Bicalutamide

For research use only.

Catalog No.S1190 Synonyms: ICI-176334

20 publications

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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Selleck's Bicalutamide has been cited by 20 publications

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 MmL4SpVv[3Srb36gZZN{[Xl? MoW5SIl{eGyjY3Xt[Y51KG:oIGuzTH1TOTh6MTDmdo9uKEGUIHnuJIh2dWGwIF3ERU1OSi12NUOgZ4VtdHNuIFXDOVA:OzFibl2= NFOwTI4zOzdzM{W2Oy=>
LNCaP cells MUHGeY5kfGmxbjDhd5NigQ>? NXPtd5ZnUW6qaXLpeIlwdiCxZjDbN2heNUSKVDDibY5lcW6pIITvJHQ5PzeDIHHu[JJw\2WwIILlZ4VxfG:{IH;mJGxPS2GSIHPlcIx{NCCNaU2zOUBvVQ>? NWnWb4FQOTV4MEO5OlA>
Freestyle293F cells NFrNUVdHfW6ldHnvckBie3OjeR?= NXzOdI41UW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgRY5lem:pZX6gdoVk\XC2b4KgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hTnKnZYP0fYxmOjl|RjDj[YxteyxiSVO1NF0xNjB3NDFOwG0> MV[yN|E6QTR5Nx?=
HEK293 cells NGr0bFlHfW6ldHnvckBie3OjeR?= NEjlV2Q{KGh? M2[zT2Rqe3CuYXPlcYVvfCCxZjDbNVcu[WyyaHGtcYV1cHmuLUPIYY1q[m:uZYLvcoUh\nKxbTDhcoRzd2enbjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHmeIVzKDNiaILzMEBKSzVyPUW0JI5O MoDvNlI{QTFyM{O=
MDA453 cells MUjGeY5kfGmxbjDhd5NigQ>? M4WwXGRqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgbY4hVUSDNEWzJINmdGy|LDDLbV03PCCwTR?= MlvYNVgzQTF4NES=
human MDA-MB-453 cells NXrNcWNmTnWwY4Tpc44h[XO|YYm= M120OWRqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hSVJiaX6gbJVu[W5iTVTBMW1DNTR3MzDj[YxteyxiSVO1NF03PCCwTR?= M1fvXFIxPTh2NkGw
COS1 cells NHLlepJHfW6ldHnvckBie3OjeR?= NH7wXZFCdnSjZ3;ubZN1KGGldHn2bZR6KGGpYXnud5QheFOJNT30ZYdo\WRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPPV|Eh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIILlZ4VxfG:{LX3l[IlifGWmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCkeTDBVk1z\We3bHH0[YQhemG2IIDyc4Jie2mwIIDyc41wfGW{IH\yZYdu\W62IHTybZZmdiCoaYLl[ox6KGy3Y3nm[ZJie2VicnXwc5J1\XJiYYPzZZktKEmFNUC9NE4xQDZ7IN88US=> NVTLUIs2OjV4NE[2OFk>
HeLa cells NXPyOYpYTnWwY4Tpc44h[XO|YYm= NGrDTodCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKGGwZILv[4VvKHKnY3XweI9zKGW6cILld5Nm\CCrbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[g[IlpgWS{b4Tld5Rwe3Sncn;u[UBqdmS3Y3XkJJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eTDifUBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVAvOTRizszN NGXxO5QyPzhyNEKyPS=>
CV1 cells MUXGeY5kfGmxbjDhd5NigQ>? MlXKRolv\GmwZzDh[oZqdmm2eTD0c{BpfW2jbjDhcoRzd2enbjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hS1ZzIHPlcIx{NCCNaU2wMlE2OSEQvF2= M3GwUFE4OjV5OEO4
monkey COS7 cells MnLWSpVv[3Srb36gZZN{[Xl? NVjhdmY3SmmwZHnu[{Bi\m[rbnn0fUB1dyCqdX3hckBidmS{b3flckBz\WOncITvdkBmgHC{ZYPz[YQhcW5ibX;ub4V6KEORU{egZ4VtdHNiYomge4hwdGViY3XscEBjcW6maX7nJIF{e2G7LDDLbV0xNjF3MTFOwG0> Moi1NVg1PDJ7MUK=
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CHO-K1 cells MojsSpVv[3Srb36gZZN{[Xl? MoDtNkBp NVrVbIVMTGm|cHzhZ4Vu\W62IH;mJHs{UF2vaXLvcIVzd26nIH\yc40hcHWvYX6gRXIh\XiycnXzd4VlKGmwIFPIU{1MOSClZXzsd{Bi\nSncjCyJIhzeyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwQVAvOiEQvF2= NH70b3IzODN6MUO2NS=>
human HT-3 cell NX;TS5FGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmTDTY5pcWKrdHnvckBw\iCqdX3hckBJXC1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63N|E{PCEQvF2= NF3ueJlUSU6JRWK=
human LNCAP cells M4SybXBzd2yrZnXyZZRqd25iYYPzZZk> MlfZN{Bl[Xm| NF20eIpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyxiSVO1NF0xNjd|Mkeg{txO NH7OSY8zPjB2NkOxNy=>
human PC3 cells M1[2Z2Z2dmO2aX;uJIF{e2G7 NX\pd2Q3TGm|cHzhZ4Vu\W62IH;mJHs{UF2UMUi4NUBnem:vIHHu[JJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIGDDN{Bk\WyuczygSWM2OD12LkOg{txO MkX2NlU2QTFyNk[=
human 22Rv1 cells NFn1WGFHfW6ldHnvckBie3OjeR?= MkjNN{Bl[Xm| MXnBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGGwZILv[4VvKHKnY3XweI9zKEh6N{TZJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBpfW2jbjCyNnJ3OSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGRJXC2rbnT1Z4VlKGOnbHyg[5Jwf3SqIHHmeIVzKDNiZHH5d{BjgSCZU2StPEBie3OjeTygTWM2OD12Lk[g{txO NFLEOnczPDlyMEW4PC=>
human CCF-STTG1 cell M3LRTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWfJcohq[mm2aX;uJI9nKGi3bXHuJGNETi2VVGTHNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:PC57MkmyPUDPxE1? NHLtfXNUSU6JRWK=
human SCC-25 cell M{nnS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MofOTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvMkWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlA5PjV4IN88US=> M4D6d3NCVkeHUh?=
human MKN45 cell M4q2dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;oO202UW6qaXLpeIlwdiCxZjDoeY1idiCPS160OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvQTZyNTFOwG0> MXjTRW5ITVJ?
human ES5 cell M2Xa[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHfDPXZKdmirYnn0bY9vKG:oIHj1cYFvKEWVNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOlEyPTRizszN NEe3XVBUSU6JRWK=
human SK-MEL-3 cell MkXlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXHJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvODl4NDFOwG0> NYHF[nlyW0GQR1XS
human PC-3 cell NInhUWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4rObWlvcGmkaYTpc44hd2ZiaIXtZY4hWENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlI4QTFizszN M3;PdnNCVkeHUh?=
human NOS-1 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWixTlVvUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjJ7MUeg{txO NXT2TGs1W0GQR1XS
human LB1047-RCC cell NWTLeWp3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV2yToo4UW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuNlU{KM7:TR?= NHrTXWxUSU6JRWK=
human CAMA-1 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVj0U|JVUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|OUK2JO69VQ>? NYizdlFQW0GQR1XS
human SAS cell M2rVbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{XoU2lvcGmkaYTpc44hd2ZiaIXtZY4hW0GVIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuN|A5OSEQvF2= NXrxcGhYW0GQR1XS
human NCI-H2228 cell NYnETGlXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnjtTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyNlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy55NUOxJO69VQ>? MkGwV2FPT0WU
human NCI-H187 cell NFPr[FVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYTUXI8xUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4Lk[2NVYh|ryP MWHTRW5ITVJ?
human BFTC-905 cell Ml7iS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DJdWlvcGmkaYTpc44hd2ZiaIXtZY4hSk[WQz25NFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy52OEW3JO69VQ>? NYLNSXU6W0GQR1XS
human G-361 cell MnK5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE\xZ4lKdmirYnn0bY9vKG:oIHj1cYFvKEdvM{[xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvQDJ4IN88US=> M4\PV3NCVkeHUh?=
human DU145 cells NEnzXVFEgXSxdH;4bYPDqGG|c3H5 M1m0fVczKGh? MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBGWmGucHjhMYRm\mmlaXXueEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEWUYnX0ZUBie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE5KM7:TR?= MnTMV2FPT0WU
human SW780 cell M4PhPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= MnT0V2FPT0WU
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human KALS-1 cell NVfVWFlET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGtCVFNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlY3OzVizszN M3q0NHNCVkeHUh?=
human AU565 cell NXj1WXVpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWTJcohq[mm2aX;uJI9nKGi3bXHuJGFWPTZ3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuO|QxOiEQvF2= MW\TRW5ITVJ?
human NCI-H2087 cell NYr0OpBCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF\yZ4lKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJzLkC1PVEh|ryP Ml7tV2FPT0WU
human RVH-421 cell M2rPWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWXJcohq[mm2aX;uJI9nKGi3bXHuJHJXUC12MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU42Pzl3IN88US=> NULwZ5NnW0GQR1XS
human SK-CO-1 cell NYDlO3R3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTDd4tOUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3DU{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwOEi3NkDPxE1? NIjr[IZUSU6JRWK=
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human NB6 cell NVnIcIVRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHGyU21KdmirYnn0bY9vKG:oIHj1cYFvKE6ENjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlkyOzVizszN NWD5N|ZsW0GQR1XS
human RO82-W-1 cell Ml\US5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIDDN|BKdmirYnn0bY9vKG:oIHj1cYFvKFKROEKtW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwMUOxPEDPxE1? NIj0UZpUSU6JRWK=
human LNCAP cells MXvDfZRwfG:6aXRCpIF{e2G7 MVyyJIRigXN? NHnGdGVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkAzKGSjeYOgZpkh[2WubDDjc5VvfGmwZzDt[ZRpd2RuIFnDOVA:OjNwN{mg{txO NETrcGozOzd{N{C0OC=>
human CTB-1 cell MmTDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{jOemlvcGmkaYTpc44hd2ZiaIXtZY4hS1SELUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE42PTN4IN88US=> MnSzV2FPT0WU
human SW48 cell MkjqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFrlN5lKdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE43PTR4IN88US=> MWXTRW5ITVJ?
human TCCSUP cell NYmyPIpFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1zoRWlvcGmkaYTpc44hd2ZiaIXtZY4hXEOFU2XQJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPzJ|MjFOwG0> MnvLV2FPT0WU
human DK-MG cell M3vLUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGRMNU2JIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuPFkyPyEQvF2= MkfwV2FPT0WU
human ST486 cell NHnpVWpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXvJcohq[mm2aX;uJI9nKGi3bXHuJHNVPDh4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkWuO|Q3PCEQvF2= Mn7QV2FPT0WU
human H4 cell NY[3ZYN5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXrMRVRuUW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK2Mlk1PThizszN M2e4XnNCVkeHUh?=
human SBC-1 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlLzTY5pcWKrdHnvckBw\iCqdX3hckBUSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlM2ODdizszN M3\RUXNCVkeHUh?=
human CAS-1 cell MlPkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\GTY5pcWKrdHnvckBw\iCqdX3hckBESVNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlYzQTRizszN M3zifHNCVkeHUh?=
human OAW-42 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M324dWlvcGmkaYTpc44hd2ZiaIXtZY4hV0GZLUSyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzF7NTFOwG0> M3juU3NCVkeHUh?=
human HCC1954 cell NWfrdIlDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnV[2dKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G5OVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQC55NUK1JO69VQ>? NVnZNI9OW0GQR1XS
human MDA-MB-453 cell MoW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHrkd4xKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk01PTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{OT65NFch|ryP M2G3dnNCVkeHUh?=
human MCF7 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4\nd2lvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO5MlMxOSEQvF2= Mke3V2FPT0WU
human PC3 cells MYDGeY5kfGmxbjDhd5NigQ>? MYqxNFDkiIEQvF2= MY[0PEBp MkK5TY5pcWKrdHnvckBw\iCjY4TpckBj[XOnZDDwd4V2\G:yb3TpZUBnd3KvYYTpc44hcW5iYX7kdo9o\W5vZHXw[Y5l\W62IHj1cYFvKFCFMzDj[YxteyCjdDCxNFAhfU1iYX\0[ZIhPDhiaILzJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJI1q[3Kxc3PvdJkh[XO|YYm= NVTTbWkxOjJ4N{K5PFQ>
human PC3 cells Mln3SpVv[3Srb36gZZN{[Xl? M4fEUFAvOS1zIN88US=> Mn7oRYdwdmm|dDDhZ5Rqfmm2eTDheEBidmS{b3flckBz\WOncITvdkBYPzRzQzDteZRidnRiZYjwdoV{e2WmIHnuJIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{B{fGmvdXzheIlwdiCxZjDy[YNmeHSxcjD0doFve2GldHn2ZZRqd25iYYSgNE4yKHSxIEGgeW0h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NH;XOmkzOjF5NU[5OC=>

... 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
  • 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
Smiles CC(O)(C[S](=O)(=O)C1=CC=C(F)C=C1)C(=O)NC2=CC=C(C#N)C(=C2)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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 Unknown status 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
NCT01415791 Completed Drug: ICI176334-1 Healthy AstraZeneca August 2011 Phase 1
NCT01415778 Completed Drug: ICI176334-1|Drug: Casodex 80 mg tablet 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

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID