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 16 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 NGHNZYNHfW6ldHnvckBie3OjeR?= NULvenV6TGm|cHzhZ4Vu\W62IH;mJHs{UF2UMUi4NUBnem:vIFHSJIlvKGi3bXHuJG1FSS2PQj20OVMh[2WubIOsJGVEPTB;M{Ggcm0> NGjl[2MzOzdzM{W2Oy=>
LNCaP cells NFWyVFRHfW6ldHnvckBie3OjeR?= NWr0[ZJYUW6qaXLpeIlwdiCxZjDbN2heNUSKVDDibY5lcW6pIITvJHQ5PzeDIHHu[JJw\2WwIILlZ4VxfG:{IH;mJGxPS2GSIHPlcIx{NCCNaU2zOUBvVQ>? NGfpUJQyPTZyM{m2NC=>
Freestyle293F cells M3XLWmZ2dmO2aX;uJIF{e2G7 M2DpNmlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFHu[JJw\2WwIILlZ4VxfG:{IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGZz\WW|dIns[VI6O0ZiY3XscJMtKEmFNUC9NE4xPTRizszN MoLLNlMyQTl2N{e=
HEK293 cells NFTCTJpHfW6ldHnvckBie3OjeR?= M2TKW|MhcA>? Mlf6SIl{eGyjY3Xt[Y51KG:oIGuxO{1idHCqYT3t[ZRpgWxvM1jdcYljd2yncn;u[UBnem:vIHHu[JJw\2WwIILlZ4VxfG:{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOyCqcoOsJGlEPTB;NUSgcm0> NFfXZZUzOjN7MUCzNy=>
MDA453 cells NXK4NoxUTnWwY4Tpc44h[XO|YYm= MVzEbZNxdGGlZX3lcpQhd2ZiW{PIYWRJXCCocn;tJIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IHnuJG1FSTR3MzDj[YxteyxiS3m9OlQhdk1? NXzITIpbOTh{OUG2OFQ>
human MDA-MB-453 cells M{jS[mZ2dmO2aX;uJIF{e2G7 M1fNTmRqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hSVJiaX6gbJVu[W5iTVTBMW1DNTR3MzDj[YxteyxiSVO1NF03PCCwTR?= M1O5OlIxPTh2NkGw
COS1 cells NV3rWHRDTnWwY4Tpc44h[XO|YYm= NHfUVndCdnSjZ3;ubZN1KGGldHn2bZR6KGGpYXnud5QheFOJNT30ZYdo\WRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPPV|Eh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIILlZ4VxfG:{LX3l[IlifGWmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCkeTDBVk1z\We3bHH0[YQhemG2IIDyc4Jie2mwIIDyc41wfGW{IH\yZYdu\W62IHTybZZmdiCoaYLl[ox6KGy3Y3nm[ZJie2VicnXwc5J1\XJiYYPzZZktKEmFNUC9NE4xQDZ7IN88US=> MWmyOVY1PjZ2OR?=
HeLa cells NYDUfGNRTnWwY4Tpc44h[XO|YYm= M1joemFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDkbYh6\HKxdHXzeI9{fGW{b37lJIlv\HWlZXSgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHL5JJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NE4yPCEQvF2= MVixO|gxPDJ{OR?=
CV1 cells NIfzd4lHfW6ldHnvckBie3OjeR?= MU\CbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEXjFiY3XscJMtKEurPUCuNVUyKM7:TR?= NFvwSZUyPzJ3N{izPC=>
monkey COS7 cells M4OyVmZ2dmO2aX;uJIF{e2G7 NGS2RYNDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCvb37r[ZkhS0:VNzDj[YxteyCkeTD3bI9t\SClZXzsJIJqdmSrbnegZZN{[XluIFvpQVAvOTVzIN88US=> NWLiS49EOTh2NEK5NVI>
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CHO-K1 cells NWj0coQ{TnWwY4Tpc44h[XO|YYm= Mn7CNkBp MVnEbZNxdGGlZX3lcpQhd2ZiW{PIYY1q[m:uZYLvcoUh\nKxbTDoeY1idiCDUjDlfJBz\XO|ZXSgbY4hS0iRLVuxJINmdGy|IHHmeIVzKDJiaILzJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTB;MD6yJO69VQ>? M1PQ[FIxOzhzM{[x
human HT-3 cell MmqyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkezNVM1KM7:TR?= MnvyV2FPT0WU
human LNCAP cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 NWW1eGRUOyCmYYnz NWjwXnhVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNuIFnDOVA:OC55M{K3JO69VQ>? NXH3endJOjZyNE[zNVM>
human PC3 cells MUPGeY5kfGmxbjDhd5NigQ>? MoLmSIl{eGyjY3Xt[Y51KG:oIGuzTH1TOTh6MTDmdo9uKGGwZILv[4VvKHKnY3XweI9zKGmwIHj1cYFvKFCFMzDj[YxteyxiRVO1NF01NjNizszN MkKwNlU2QTFyNk[=
human 22Rv1 cells NFLGdWhHfW6ldHnvckBie3OjeR?= MWGzJIRigXN? M3z3NWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiYX7kdo9o\W5icnXj[ZB1d3JiSEi3OHkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKGi3bXHuJFIzWnZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTEiWLXnu[JVk\WRiY3XscEBoem:5dHigZYZ1\XJiMzDkZZl{KGK7IGfTWE05KGG|c3H5MEBKSzVyPUSuOkDPxE1? MWKyOFkxODV6OB?=
human CCF-STTG1 cell M1nEU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGLwXIpKdmirYnn0bY9vKG:oIHj1cYFvKEOFRj3TWHRIOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;ND65NlkzQSEQvF2= MlzZV2FPT0WU
human SCC-25 cell MlyzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoftTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvMkWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlA5PjV4IN88US=> NHfNOWZUSU6JRWK=
human MKN45 cell MmXmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmL0TY5pcWKrdHnvckBw\iCqdX3hckBOU052NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uPVYxPSEQvF2= NFPvRldUSU6JRWK=
human ES5 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3\TOGlvcGmkaYTpc44hd2ZiaIXtZY4hTVN3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OD62NVE2PCEQvF2= M3HKdnNCVkeHUh?=
human SK-MEL-3 cell M2\heGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlnCTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjB7NkSg{txO M{\G[HNCVkeHUh?=
human PC-3 cell NV:2WVNxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJHBENTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMD6yO|kyKM7:TR?= M1;ifnNCVkeHUh?=
human NOS-1 cell NEO0O2xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnPCTY5pcWKrdHnvckBw\iCqdX3hckBPV1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlI6OTdizszN M1uwe3NCVkeHUh?=
human LB1047-RCC cell NYfrZmoxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4O3e2lvcGmkaYTpc44hd2ZiaIXtZY4hVEJzMES3MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{LkK1N{DPxE1? MWDTRW5ITVJ?
human CAMA-1 cell NEjvXHJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGNCVUFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlM6OjZizszN M{fZPHNCVkeHUh?=
human SAS cell NWLufI1wT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmTYTY5pcWKrdHnvckBw\iCqdX3hckBUSVNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6zNFgyKM7:TR?= MlrpV2FPT0WU
human NCI-H2228 cell M1TTbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmSxTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyNlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy55NUOxJO69VQ>? M1LQVHNCVkeHUh?=
human NCI-H187 cell NI\yc|dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M320bmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi54NkG2JO69VQ>? MoXCV2FPT0WU
human BFTC-905 cell MnfhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1zQSmlvcGmkaYTpc44hd2ZiaIXtZY4hSk[WQz25NFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy52OEW3JO69VQ>? M{XrTnNCVkeHUh?=
human G-361 cell NVvme2RrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{PVSWlvcGmkaYTpc44hd2ZiaIXtZY4hTy1|NkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xO{45OjZizszN NUXNfo9JW0GQR1XS
human DU145 cells M{DpN2N6fG:2b4jpZ:Kh[XO|YYm= NIfPe4k4OiCq Ml;6R5l1d3SxeHnjbZR6KGGpYXnud5QhTVKjbIDoZU1l\W[rY3nlcpQhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCHUnLleIEh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yQCEQvF2= MWHTRW5ITVJ?
human SW780 cell M4HG[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= MmWyV2FPT0WU
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human KALS-1 cell NUK3OZNXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGHNfGRKdmirYnn0bY9vKG:oIHj1cYFvKEuDTGOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6NjZ4M{Wg{txO MmGwV2FPT0WU
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human RVH-421 cell NXf0SZNET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUnhTos4UW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwNUe5OUDPxE1? M1;BbHNCVkeHUh?=
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human RO82-W-1 cell M3XaR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MonwTY5pcWKrdHnvckBw\iCqdX3hckBTVzh{LWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjF|MUig{txO M37lO3NCVkeHUh?=
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human CTB-1 cell M{HwbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGDReWxKdmirYnn0bY9vKG:oIHj1cYFvKEOWQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPTV|NjFOwG0> MmPvV2FPT0WU
human SW48 cell MnzlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWrNdG46UW6qaXLpeIlwdiCxZjDoeY1idiCVV{S4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPjV2NjFOwG0> MoS4V2FPT0WU
human TCCSUP cell NHqwdm5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJHRES1OXUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlczOzJizszN NWnyZ4REW0GQR1XS
human DK-MG cell M4fwV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVjJcohq[mm2aX;uJI9nKGi3bXHuJGRMNU2JIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuPFkyPyEQvF2= NYnrNoZFW0GQR1XS
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human H4 cell M3e0TWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYLJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjZwOUS1PEDPxE1? NVzaXG1LW0GQR1XS
human SBC-1 cell M3vNd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYrJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkiuN|UxPyEQvF2= M1TWRXNCVkeHUh?=
human CAS-1 cell MoPrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGNCWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkiuOlI6PCEQvF2= M4LHO3NCVkeHUh?=
human OAW-42 cell M{T1Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKGi3bXHuJG9CXy12MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlcyQTVizszN MVXTRW5ITVJ?
human HCC1954 cell Ml7OS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzF7NUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE44PTJ3IN88US=> MYrTRW5ITVJ?
human MDA-MB-453 cell M3;oOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20OVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQS57MEeg{txO NEXpV2dUSU6JRWK=
human MCF7 cell NXHJWJlET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX7Jcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|OT6zNFEh|ryP MYPTRW5ITVJ?
human PC3 cells NFPUVJVHfW6ldHnvckBie3OjeR?= NWHqTI9uOTBy45EA{txO Mm\KOFghcA>? MWHJcohq[mm2aX;uJI9nKGGldHnuJIJie2WmIIDz[ZVld3CxZHnhJIZwem2jdHnvckBqdiCjbnTyc4dmdi2mZYDlcoRmdnRiaIXtZY4hWEN|IHPlcIx{KGG2IEGwNEB2VSCjZoTldkA1QCCqcoOgZpkhTEGSSTDzeIFqdmmwZzDiZZNm\CCobIXvdoV{[2WwY3WgcYlkem:|Y3;wfUBie3OjeR?= M1TqV|IzPjd{OUi0
human PC3 cells MoXDSpVv[3Srb36gZZN{[Xl? M4PiWlAvOS1zIN88US=> NITaO5FC\2:waYP0JIFkfGm4aYT5JIF1KGGwZILv[4VvKHKnY3XweI9zKFd5NEHDJI12fGGwdDDlfJBz\XO|ZXSgbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KHO2aX31cIF1cW:wIH;mJJJm[2WydH;yJJRz[W6|YXP0bZZifGmxbjDheEAxNjFidH:gNUB2VSCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> MX:yNlE4PTZ7NB?=

... 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
  • 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)

  • 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 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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID