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 NEX6dIpHfW6ldHnvckBie3OjeR?= M3rBfWRqe3CuYXPlcYVvfCCxZjDbN2heWjF6OEGg[pJwdSCDUjDpckBpfW2jbjDNSGEuVUJvNEWzJINmdGy|LDDFR|UxRTNzIH7N NHfzTmYzOzdzM{W2Oy=>
LNCaP cells MYPGeY5kfGmxbjDhd5NigQ>? M3jKdGlvcGmkaYTpc44hd2ZiW{PIYU1FUFRiYnnu[Ilv\yC2bzDUPFc4SSCjbnTyc4dmdiC{ZXPldJRweiCxZjDMUmNiWCClZXzsd{whU2l;M{Wgcm0> Mn\JNVU3ODN7NkC=
Freestyle293F cells NXPIXnV6TnWwY4Tpc44h[XO|YYm= NWi5dIxPUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgRY5lem:pZX6gdoVk\XC2b4KgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hTnKnZYP0fYxmOjl|RjDj[YxteyxiSVO1NF0xNjB3NDFOwG0> NYnLeXZtOjNzOUm0O|c>
HEK293 cells MXrGeY5kfGmxbjDhd5NigQ>? NFfwfXU{KGh? NIPYblhFcXOybHHj[Y1mdnRib3[gX|E4NWGucHjhMY1mfGi7bD2zTH1ucWKxbHXyc45mKG[{b32gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDh[pRmeiB|IHjyd{whUUN3ME21OEBvVQ>? MnXlNlI{QTFyM{O=
MDA453 cells MUXGeY5kfGmxbjDhd5NigQ>? Mk\YSIl{eGyjY3Xt[Y51KG:oIGuzTH1FUFRiZoLvcUBpfW2jbjDhcoRzd2enbjDy[YNmeHSxcjDpckBOTEF2NUOgZ4VtdHNuIFvpQVY1KG6P NETDfoMyQDJ7MU[0OC=>
human MDA-MB-453 cells NXzUWlFRTnWwY4Tpc44h[XO|YYm= NGXG[ppFcXOybHHj[Y1mdnRib3[gX|NJZUSKVDDmdo9uKEGUIHnuJIh2dWGwIF3ERU1OSi12NUOgZ4VtdHNuIFnDOVA:PjRibl2= MnXMNlA2QDR4MUC=
COS1 cells NIDkZ|JHfW6ldHnvckBie3OjeR?= MkHKRY51[WexbnnzeEBi[3Srdnn0fUBi\2GrboP0JJBUTzVvdHHn[4VlKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCFT2OxJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC{ZXPldJRwei2vZXTpZZRm\CC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkh[nliQWKtdoVofWyjdHXkJJJifCCycn;iZZNqdiCycn;tc5RmeiCocnHncYVvfCCmcnn2[Y4h\mm{ZX\sfUBtfWOrZnXyZZNmKHKncH;yeIVzKGG|c3H5MEBKSzVyPUCuNFg3QSEQvF2= MWGyOVY1PjZ2OR?=
HeLa cells MVzGeY5kfGmxbjDhd5NigQ>? NHj6W4pCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKGGwZILv[4VvKHKnY3XweI9zKGW6cILld5Nm\CCrbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[g[IlpgWS{b4Tld5Rwe3Sncn;u[UBqdmS3Y3XkJJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eTDifUBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVAvOTRizszN M3WwVVE4QDB2MkK5
CV1 cells M3v5SWZ2dmO2aX;uJIF{e2G7 M1TrXmJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEOYMTDj[YxteyxiS3m9NE4yPTFizszN M1rNTFE4OjV5OEO4
monkey COS7 cells NXrEZ2FnTnWwY4Tpc44h[XO|YYm= NHnueJlDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCvb37r[ZkhS0:VNzDj[YxteyCkeTD3bI9t\SClZXzsJIJqdmSrbnegZZN{[XluIFvpQVAvOTVzIN88US=> NH3jUI8yQDR2MkmxNi=>
COS7 cells NX3LOlZHTnWwY4Tpc44h[XO|YYm= NF7FeZpC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJHc4PDGFIH31eIFvfCCneIDy[ZN{\WRiaX6gR29UPyClZXzsd{Bie3Onc4Pl[EBieyCudXPp[oVz[XOnIHHjeIl3cXS7IHHmeIVzKDJ2IHjyd{BjgSC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMUig{txO NVLPO5NwOjJyOUSyO|k>
CHO-K1 cells MonvSpVv[3Srb36gZZN{[Xl? MYKyJIg> NVLkPHFwTGm|cHzhZ4Vu\W62IH;mJHs{UF2vaXLvcIVzd26nIH\yc40hcHWvYX6gRXIh\XiycnXzd4VlKGmwIFPIU{1MOSClZXzsd{Bi\nSncjCyJIhzeyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwQVAvOiEQvF2= M{DDXVIxOzhzM{[x
human HT-3 cell NG\EZ5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkezNVM1KM7:TR?= NGrQdlJUSU6JRWK=
human LNCAP cells M3T6OnBzd2yrZnXyZZRqd25iYYPzZZk> NVrMWZQxOyCmYYnz M3\OeGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiMzDkZZl{NCCLQ{WwQVAvPzN{NzFOwG0> NFO5dW0zPjB2NkOxNy=>
human PC3 cells NHHPXZJHfW6ldHnvckBie3OjeR?= M4r5cmRqe3CuYXPlcYVvfCCxZjDbN2heWjF6OEGg[pJwdSCjbnTyc4dmdiC{ZXPldJRweiCrbjDoeY1idiCSQ{OgZ4VtdHNuIFXDOVA:PC5|IN88US=> MVSyOVU6OTB4Nh?=
human 22Rv1 cells NFXhWYJHfW6ldHnvckBie3OjeR?= M13QdlMh\GG7cx?= NXPkU2VUSW62YXfvcol{fCCjY4Tpeol1gSCjdDDhcoRzd2enbjDy[YNmeHSxcjDIPFc1YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hOjKUdkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCGSGStbY5lfWOnZDDj[YxtKGe{b4f0bEBi\nSncjCzJIRigXNiYomgW3NVNThiYYPzZZktKEmFNUC9OE43KM7:TR?= MYSyOFkxODV6OB?=
human CCF-STTG1 cell MkjBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DGNWlvcGmkaYTpc44hd2ZiaIXtZY4hS0OILWPUWGcyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD12LkmyPVI6KM7:TR?= M4PnZXNCVkeHUh?=
human SCC-25 cell NWjaeok5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF7BSGZKdmirYnn0bY9vKG:oIHj1cYFvKFOFQz2yOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvODh4NU[g{txO NUntOm91W0GQR1XS
human MKN45 cell MmfnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2Xx[mlvcGmkaYTpc44hd2ZiaIXtZY4hVUuQNEWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Mlk3ODVizszN NV;kOGdiW0GQR1XS
human ES5 cell NH\CUYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJGVUPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRThwNkGxOVQh|ryP NEjV[YlUSU6JRWK=
human SK-MEL-3 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlLNTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjB7NkSg{txO MXzTRW5ITVJ?
human PC-3 cell M{GxT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1PiPWlvcGmkaYTpc44hd2ZiaIXtZY4hWENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlI4QTFizszN MVjTRW5ITVJ?
human NOS-1 cell M1jMXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoT0TY5pcWKrdHnvckBw\iCqdX3hckBPV1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlI6OTdizszN M1fhSHNCVkeHUh?=
human LB1047-RCC cell NXS3cnBnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYLJcohq[mm2aX;uJI9nKGi3bXHuJGxDOTB2Nz3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5{NUOg{txO NXy3VFlsW0GQR1XS
human CAMA-1 cell NHP0SGdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWHES2JyUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|OUK2JO69VQ>? NFrwbGxUSU6JRWK=
human SAS cell NVfqUItOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEf6VnJKdmirYnn0bY9vKG:oIHj1cYFvKFODUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlMxQDFizszN NYD3TJFZW0GQR1XS
human NCI-H2228 cell Mn;ZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkKyPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{Njd3M{Gg{txO M2nZNXNCVkeHUh?=
human NCI-H187 cell M3v6S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF7US3lKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVg4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwNk[xOkDPxE1? NXHyZ2szW0GQR1XS
human BFTC-905 cell M{TpSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4mxb2lvcGmkaYTpc44hd2ZiaIXtZY4hSk[WQz25NFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy52OEW3JO69VQ>? NX\FUm8zW0GQR1XS
human G-361 cell NEK2N29Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYfKfYVlUW6qaXLpeIlwdiCxZjDoeY1idiCJLUO2NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE4Njh{NjFOwG0> M4rEfHNCVkeHUh?=
human DU145 cells MoO0R5l1d3SxeHnjxsBie3OjeR?= MWe3NkBp MonjR5l1d3SxeHnjbZR6KGGpYXnud5QhTVKjbIDoZU1l\W[rY3nlcpQhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCHUnLleIEh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yQCEQvF2= MkTQV2FPT0WU
human SW780 cell NYHJRXdwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{PSUWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfS=> M2X3dHNCVkeHUh?=
human BB49-HNC cell MlruS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVgvQTV|MjFOwG0> MkPzV2FPT0WU
human KALS-1 cell NV:4[WFpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoTlTY5pcWKrdHnvckBw\iCqdX3hckBMSUyVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU43PjN3IN88US=> NGHISI5USU6JRWK=
human AU565 cell M4TGcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlfaTY5pcWKrdHnvckBw\iCqdX3hckBCXTV4NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5Mlc1ODJizszN Mnj3V2FPT0WU
human NCI-H2087 cell M2jhN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkC4O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjB3OUGg{txO NU\O[ndbW0GQR1XS
human RVH-421 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXLJcohq[mm2aX;uJI9nKGi3bXHuJHJXUC12MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU42Pzl3IN88US=> MUHTRW5ITVJ?
human SK-CO-1 cell NHzaO5lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWfENWhNUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3DU{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwOEi3NkDPxE1? MYDTRW5ITVJ?
human KU-19-19 cell NVLzRZdlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGtWNTF7LUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvODJ2MjFOwG0> M2\YfXNCVkeHUh?=
human NB6 cell NWfaeJRST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJG5DPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ{LkmxN|Uh|ryP NEfQVFVUSU6JRWK=
human RO82-W-1 cell NIj6W5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYC4dZZxUW6qaXLpeIlwdiCxZjDoeY1idiCUT{iyMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ|LkGzNVgh|ryP NXexdHNLW0GQR1XS
human LNCAP cells M13NfWN6fG:2b4jpZ:Kh[XO|YYm= MXiyJIRigXN? Ml\jR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5ESVBiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgNkBl[Xm|IHL5JINmdGxiY3;1cpRqdmdibXX0bI9lNCCLQ{WwQVI{Njd7IN88US=> MX[yN|czPzB2NB?=
human CTB-1 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3jTc2lvcGmkaYTpc44hd2ZiaIXtZY4hS1SELUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE42PTN4IN88US=> MXLTRW5ITVJ?
human SW48 cell NEPFV|VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXnJcohq[mm2aX;uJI9nKGi3bXHuJHNYPDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{ND62OVQ3KM7:TR?= MXnTRW5ITVJ?
human TCCSUP cell NFroSVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NED4RplKdmirYnn0bY9vKG:oIHj1cYFvKFSFQ2PVVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1Njd{M{Kg{txO M{jUb3NCVkeHUh?=
human DK-MG cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVXpZ4RnUW6qaXLpeIlwdiCxZjDoeY1idiCGSz3NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1Njh7MUeg{txO M3TDOnNCVkeHUh?=
human ST486 cell MnK1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnjETY5pcWKrdHnvckBw\iCqdX3hckBUXDR6NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK1Mlc1PjRizszN NF;MUZBUSU6JRWK=
human H4 cell M4jjdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUfNU3ZmUW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK2Mlk1PThizszN M{T4ZnNCVkeHUh?=
human SBC-1 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEDkSI9KdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvOzVyNzFOwG0> NV;3bYVOW0GQR1XS
human CAS-1 cell NGrocohIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NILYUpJKdmirYnn0bY9vKG:oIHj1cYFvKEODUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPjJ7NDFOwG0> MY\TRW5ITVJ?
human OAW-42 cell M1HjVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4DHfmlvcGmkaYTpc44hd2ZiaIXtZY4hV0GZLUSyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzF7NTFOwG0> NFv2UmNUSU6JRWK=
human HCC1954 cell NETKeI9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnxUHRqUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxPVU1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjhwN{WyOUDPxE1? NWrMR29EW0GQR1XS
human MDA-MB-453 cell M3;lNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20OVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQS57MEeg{txO NYW2cnp{W0GQR1XS
human MCF7 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUi2SXVXUW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvOzBzIN88US=> MXnTRW5ITVJ?
human PC3 cells MmLTSpVv[3Srb36gZZN{[Xl? MX[xNFDkiIEQvF2= NIfWe|Y1QCCq M4PpPGlvcGmkaYTpc44hd2ZiYXP0bY4h[mG|ZXSgdJNmfWSxcH;kbYEh\m:{bXH0bY9vKGmwIHHu[JJw\2WwLXTldIVv\GWwdDDoeY1idiCSQ{OgZ4VtdHNiYYSgNVAxKHWPIHHmeIVzKDR6IHjyd{BjgSCGQWDJJJN1[WmwaX7nJIJie2WmIH\seY9z\XOlZX7j[UBucWO{b4Pjc5B6KGG|c3H5 MVeyNlY4Ojl6NB?=
human PC3 cells NFnSbohHfW6ldHnvckBie3OjeR?= MYiwMlEuOSEQvF2= MWHB[49vcXO2IHHjeIl3cXS7IHH0JIFv\HKxZ3XuJJJm[2WydH;yJHc4PDGFIH31eIFvfCCneIDy[ZN{\WRiaX6gbJVu[W5iUFOzJINmdGy|IHHzd4V{e2WmIHHzJJN1cW23bHH0bY9vKG:oIILlZ4VxfG:{IITyZY5{[WO2aY\heIlwdiCjdDCwMlEhfG9iMTD1UUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MUGyNlE4PTZ7NB?=

... 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
    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 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