Bicalutamide

For research use only.

Catalog No.S1190 Synonyms: ICI-176334

30 publications

Bicalutamide 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.

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Selleck's Bicalutamide has been cited by 30 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 MVTGeY5kfGmxbjDhd5NigQ>? NIjkVoVFcXOybHHj[Y1mdnRib3[gX|NJZVJzOEixJIZzd21iQWKgbY4hcHWvYX6gUWRCNU2ELUS1N{Bk\WyuczygSWM2OD1|MTDuUS=> NXLaO5Y5OjN5MUO1Olc>
LNCaP cells NX7mW41YTnWwY4Tpc44h[XO|YYm= MVjJcohq[mm2aX;uJI9nKFt|SG2tSGhVKGKrbnTpcochfG9iVEi3O2Eh[W6mcn;n[Y4hemWlZYD0c5Ihd2ZiTF7DZXAh[2WubIOsJGtqRTN3IH7N Mnj0NVU3ODN7NkC=
Freestyle293F cells NELJOXhHfW6ldHnvckBie3OjeR?= MnjGTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViQX7kdo9o\W5icnXj[ZB1d3JiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gSpJm\XO2eXzlNlk{TiClZXzsd{whUUN3ME2wMlA2PCEQvF2= MV2yN|E6QTR5Nx?=
HEK293 cells NYe2U2xDTnWwY4Tpc44h[XO|YYm= M{fsfFMhcA>? M3\ke2Rqe3CuYXPlcYVvfCCxZjDbNVcu[WyyaHGtcYV1cHmuLUPIYY1q[m:uZYLvcoUh\nKxbTDhcoRzd2enbjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHmeIVzKDNiaILzMEBKSzVyPUW0JI5O MnT3NlI{QTFyM{O=
MDA453 cells MXXGeY5kfGmxbjDhd5NigQ>? M1;kSWRqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgbY4hVUSDNEWzJINmdGy|LDDLbV03PCCwTR?= MlnGNVgzQTF4NES=
human MDA-MB-453 cells M{DPemZ2dmO2aX;uJIF{e2G7 MknxSIl{eGyjY3Xt[Y51KG:oIGuzTH1FUFRiZoLvcUBCWiCrbjDoeY1idiCPRFGtUWIuPDV|IHPlcIx{NCCLQ{WwQVY1KG6P MWiyNFU5PDZzMB?=
COS1 cells M1vMVmZ2dmO2aX;uJIF{e2G7 NXyxemNpSW62YXfvcol{fCCjY4Tpeol1gSCjZ3HpcpN1KHCVR{WteIFo\2WmIHj1cYFvKGGwZILv[4VvKHKnY3XweI9zKGW6cILld5Nm\CCrbjDDU3MyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDy[YNmeHSxcj3t[YRq[XSnZDD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliYomgRXIuemWpdXzheIVlKHKjdDDwdo9j[XOrbjDwdo9ud3SncjDmdoFodWWwdDDkdol3\W5iZnny[YZtgSCudXPp[oVz[XOnIILldI9zfGW{IHHzd4F6NCCLQ{WwQVAvODh4OTFOwG0> M4r4dFI2PjR4NkS5
HeLa cells MmezSpVv[3Srb36gZZN{[Xl? NXX0dlRtSW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCjbnTyc4dmdiC{ZXPldJRweiCneIDy[ZN{\WRiaX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIRqcHmmcn;0[ZN1d3O2ZYLvcoUhcW6mdXPl[EB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgZpkhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF0xNjF2IN88US=> MljtNVc5ODR{Mkm=
CV1 cells NUjHdpJ3TnWwY4Tpc44h[XO|YYm= MnS2Rolv\GmwZzDh[oZqdmm2eTD0c{BpfW2jbjDhcoRzd2enbjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hS1ZzIHPlcIx{NCCNaU2wMlE2OSEQvF2= MYGxO|I2Pzh|OB?=
monkey COS7 cells M3rPUmZ2dmO2aX;uJIF{e2G7 MnnqRolv\GmwZzDh[oZqdmm2eTD0c{BpfW2jbjDhcoRzd2enbjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hdW:wa3X5JGNQWzdiY3XscJMh[nlid3jvcIUh[2WubDDibY5lcW6pIHHzd4F6NCCNaU2wMlE2OSEQvF2= NYfqRlk6OTh2NEK5NVI>
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CHO-K1 cells NXHxfpRlTnWwY4Tpc44h[XO|YYm= NWXFWmE5OiCq NXTLW3FMTGm|cHzhZ4Vu\W62IH;mJHs{UF2vaXLvcIVzd26nIH\yc40hcHWvYX6gRXIh\XiycnXzd4VlKGmwIFPIU{1MOSClZXzsd{Bi\nSncjCyJIhzeyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwQVAvOiEQvF2= NV35ZYN7OjB|OEGzOlE>
human HT-3 cell NY\tXo13T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGrUeXJKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc{OTN2IN88US=> Mli0V2FPT0WU
human LNCAP cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 M4j6SlMh\GG7cx?= NIq5ZnZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyxiSVO1NF0xNjd|Mkeg{txO NEHGV4wzPjB2NkOxNy=>
human PC3 cells M4PXbmZ2dmO2aX;uJIF{e2G7 MmP6SIl{eGyjY3Xt[Y51KG:oIGuzTH1TOTh6MTDmdo9uKGGwZILv[4VvKHKnY3XweI9zKGmwIHj1cYFvKFCFMzDj[YxteyxiRVO1NF01NjNizszN NWH1To9TOjV3OUGwOlY>
human 22Rv1 cells NVnHc|FpTnWwY4Tpc44h[XO|YYm= MnXwN{Bl[Xm| M2TwdGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiYX7kdo9o\W5icnXj[ZB1d3JiSEi3OHkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKGi3bXHuJFIzWnZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTEiWLXnu[JVk\WRiY3XscEBoem:5dHigZYZ1\XJiMzDkZZl{KGK7IGfTWE05KGG|c3H5MEBKSzVyPUSuOkDPxE1? MmTZNlQ6ODB3OEi=
human CCF-STTG1 cell NYXCRXI4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3LtOmlvcGmkaYTpc44hd2ZiaIXtZY4hS0OILWPUWGcyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD12LkmyPVI6KM7:TR?= NX\Jc4hrW0GQR1XS
human SCC-25 cell NUnOSGQ1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWLJcohq[mm2aX;uJI9nKGi3bXHuJHNESy1{NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNFg3PTZizszN NHTCV|BUSU6JRWK=
human MKN45 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKGi3bXHuJG1MVjR3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj65OlA2KM7:TR?= NFnEfIpUSU6JRWK=
human ES5 cell M4rxfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWPPT2tkUW6qaXLpeIlwdiCxZjDoeY1idiCHU{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlYyOTV2IN88US=> M1HEenNCVkeHUh?=
human SK-MEL-3 cell NWn6ZVNZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2jORWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5yOU[0JO69VQ>? NWO1OploW0GQR1XS
human PC-3 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmPSTY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNlc6OSEQvF2= NVrsT4NzW0GQR1XS
human NOS-1 cell MmDlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX7vSnFHUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjJ7MUeg{txO MWLTRW5ITVJ?
human LB1047-RCC cell M{L0N2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzs[5A5UW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuNlU{KM7:TR?= M33LZ3NCVkeHUh?=
human CAMA-1 cell NIjOWXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJGNCVUFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlM6OjZizszN NXzhfYxQW0GQR1XS
human SAS cell NX7WfZV1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnSZo1KdmirYnn0bY9vKG:oIHj1cYFvKFODUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlMxQDFizszN NV3yUlNZW0GQR1XS
human NCI-H2228 cell MmTnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DNcGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNlI5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwN{WzNUDPxE1? MXnTRW5ITVJ?
human NCI-H187 cell M{Hq[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXHYTW53UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4Lk[2NVYh|ryP MXrTRW5ITVJ?
human BFTC-905 cell NE\TOVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvPDh3NzFOwG0> MoDNV2FPT0WU
human G-361 cell M2nTeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUPrVYU{UW6qaXLpeIlwdiCxZjDoeY1idiCJLUO2NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE4Njh{NjFOwG0> NHrkbIRUSU6JRWK=
human DU145 cells NIPVdmNEgXSxdH;4bYPDqGG|c3H5 MXy3NkBp M3m0[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEWUYXzwbIEu\GWoaXPp[Y51KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiRWLi[ZRiKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OThizszN NE\XPVFUSU6JRWK=
human SW780 cell MoLIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXPJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= M2HUSnNCVkeHUh?=
human BB49-HNC cell MkDWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFXRUZFKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwOUWzNkDPxE1? MVvTRW5ITVJ?
human KALS-1 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1LEOmlvcGmkaYTpc44hd2ZiaIXtZY4hU0GOUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPjZ|NTFOwG0> NH;QNpRUSU6JRWK=
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human NCI-H2087 cell NWDGU297T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlL1TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS5yNUmxJO69VQ>? MYfTRW5ITVJ?
human RVH-421 cell NHHHfnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXPnOZljUW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwNUe5OUDPxE1? Mn[0V2FPT0WU
human SK-CO-1 cell MkDVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M13hb2lvcGmkaYTpc44hd2ZiaIXtZY4hW0tvQ1:tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjh6N{Kg{txO MmX3V2FPT0WU
human KU-19-19 cell Mle4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUn6cm06UW6qaXLpeIlwdiCxZjDoeY1idiCNVT2xPU0yQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ{LkCyOFIh|ryP MnK1V2FPT0WU
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human RO82-W-1 cell NY\icph2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NE\RbZJKdmirYnn0bY9vKG:oIHj1cYFvKFKROEKtW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwMUOxPEDPxE1? MmfzV2FPT0WU
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human CTB-1 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{XXeWlvcGmkaYTpc44hd2ZiaIXtZY4hS1SELUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE42PTN4IN88US=> NEWyUllUSU6JRWK=
human SW48 cell NI\aUFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn\iTY5pcWKrdHnvckBw\iCqdX3hckBUXzR6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuOlU1PiEQvF2= MoLhV2FPT0WU
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human DK-MG cell NXrVVldsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2CxRmlvcGmkaYTpc44hd2ZiaIXtZY4hTEtvTVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE45QTF5IN88US=> NVfGS3cxW0GQR1XS
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human SBC-1 cell NYqxeHFYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIm2TFdKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvOzVyNzFOwG0> M{TmUHNCVkeHUh?=
human CAS-1 cell M4PjVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2izemlvcGmkaYTpc44hd2ZiaIXtZY4hS0GVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE43Ojl2IN88US=> NV3pTlkyW0GQR1XS
human OAW-42 cell MkjSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NITFXlVKdmirYnn0bY9vKG:oIHj1cYFvKE:DVz20NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5NjdzOUWg{txO M4rZZnNCVkeHUh?=
human HCC1954 cell M{W0eWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfBTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzOUW0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzV{NTFOwG0> Mk\TV2FPT0WU
human MDA-MB-453 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20OVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQS57MEeg{txO M1y3XHNCVkeHUh?=
human MCF7 cell NX\rOZN4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\4dmlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO5MlMxOSEQvF2= MVTTRW5ITVJ?
human PC3 cells MWnGeY5kfGmxbjDhd5NigQ>? M{e1[lExOOPCgN88US=> NXW2VpFzPDhiaB?= MYHJcohq[mm2aX;uJI9nKGGldHnuJIJie2WmIIDz[ZVld3CxZHnhJIZwem2jdHnvckBqdiCjbnTyc4dmdi2mZYDlcoRmdnRiaIXtZY4hWEN|IHPlcIx{KGG2IEGwNEB2VSCjZoTldkA1QCCqcoOgZpkhTEGSSTDzeIFqdmmwZzDiZZNm\CCobIXvdoV{[2WwY3WgcYlkem:|Y3;wfUBie3OjeR?= Ml7YNlI3PzJ7OES=
human PC3 cells M3fB[2Z2dmO2aX;uJIF{e2G7 M1i0V|AvOS1zIN88US=> MoTtRYdwdmm|dDDhZ5Rqfmm2eTDheEBidmS{b3flckBz\WOncITvdkBYPzRzQzDteZRidnRiZYjwdoV{e2WmIHnuJIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{B{fGmvdXzheIlwdiCxZjDy[YNmeHSxcjD0doFve2GldHn2ZZRqd25iYYSgNE4yKHSxIEGgeW0h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 MonyNlIyPzV4OUS=

... 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(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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Step 2: Enter the in vivo formulation ()
% 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
NCT04573231 Recruiting Drug: 18F-DCFPyL Breast Cancer|HER2-negative Breast Cancer|Metastatic Breast Cancer University of Wisconsin Madison December 2020 Phase 2
NCT04443062 Recruiting Drug: 177Lu-PSMA-I&T Prostate Cancer Radboud University|Prostaatkankerstichting 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

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