M{\sO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXHJbItxUW6qaXLpeIlwdiCxZjDoeY1idiCWQ1PTWXAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPC55MkOyJO69VQ>? MnviV2FPT0WU
human DK-MG cell NGjTPIJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKGi3bXHuJGRMNU2JIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuPFkyPyEQvF2= NHjtNFlUSU6JRWK=
human ST486 cell MkTrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn3DTY5pcWKrdHnvckBw\iCqdX3hckBUXDR6NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK1Mlc1PjRizszN MU\TRW5ITVJ?
human H4 cell NIC2U5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2PkWGlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Nj65OFU5KM7:TR?= NVHER45mW0GQR1XS
human SBC-1 cell NGXoVHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGPyd5ZKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvOzVyNzFOwG0> NInRfIJUSU6JRWK=
human CAS-1 cell NG\rTVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGNCWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkiuOlI6PCEQvF2= Ml;LV2FPT0WU
human OAW-42 cell M1rlfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXyxWXZXUW6qaXLpeIlwdiCxZjDoeY1idiCRQWetOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQC55MUm1JO69VQ>? Mn;yV2FPT0WU
human HCC1954 cell NYHVNodET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M17OZWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUm1OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5Njd3MkWg{txO MUjTRW5ITVJ?
human MDA-MB-453 cell Mmn0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIfVZplKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk01PTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{OT65NFch|ryP NHGyfpFUSU6JRWK=
human MCF7 cell NGPGV49Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2jw[mlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO5MlMxOSEQvF2= M2Dq[HNCVkeHUh?=
human PC3 cells M1X0TWZ2dmO2aX;uJIF{e2G7 NEPhcpEyODElgJFOwG0> MmrSOFghcA>? NETKXGlKdmirYnn0bY9vKG:oIHHjeIlvKGKjc3XkJJB{\XWmb4Dv[IliKG[xcn3heIlwdiCrbjDhcoRzd2enbj3k[ZBmdmSnboSgbJVu[W5iUFOzJINmdGy|IHH0JFExOCC3TTDh[pRmeiB2ODDodpMh[nliRFHQTUB{fGGrbnnu[{Bj[XOnZDDmcJVwemW|Y3XuZ4UhdWmlcn;zZ49xgSCjc4PhfS=> M4\PUlIzPjd{OUi0
human PC3 cells M4\oR2Z2dmO2aX;uJIF{e2G7 MoPRNE4yNTFizszN M3z1R2Fod26rc4SgZYN1cX[rdImgZZQh[W6mcn;n[Y4hemWlZYD0c5IhXzd2MVOgcZV1[W62IHX4dJJme3OnZDDpckBpfW2jbjDQR|Mh[2WubIOgZZN{\XO|ZXSgZZMhe3SrbYXsZZRqd25ib3[gdoVk\XC2b4KgeJJidnOjY4TpeoF1cW:wIHH0JFAvOSC2bzCxJJVOKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> MVSyNlE4PTZ7NB?=

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • Animal Models: Male nude mice bearing C4-2 cells
  • Formulation: 4% ethanol, 5% Tween 80, and 5% propylene glycol
  • Dosages: 10 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (199.82 mM)
Ethanol 5 mg/mL (11.61 mM)
Water Insoluble

* 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 ICI-176334

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
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*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
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    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):
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    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 Conditions Sponsor/Collaborators Start Date Phases
NCT03650894 Not yet recruiting Breast Neoplasm Female|Breast Cancer|Breast Carcinoma|Breast Tumor Providence Health & Services|Bristol-Myers Squibb|Memorial Sloan Kettering Cancer Center October 2019 Phase 2
NCT03650894 Not yet recruiting Breast Neoplasm Female|Breast Cancer|Breast Carcinoma|Breast Tumor Providence Health & Services|Bristol-Myers Squibb|Memorial Sloan Kettering Cancer Center October 2019 Phase 2
NCT03809000 Not yet recruiting Prostate Cancer RTOG Foundation Inc.|Pfizer|Astellas Pharma Inc February 15 2019 Phase 2
NCT03809000 Not yet recruiting Prostate Cancer RTOG Foundation Inc.|Pfizer|Astellas Pharma Inc February 15 2019 Phase 2
NCT03678025 Recruiting Castration Levels of Testosterone|Metastatic Prostatic Adenocarcinoma|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8 Southwest Oncology Group|National Cancer Institute (NCI) September 17 2018 Phase 3
NCT03678025 Recruiting Castration Levels of Testosterone|Metastatic Prostatic Adenocarcinoma|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8 Southwest Oncology Group|National Cancer Institute (NCI) September 17 2018 Phase 3

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