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 13 Publications

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  • 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.

  • 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.

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

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 NXXUXWhYTnWwY4Tpc44h[XO|YYm= MV3EbZNxdGGlZX3lcpQhd2ZiW{PIYXIyQDhzIH\yc40hSVJiaX6gbJVu[W5iTVTBMW1DNTR3MzDj[YxteyxiRVO1NF0{OSCwTR?= MYCyN|cyOzV4Nx?=
LNCaP cells M4\DWWZ2dmO2aX;uJIF{e2G7 M1;wVWlvcGmkaYTpc44hd2ZiW{PIYU1FUFRiYnnu[Ilv\yC2bzDUPFc4SSCjbnTyc4dmdiC{ZXPldJRweiCxZjDMUmNiWCClZXzsd{whU2l;M{Wgcm0> MorrNVU3ODN7NkC=
Freestyle293F cells MUTGeY5kfGmxbjDhd5NigQ>? NX;FTZR5UW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgRY5lem:pZX6gdoVk\XC2b4KgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hTnKnZYP0fYxmOjl|RjDj[YxteyxiSVO1NF0xNjB3NDFOwG0> Mn7TNlMyQTl2N{e=
HEK293 cells M2O5S2Z2dmO2aX;uJIF{e2G7 M2joV|MhcA>? NV;nZ4gyTGm|cHzhZ4Vu\W62IH;mJHsyPy2jbIDoZU1u\XSqeXytN2hedWmkb3zldo9v\SCocn;tJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZYZ1\XJiMzDodpMtKEmFNUC9OVQhdk1? M{\2c|IzOzlzMEOz
MDA453 cells MnLlSpVv[3Srb36gZZN{[Xl? MV3EbZNxdGGlZX3lcpQhd2ZiW{PIYWRJXCCocn;tJIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IHnuJG1FSTR3MzDj[YxteyxiS3m9OlQhdk1? MYmxPFI6OTZ2NB?=
human MDA-MB-453 cells NUjZbm53TnWwY4Tpc44h[XO|YYm= M4L3fWRqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hSVJiaX6gbJVu[W5iTVTBMW1DNTR3MzDj[YxteyxiSVO1NF03PCCwTR?= MlThNlA2QDR4MUC=
COS1 cells MoDjSpVv[3Srb36gZZN{[Xl? NITVVHlCdnSjZ3;ubZN1KGGldHn2bZR6KGGpYXnud5QheFOJNT30ZYdo\WRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPPV|Eh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIILlZ4VxfG:{LX3l[IlifGWmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCkeTDBVk1z\We3bHH0[YQhemG2IIDyc4Jie2mwIIDyc41wfGW{IH\yZYdu\W62IHTybZZmdiCoaYLl[ox6KGy3Y3nm[ZJie2VicnXwc5J1\XJiYYPzZZktKEmFNUC9NE4xQDZ7IN88US=> NXjUWoRmOjV4NE[2OFk>
HeLa cells NUO5UnExTnWwY4Tpc44h[XO|YYm= NVXMSVhMSW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCjbnTyc4dmdiC{ZXPldJRweiCneIDy[ZN{\WRiaX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIRqcHmmcn;0[ZN1d3O2ZYLvcoUhcW6mdXPl[EB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgZpkhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF0xNjF2IN88US=> NX\iZnA4OTd6MESyNlk>
CV1 cells NGLZbG1HfW6ldHnvckBie3OjeR?= MXLCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEXjFiY3XscJMtKEurPUCuNVUyKM7:TR?= MWWxO|I2Pzh|OB?=
monkey COS7 cells NH\OXo5HfW6ldHnvckBie3OjeR?= NV7MdGFqSmmwZHnu[{Bi\m[rbnn0fUB1dyCqdX3hckBidmS{b3flckBz\WOncITvdkBmgHC{ZYPz[YQhcW5ibX;ub4V6KEORU{egZ4VtdHNiYomge4hwdGViY3XscEBjcW6maX7nJIF{e2G7LDDLbV0xNjF3MTFOwG0> MV[xPFQ1OjlzMh?=
COS7 cells NGG4dFBHfW6ldHnvckBie3OjeR?= MWfB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IGe3OFFEKG23dHHueEBmgHC{ZYPz[YQhcW5iQ1;TO{Bk\WyuczDhd5Nme3OnZDDhd{BtfWOrZnXyZZNmKGGldHn2bZR6KGGodHXyJFI1KGi{czDifUBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvOThizszN MUeyNlA6PDJ5OR?=
CHO-K1 cells NXjldVkyTnWwY4Tpc44h[XO|YYm= MXyyJIg> NX:3Z4dDTGm|cHzhZ4Vu\W62IH;mJHs{UF2vaXLvcIVzd26nIH\yc40hcHWvYX6gRXIh\XiycnXzd4VlKGmwIFPIU{1MOSClZXzsd{Bi\nSncjCyJIhzeyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwQVAvOiEQvF2= NHH2VoEzODN6MUO2NS=>
human HT-3 cell NUjJeYNRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWDJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkezNVM1KM7:TR?= MX\TRW5ITVJ?
human LNCAP cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 MYSzJIRigXN? NEPNNoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyxiSVO1NF0xNjd|Mkeg{txO NILNWoYzPjB2NkOxNy=>
human PC3 cells M4G5[WZ2dmO2aX;uJIF{e2G7 NXHSS3gxTGm|cHzhZ4Vu\W62IH;mJHs{UF2UMUi4NUBnem:vIHHu[JJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIGDDN{Bk\WyuczygSWM2OD12LkOg{txO NIrWNJAzPTV7MUC2Oi=>
human 22Rv1 cells MnWxSpVv[3Srb36gZZN{[Xl? M1u1NVMh\GG7cx?= NG[zOVZCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHHu[JJw\2WwIILlZ4VxfG:{IFi4O|R[KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCqdX3hckAzOlK4MTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKESKVD3pcoR2[2WmIHPlcIwh\3Kxd4ToJIFnfGW{IEOg[IF6eyCkeTDXV3QuQCCjc4PhfUwhUUN3ME20MlYh|ryP MWmyOFkxODV6OB?=
human CCF-STTG1 cell NHjaWnZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXfJcohq[mm2aX;uJI9nKGi3bXHuJGNETi2VVGTHNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:PC57MkmyPUDPxE1? NUDURoV1W0GQR1XS
human SCC-25 cell Mlz2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXHXWZpDUW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtNlUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjB6NkW2JO69VQ>? M3rscnNCVkeHUh?=
human MKN45 cell Ml21S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4T2dWlvcGmkaYTpc44hd2ZiaIXtZY4hVUuQNEWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Mlk3ODVizszN MlK1V2FPT0WU
human ES5 cell NUW4UJVOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHPoS3JKdmirYnn0bY9vKG:oIHj1cYFvKEWVNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOlEyPTRizszN MXXTRW5ITVJ?
human SK-MEL-3 cell NH;SXVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFO5e5JKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBwMEm2OEDPxE1? M3n0VHNCVkeHUh?=
human PC-3 cell NHzjOG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MofqTY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNlc6OSEQvF2= NIr0XHdUSU6JRWK=
human NOS-1 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYD0XYhYUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjJ7MUeg{txO NWnidGM4W0GQR1XS
human LB1047-RCC cell NV3FdWp3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mk\yTY5pcWKrdHnvckBw\iCqdX3hckBNSjFyNEetVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwMkWzJO69VQ>? MkD1V2FPT0WU
human CAMA-1 cell NWPCdJV5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1XwPWlvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvOzl{NjFOwG0> MVvTRW5ITVJ?
human SAS cell Mo\VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKGi3bXHuJHNCWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkOwPFEh|ryP MlvVV2FPT0WU
human NCI-H2228 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TRWWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNlI5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwN{WzNUDPxE1? NUX3U4o3W0GQR1XS
human NCI-H187 cell NYPKSYxbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXHSN3dmUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4Lk[2NVYh|ryP MoPpV2FPT0WU
human BFTC-905 cell NGn2OIJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLqOIZKdmirYnn0bY9vKG:oIHj1cYFvKEKIVFOtPVA2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTdwNEi1O{DPxE1? M3HBbHNCVkeHUh?=
human G-361 cell M{HRV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NE\H[XNKdmirYnn0bY9vKG:oIHj1cYFvKEdvM{[xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvQDJ4IN88US=> MYjTRW5ITVJ?
human DU145 cells NYP4ZlRuS3m2b4TvfIlkyqCjc4PhfS=> MXW3NkBp M37kVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEWUYXzwbIEu\GWoaXPp[Y51KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiRWLi[ZRiKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OThizszN NIHsfWNUSU6JRWK=
human SW780 cell MlzLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XrWmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfS=> MmTlV2FPT0WU
human BB49-HNC cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWXJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVgvQTV|MjFOwG0> NX3DZ|hHW0GQR1XS
human KALS-1 cell MnvkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlzNTY5pcWKrdHnvckBw\iCqdX3hckBMSUyVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU43PjN3IN88US=> NFH1ZopUSU6JRWK=
human AU565 cell NVrDUY9YT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFfKSXRKdmirYnn0bY9vKG:oIHj1cYFvKEGXNU[1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPzRyMjFOwG0> NXLWdVQyW0GQR1XS
human NCI-H2087 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3;JcWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFg4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwMEW5NUDPxE1? NXHFNGxJW0GQR1XS
human RVH-421 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGDEU29KdmirYnn0bY9vKG:oIHj1cYFvKFKYSD20NlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS53N{m1JO69VQ>? NWTsdJlzW0GQR1XS
human SK-CO-1 cell MmDiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHHiVlZKdmirYnn0bY9vKG:oIHj1cYFvKFONLVPPMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS56OEeyJO69VQ>? MW\TRW5ITVJ?
human KU-19-19 cell M3vPSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MULJcohq[mm2aX;uJI9nKGi3bXHuJGtWNTF7LUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvODJ2MjFOwG0> MVXTRW5ITVJ?
human NB6 cell NXezb3JkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1rCeWlvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkKuPVE{PSEQvF2= M3\Q[3NCVkeHUh?=
human RO82-W-1 cell MlPTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWrJcohq[mm2aX;uJI9nKGi3bXHuJHJQQDJvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvOTNzODFOwG0> MknJV2FPT0WU
human LNCAP cells MWTDfZRwfG:6aXRCpIF{e2G7 NYDrPFBpOiCmYYnz MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjCyJIRigXNiYomgZ4VtdCClb4XueIlv\yCvZYToc4QtKEmFNUC9NlMvPzlizszN Mlq1NlM4OjdyNES=
human CTB-1 cell NFS0O49Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlPKTY5pcWKrdHnvckBw\iCqdX3hckBEXEJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlU2OzZizszN M4TucnNCVkeHUh?=
human SW48 cell M1XjNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\xW2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d2ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlY2PDZizszN MUnTRW5ITVJ?
human TCCSUP cell NYO1W|J5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;kTY5pcWKrdHnvckBw\iCqdX3hckBVS0OVVWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE44OjN{IN88US=> NHjGO5VUSU6JRWK=
human DK-MG cell NGCw[mtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXzoUWczUW6qaXLpeIlwdiCxZjDoeY1idiCGSz3NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1Njh7MUeg{txO NFW5XWdUSU6JRWK=
human ST486 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHNVPDh4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkWuO|Q3PCEQvF2= MUXTRW5ITVJ?
human H4 cell NVHSNGl2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3r2d2lvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Nj65OFU5KM7:TR?= MmLDV2FPT0WU
human SBC-1 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3\JNGlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE4{PTB5IN88US=> Ml36V2FPT0WU
human CAS-1 cell M{XnOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX3QW2NFUW6qaXLpeIlwdiCxZjDoeY1idiCFQWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5NjZ{OUSg{txO NF3XNHlUSU6JRWK=
human OAW-42 cell Mn\SS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3\DZmlvcGmkaYTpc44hd2ZiaIXtZY4hV0GZLUSyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzF7NTFOwG0> MnrkV2FPT0WU
human HCC1954 cell M{foT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\OZ3NyUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxPVU1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjhwN{WyOUDPxE1? NWDJbI1OW0GQR1XS
human MDA-MB-453 cell NX\o[pdQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEfvO3pKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk01PTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{OT65NFch|ryP MYXTRW5ITVJ?
human MCF7 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4PMRmlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO5MlMxOSEQvF2= M1mwdnNCVkeHUh?=
human PC3 cells M2PSW2Z2dmO2aX;uJIF{e2G7 NET3XlYyODElgJFOwG0> NU\uSlZPPDhiaB?= NGfDUHpKdmirYnn0bY9vKG:oIHHjeIlvKGKjc3XkJJB{\XWmb4Dv[IliKG[xcn3heIlwdiCrbjDhcoRzd2enbj3k[ZBmdmSnboSgbJVu[W5iUFOzJINmdGy|IHH0JFExOCC3TTDh[pRmeiB2ODDodpMh[nliRFHQTUB{fGGrbnnu[{Bj[XOnZDDmcJVwemW|Y3XuZ4UhdWmlcn;zZ49xgSCjc4PhfS=> MoH2NlI3PzJ7OES=
human PC3 cells M1;uXWZ2dmO2aX;uJIF{e2G7 MXqwMlEuOSEQvF2= MmPuRYdwdmm|dDDhZ5Rqfmm2eTDheEBidmS{b3flckBz\WOncITvdkBYPzRzQzDteZRidnRiZYjwdoV{e2WmIHnuJIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{B{fGmvdXzheIlwdiCxZjDy[YNmeHSxcjD0doFve2GldHn2ZZRqd25iYYSgNE4yKHSxIEGgeW0h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 M2jLW|IzOTd3Nkm0

... 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]
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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]
+ 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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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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 )

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* 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02910050 Recruiting Drug: Bicalutamide|Drug: Aromatase Inhibitor Breast Cancer Xu fei|Sun Yat-sen University January 2016 Phase 2
NCT02614859 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
NCT01415791 Completed Drug: ICI176334-1 Healthy AstraZeneca August 2011 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID