Bicalutamide (ICI-176334)

For research use only.

Catalog No.S1190

38 publications

Bicalutamide (ICI-176334) Chemical Structure

CAS No. 90357-06-5

Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.

Selleck's Bicalutamide (ICI-176334) has been cited by 38 publications

Purity & Quality Control

Choose Selective Androgen Receptor Inhibitors

Biological Activity

Description Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
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 NUTw[FVbTnWwY4Tpc44h[XO|YYm= NULlXGRxTGm|cHzhZ4Vu\W62IH;mJHs{UF2UMUi4NUBnem:vIFHSJIlvKGi3bXHuJG1FSS2PQj20OVMh[2WubIOsJGVEPTB;M{Ggcm0> NE\qZ5UzOzdzM{W2Oy=>
LNCaP cells NGnlcZhHfW6ldHnvckBie3OjeR?= NF\3dHpKdmirYnn0bY9vKG:oIGuzTH0uTEiWIHLpcoRqdmdidH:gWFg4P0FiYX7kdo9o\W5icnXj[ZB1d3Jib3[gUG5E[VBiY3XscJMtKEurPUO1JI5O MoW4NVU3ODN7NkC=
Freestyle293F cells M3LMWWZ2dmO2aX;uJIF{e2G7 M1u4TmlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFHu[JJw\2WwIILlZ4VxfG:{IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGZz\WW|dIns[VI6O0ZiY3XscJMtKEmFNUC9NE4xPTRizszN NEDzOZczOzF7OUS3Oy=>
HEK293 cells MWLGeY5kfGmxbjDhd5NigQ>? NU\GTm9OOyCq NHXXZlZFcXOybHHj[Y1mdnRib3[gX|E4NWGucHjhMY1mfGi7bD2zTH1ucWKxbHXyc45mKG[{b32gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDh[pRmeiB|IHjyd{whUUN3ME21OEBvVQ>? MWOyNlM6OTB|Mx?=
MDA453 cells M{DXSGZ2dmO2aX;uJIF{e2G7 MXHEbZNxdGGlZX3lcpQhd2ZiW{PIYWRJXCCocn;tJIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IHnuJG1FSTR3MzDj[YxteyxiS3m9OlQhdk1? NXPwSI12OTh{OUG2OFQ>
human MDA-MB-453 cells MlL4SpVv[3Srb36gZZN{[Xl? MVrEbZNxdGGlZX3lcpQhd2ZiW{PIYWRJXCCocn;tJGFTKGmwIHj1cYFvKE2GQT3NRk01PTNiY3XscJMtKEmFNUC9OlQhdk1? MUWyNFU5PDZzMB?=
COS1 cells NXjidWFYTnWwY4Tpc44h[XO|YYm= MX7BcpRi\2:waYP0JIFkfGm4aYT5JIFo[Wmwc4SgdHNIPS22YXfn[YQhcHWvYX6gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEORU{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKHKnY3XweI9zNW2nZHnheIVlKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBjgSCDUj3y[Yd2dGG2ZXSgdoF1KHC{b3Lhd4lvKHC{b33veIVzKG[{YXft[Y51KGS{aY\lckBncXKnZnz5JIx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmsJGlEPTB;MD6wPFY6KM7:TR?= NX;zS4pSOjV4NE[2OFk>
HeLa cells NVvpdnF5TnWwY4Tpc44h[XO|YYm= M2PYWWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDkbYh6\HKxdHXzeI9{fGW{b37lJIlv\HWlZXSgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHL5JJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NE4yPCEQvF2= M1PXOVE4QDB2MkK5
CV1 cells NVrJcnNtTnWwY4Tpc44h[XO|YYm= NFfZe3hDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCFVkGgZ4VtdHNuIFvpQVAvOTVzIN88US=> M4K1cVE4OjV5OEO4
monkey COS7 cells MXjGeY5kfGmxbjDhd5NigQ>? M4LXRWJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKG2xbnvlfUBEV1N5IHPlcIx{KGK7IIfoc4xmKGOnbHygZolv\GmwZzDhd5NigSxiS3m9NE4yPTFizszN M1nZ[lE5PDR{OUGy
COS7 cells M4PLPWZ2dmO2aX;uJIF{e2G7 NGjjd2xC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJHc4PDGFIH31eIFvfCCneIDy[ZN{\WRiaX6gR29UPyClZXzsd{Bie3Onc4Pl[EBieyCudXPp[oVz[XOnIHHjeIl3cXS7IHHmeIVzKDJ2IHjyd{BjgSC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMUig{txO NYHU[ldoOjJyOUSyO|k>
CHO-K1 cells Mn3pSpVv[3Srb36gZZN{[Xl? NFrh[ZYzKGh? NXzzS29ETGm|cHzhZ4Vu\W62IH;mJHs{UF2vaXLvcIVzd26nIH\yc40hcHWvYX6gRXIh\XiycnXzd4VlKGmwIFPIU{1MOSClZXzsd{Bi\nSncjCyJIhzeyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwQVAvOiEQvF2= MmPNNlA{QDF|NkG=
human HT-3 cell NYnafWlHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHzDVI5KdmirYnn0bY9vKG:oIHj1cYFvKEiWLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc{OTN2IN88US=> NYnQd5RCW0GQR1XS
human LNCAP cells MlXxVJJwdGmoZYLheIlwdiCjc4PhfS=> MoPyN{Bl[Xm| M3ywXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiMzDkZZl{NCCLQ{WwQVAvPzN{NzFOwG0> M4XLblI3ODR4M{Gz
human PC3 cells MlG5SpVv[3Srb36gZZN{[Xl? NUPyNpZjTGm|cHzhZ4Vu\W62IH;mJHs{UF2UMUi4NUBnem:vIHHu[JJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIGDDN{Bk\WyuczygSWM2OD12LkOg{txO NEnDTWQzPTV7MUC2Oi=>
human 22Rv1 cells MlnmSpVv[3Srb36gZZN{[Xl? MnLNN{Bl[Xm| NGrsRYFCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHHu[JJw\2WwIILlZ4VxfG:{IFi4O|R[KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCqdX3hckAzOlK4MTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKESKVD3pcoR2[2WmIHPlcIwh\3Kxd4ToJIFnfGW{IEOg[IF6eyCkeTDXV3QuQCCjc4PhfUwhUUN3ME20MlYh|ryP NGmyUlAzPDlyMEW4PC=>
human CCF-STTG1 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3TMcWlvcGmkaYTpc44hd2ZiaIXtZY4hS0OILWPUWGcyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD12LkmyPVI6KM7:TR?= Mnz6V2FPT0WU
human SCC-25 cell NV7uVFhKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlfPTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvMkWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlA5PjV4IN88US=> NGX2SXZUSU6JRWK=
human MKN45 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXXTVJVXUW6qaXLpeIlwdiCxZjDoeY1idiCPS160OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvQTZyNTFOwG0> NGXHVWRUSU6JRWK=
human ES5 cell NGnQfYxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4XRO2lvcGmkaYTpc44hd2ZiaIXtZY4hTVN3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OD62NVE2PCEQvF2= NIS0cYdUSU6JRWK=
human SK-MEL-3 cell NEO3U2VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlKzTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjB7NkSg{txO NYPFeXVbW0GQR1XS
human PC-3 cell NXXGUGNyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mme4TY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNlc6OSEQvF2= M3HTfnNCVkeHUh?=
human NOS-1 cell M2HXTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;2XHZ{UW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjJ7MUeg{txO M2rvN3NCVkeHUh?=
human LB1047-RCC cell MoPGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH:yS|lKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj6yOVMh|ryP MXrTRW5ITVJ?
human CAMA-1 cell NYTQW4JWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVjFOoFnUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|OUK2JO69VQ>? M2D2VHNCVkeHUh?=
human SAS cell NFH3c2VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWLwTnFtUW6qaXLpeIlwdiCxZjDoeY1idiCVQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4{ODhzIN88US=> NXji[JliW0GQR1XS
human NCI-H2228 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYrJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkKyPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{Njd3M{Gg{txO NUPu[HpoW0GQR1XS
human NCI-H187 cell MluxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmfKTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG4O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3NjZ4MU[g{txO MnvPV2FPT0WU
human BFTC-905 cell NXPqN3k2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVrucXYzUW6qaXLpeIlwdiCxZjDoeY1idiCERmTDMVkxPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF5LkS4OVch|ryP M{e2XHNCVkeHUh?=
human G-361 cell M4XhVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV:0d3l5UW6qaXLpeIlwdiCxZjDoeY1idiCJLUO2NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE4Njh{NjFOwG0> NGXsc4tUSU6JRWK=
human DU145 cells MV;DfZRwfG:6aXRCpIF{e2G7 MmDNO|IhcA>? MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBGWmGucHjhMYRm\mmlaXXueEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEWUYnX0ZUBie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE5KM7:TR?= Ml:wV2FPT0WU
human SW780 cell NITCOWhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;6OWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfS=> NYHtNIdPW0GQR1XS
human BB49-HNC cell NV3FRldqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVgvQTV|MjFOwG0> NEjyZo5USU6JRWK=
human KALS-1 cell M3v5SWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlrsTY5pcWKrdHnvckBw\iCqdX3hckBMSUyVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU43PjN3IN88US=> NV\BUIVWW0GQR1XS
human AU565 cell NEPrbXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmGzTY5pcWKrdHnvckBw\iCqdX3hckBCXTV4NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5Mlc1ODJizszN MWPTRW5ITVJ?
human NCI-H2087 cell M2H0Nmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIDTU2RKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJzLkC1PVEh|ryP NHP3dXBUSU6JRWK=
human RVH-421 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{jUdGlvcGmkaYTpc44hd2ZiaIXtZY4hWl[KLUSyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjV5OUWg{txO NYnXeJJKW0GQR1XS
human SK-CO-1 cell NHrwcVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV64OXpTUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3DU{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwOEi3NkDPxE1? NV;uS|Z[W0GQR1XS
human KU-19-19 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4TtWWlvcGmkaYTpc44hd2ZiaIXtZY4hU1VvMUmtNVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOi5yMkSyJO69VQ>? Mkm1V2FPT0WU
human NB6 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF22XYJKdmirYnn0bY9vKG:oIHj1cYFvKE6ENjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlkyOzVizszN NEXSR2pUSU6JRWK=
human RO82-W-1 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoDxTY5pcWKrdHnvckBw\iCqdX3hckBTVzh{LWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjF|MUig{txO MVXTRW5ITVJ?
human LNCAP cells MmHoR5l1d3SxeHnjxsBie3OjeR?= MYCyJIRigXN? M3LzOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxPS0GSIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFIh\GG7czDifUBk\WyuIHPveY51cW6pIH3leIhw\CxiSVO1NF0zOy55OTFOwG0> MV[yN|czPzB2NB?=
human CTB-1 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWHobWhyUW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1NjV3M{[g{txO MXvTRW5ITVJ?
human SW48 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1nYeGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d2ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlY2PDZizszN MmLJV2FPT0WU
human TCCSUP cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mo[wTY5pcWKrdHnvckBw\iCqdX3hckBVS0OVVWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE44OjN{IN88US=> NYDjVmpQW0GQR1XS
human DK-MG cell NIDUSVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkfTTY5pcWKrdHnvckBw\iCqdX3hckBFUy2PRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0Mlg6OTdizszN NYPveW9PW0GQR1XS
human ST486 cell NVzw[4I5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFfk[HFKdmirYnn0bY9vKG:oIHj1cYFvKFOWNEi2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvPzR4NDFOwG0> Ml\NV2FPT0WU
human H4 cell NYL0OoNlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlK3TY5pcWKrdHnvckBw\iCqdX3hckBJPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ4Lkm0OVgh|ryP NF;1e2dUSU6JRWK=
human SBC-1 cell MmjXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXrJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkiuN|UxPyEQvF2= M2mwPHNCVkeHUh?=
human CAS-1 cell NWPKNmc6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUXUS4VSUW6qaXLpeIlwdiCxZjDoeY1idiCFQWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5NjZ{OUSg{txO Ml;CV2FPT0WU
human OAW-42 cell NUfXN41qT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3XKZ2lvcGmkaYTpc44hd2ZiaIXtZY4hV0GZLUSyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzF7NTFOwG0> NFnWO3RUSU6JRWK=
human HCC1954 cell NVvqUVlGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXLEdm9xUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxPVU1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjhwN{WyOUDPxE1? NFfYNpVUSU6JRWK=
human MDA-MB-453 cell NUjDdZJnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnadldKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk01PTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{OT65NFch|ryP MYnTRW5ITVJ?
human MCF7 cell M1i4VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4OwWGlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO5MlMxOSEQvF2= NWrKS2ZyW0GQR1XS
human PC3 cells M4jV[2Z2dmO2aX;uJIF{e2G7 NEPrVIEyODElgJFOwG0> NHjEenA1QCCq MnfQTY5pcWKrdHnvckBw\iCjY4TpckBj[XOnZDDwd4V2\G:yb3TpZUBnd3KvYYTpc44hcW5iYX7kdo9o\W5vZHXw[Y5l\W62IHj1cYFvKFCFMzDj[YxteyCjdDCxNFAhfU1iYX\0[ZIhPDhiaILzJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJI1q[3Kxc3PvdJkh[XO|YYm= MWSyNlY4Ojl6NB?=
human PC3 cells MXLGeY5kfGmxbjDhd5NigQ>? NU\GTGo2OC5zLUGg{txO MkC4RYdwdmm|dDDhZ5Rqfmm2eTDheEBidmS{b3flckBz\WOncITvdkBYPzRzQzDteZRidnRiZYjwdoV{e2WmIHnuJIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{B{fGmvdXzheIlwdiCxZjDy[YNmeHSxcjD0doFve2GldHn2ZZRqd25iYYSgNE4yKHSxIEGgeW0h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 M2fSS|IzOTd3Nkm0

... 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)
Water Insoluble
Ethanol '5 mg/mL

* 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 N/A
Smiles CC(CS(=O)(=O)C1=CC=C(C=C1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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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 SDS / 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 SDS / 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
NCT04573231 Recruiting Drug: 18F-DCFPyL Breast Cancer|HER2-negative Breast Cancer|Metastatic Breast Cancer University of Wisconsin Madison May 24 2021 Phase 2
NCT04443062 Recruiting Drug: 177Lu-PSMA-617 Prostate Cancer Radboud University|Prostaatkankerstichting|Advanced Accelerator Applications July 20 2020 Phase 2
NCT02910050 Unknown status Drug: Bicalutamide|Drug: Aromatase Inhibitor Breast Cancer Xu fei|Sun Yat-sen University January 2016 Phase 2
NCT02614859 Active not 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

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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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID