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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In DMSO USD 109 In stock
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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 NXnQNlNNTnWwY4Tpc44h[XO|YYm= M3Ls[WRqe3CuYXPlcYVvfCCxZjDbN2heWjF6OEGg[pJwdSCDUjDpckBpfW2jbjDNSGEuVUJvNEWzJINmdGy|LDDFR|UxRTNzIH7N MorJNlM4OTN3Nke=
LNCaP cells MnjzSpVv[3Srb36gZZN{[Xl? NYXufXF6UW6qaXLpeIlwdiCxZjDbN2heNUSKVDDibY5lcW6pIITvJHQ5PzeDIHHu[JJw\2WwIILlZ4VxfG:{IH;mJGxPS2GSIHPlcIx{NCCNaU2zOUBvVQ>? MWqxOVYxOzl4MB?=
Freestyle293F cells MVjGeY5kfGmxbjDhd5NigQ>? Mlu1TY5pcWKrdHnvckBw\iC5aXzkJJR6eGViQX7kdo9o\W5icnXj[ZB1d3JiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gSpJm\XO2eXzlNlk{TiClZXzsd{whUUN3ME2wMlA2PCEQvF2= MljrNlMyQTl2N{e=
HEK293 cells MWDGeY5kfGmxbjDhd5NigQ>? MX2zJIg> MkPSSIl{eGyjY3Xt[Y51KG:oIGuxO{1idHCqYT3t[ZRpgWxvM1jdcYljd2yncn;u[UBnem:vIHHu[JJw\2WwIILlZ4VxfG:{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOyCqcoOsJGlEPTB;NUSgcm0> MVuyNlM6OTB|Mx?=
MDA453 cells NVn1SYY3TnWwY4Tpc44h[XO|YYm= NXX4b4lITGm|cHzhZ4Vu\W62IH;mJHs{UF2GSGSg[pJwdSCqdX3hckBidmS{b3flckBz\WOncITvdkBqdiCPRFG0OVMh[2WubIOsJGtqRTZ2IH7N M4jqSlE5OjlzNkS0
human MDA-MB-453 cells MUXGeY5kfGmxbjDhd5NigQ>? NIWzNZNFcXOybHHj[Y1mdnRib3[gX|NJZUSKVDDmdo9uKEGUIHnuJIh2dWGwIF3ERU1OSi12NUOgZ4VtdHNuIFnDOVA:PjRibl2= NIDVeHozODV6NE[xNC=>
COS1 cells Mmr4SpVv[3Srb36gZZN{[Xl? MnfCRY51[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= MmjTNlU3PDZ4NEm=
HeLa cells MnPUSpVv[3Srb36gZZN{[Xl? NVS3OYx4SW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCjbnTyc4dmdiC{ZXPldJRweiCneIDy[ZN{\WRiaX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIRqcHmmcn;0[ZN1d3O2ZYLvcoUhcW6mdXPl[EB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgZpkhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF0xNjF2IN88US=> M4q5blE4QDB2MkK5
CV1 cells MnHDSpVv[3Srb36gZZN{[Xl? M4nLc2JqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEOYMTDj[YxteyxiS3m9NE4yPTFizszN NYLPTXpPOTd{NUe4N|g>
monkey COS7 cells MUTGeY5kfGmxbjDhd5NigQ>? NVT4[4lHSmmwZHnu[{Bi\m[rbnn0fUB1dyCqdX3hckBidmS{b3flckBz\WOncITvdkBmgHC{ZYPz[YQhcW5ibX;ub4V6KEORU{egZ4VtdHNiYomge4hwdGViY3XscEBjcW6maX7nJIF{e2G7LDDLbV0xNjF3MTFOwG0> NY\xcIFGOTh2NEK5NVI>
COS7 cells M{TPOmZ2dmO2aX;uJIF{e2G7 NV\4RoVDSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBidmS{b3flckBz\WOncITvdkBYPzRzQzDteZRidnRiZYjwdoV{e2WmIHnuJGNQWzdiY3XscJMh[XO|ZYPz[YQh[XNibIXjbYZmemG|ZTDhZ5Rqfmm2eTDh[pRmeiB{NDDodpMh[nlicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkG4JO69VQ>? NInNOYYzOjB7NEK3PS=>
CHO-K1 cells MmnLSpVv[3Srb36gZZN{[Xl? MVOyJIg> MnzwSIl{eGyjY3Xt[Y51KG:oIGuzTH1ucWKxbHXyc45mKG[{b32gbJVu[W5iQWKg[ZhxemW|c3XkJIlvKEOKTz3LNUBk\WyuczDh[pRmeiB{IHjyd{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyPUCuNkDPxE1? MWOyNFM5OTN4MR?=
human HT-3 cell MnPXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF7mW|FKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc{OTN2IN88US=> MkPlV2FPT0WU
human LNCAP cells NIT0XJRRem:uaX\ldoF1cW:wIHHzd4F6 Mn\IN{Bl[Xm| MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{whUUN3ME2wMlc{OjdizszN MVGyOlA1PjNzMx?=
human PC3 cells MnHVSpVv[3Srb36gZZN{[Xl? NEHJTVNFcXOybHHj[Y1mdnRib3[gX|NJZVJzOEixJIZzd21iYX7kdo9o\W5icnXj[ZB1d3JiaX6gbJVu[W5iUFOzJINmdGy|LDDFR|UxRTRwMzFOwG0> NFi5WY8zPTV7MUC2Oi=>
human 22Rv1 cells MYLGeY5kfGmxbjDhd5NigQ>? NGTPfVk{KGSjeYO= NXvU[nlJSW62YXfvcol{fCCjY4Tpeol1gSCjdDDhcoRzd2enbjDy[YNmeHSxcjDIPFc1YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hOjKUdkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCGSGStbY5lfWOnZDDj[YxtKGe{b4f0bEBi\nSncjCzJIRigXNiYomgW3NVNThiYYPzZZktKEmFNUC9OE43KM7:TR?= NWHrbVI6OjR7MEC1PFg>
human CCF-STTG1 cell MnjIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYXJcohq[mm2aX;uJI9nKGi3bXHuJGNETi2VVGTHNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:PC57MkmyPUDPxE1? MX3TRW5ITVJ?
human SCC-25 cell NGrZW5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUnJcohq[mm2aX;uJI9nKGi3bXHuJHNESy1{NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNFg3PTZizszN Ml62V2FPT0WU
human MKN45 cell NFzHRVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3H6PGlvcGmkaYTpc44hd2ZiaIXtZY4hVUuQNEWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Mlk3ODVizszN M3i4c3NCVkeHUh?=
human ES5 cell NIDiZlNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NELDOZhKdmirYnn0bY9vKG:oIHj1cYFvKEWVNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOlEyPTRizszN MnvIV2FPT0WU
human SK-MEL-3 cell M3OxXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUG4fnNKUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFyLkC5OlQh|ryP MofSV2FPT0WU
human PC-3 cell NVq2TndzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV7ue2VZUW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvOjd7MTFOwG0> MV7TRW5ITVJ?
human NOS-1 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWi1NnlbUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjJ7MUeg{txO NUO2Soc1W0GQR1XS
human LB1047-RCC cell NIXJ[nFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWW0O|ZiUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuNlU{KM7:TR?= MmKyV2FPT0WU
human CAMA-1 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfHZZFKdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjN7Mk[g{txO NXXrOIJ4W0GQR1XS
human SAS cell MmjOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M33xSGlvcGmkaYTpc44hd2ZiaIXtZY4hW0GVIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuN|A5OSEQvF2= MUjTRW5ITVJ?
human NCI-H2228 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHKXmFyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzOjhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz63OVMyKM7:TR?= MWnTRW5ITVJ?
human NCI-H187 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYLxb4ZXUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4Lk[2NVYh|ryP MYPTRW5ITVJ?
human BFTC-905 cell NF3ifoJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mk\HTY5pcWKrdHnvckBw\iCqdX3hckBDTlSFLUmwOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE4NjR6NUeg{txO MXnTRW5ITVJ?
human G-361 cell M{H3NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfMTY5pcWKrdHnvckBw\iCqdX3hckBINTN4MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG3MlgzPiEQvF2= NXfEWIJ1W0GQR1XS
human DU145 cells NHe2UVJEgXSxdH;4bYPDqGG|c3H5 NHj0d3g4OiCq M3[xcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEWUYXzwbIEu\GWoaXPp[Y51KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiRWLi[ZRiKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OThizszN NIPVfmtUSU6JRWK=
human SW780 cell NX23WmFYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVXJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= NGW2Xm1USU6JRWK=
human BB49-HNC cell NH;ZfphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2HTe2lvcGmkaYTpc44hd2ZiaIXtZY4hSkJ2OT3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQC57NUOyJO69VQ>? NHrLVVFUSU6JRWK=
human KALS-1 cell M3ja[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX;1PYpPUW6qaXLpeIlwdiCxZjDoeY1idiCNQVzTMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQS54NkO1JO69VQ>? NYHx[2lyW0GQR1XS
human AU565 cell MmGzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlzETY5pcWKrdHnvckBw\iCqdX3hckBCXTV4NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5Mlc1ODJizszN M2rlPXNCVkeHUh?=
human NCI-H2087 cell M334eWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkHBTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS5yNUmxJO69VQ>? NHLE[GxUSU6JRWK=
human RVH-421 cell MlflS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2noTGlvcGmkaYTpc44hd2ZiaIXtZY4hWl[KLUSyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjV5OUWg{txO MX7TRW5ITVJ?
human SK-CO-1 cell M{jTfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFjtO5ZKdmirYnn0bY9vKG:oIHj1cYFvKFONLVPPMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS56OEeyJO69VQ>? MUPTRW5ITVJ?
human KU-19-19 cell NGLDPG1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGtWNTF7LUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvODJ2MjFOwG0> NEOxPIVUSU6JRWK=
human NB6 cell M2TSOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEe0eG5KdmirYnn0bY9vKG:oIHj1cYFvKE6ENjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlkyOzVizszN MnTvV2FPT0WU
human RO82-W-1 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3rGRWlvcGmkaYTpc44hd2ZiaIXtZY4hWk96Mj3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOy5zM{G4JO69VQ>? MXTTRW5ITVJ?
human LNCAP cells NXvycWh5S3m2b4TvfIlkyqCjc4PhfS=> NHjwSJEzKGSjeYO= M{TENWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxPS0GSIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFIh\GG7czDifUBk\WyuIHPveY51cW6pIH3leIhw\CxiSVO1NF0zOy55OTFOwG0> NEGxc28zOzd{N{C0OC=>
human CTB-1 cell M1qwZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGrpV2dKdmirYnn0bY9vKG:oIHj1cYFvKEOWQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPTV|NjFOwG0> Moj3V2FPT0WU
human SW48 cell M1\VWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHHYNJBKdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE43PTR4IN88US=> NV\GRVVoW0GQR1XS
human TCCSUP cell NH3YR4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoqxTY5pcWKrdHnvckBw\iCqdX3hckBVS0OVVWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE44OjN{IN88US=> NVPQ[opQW0GQR1XS
human DK-MG cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXPpbnZWUW6qaXLpeIlwdiCxZjDoeY1idiCGSz3NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1Njh7MUeg{txO MkLNV2FPT0WU
human ST486 cell NHHJfHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3Txd2lvcGmkaYTpc44hd2ZiaIXtZY4hW1R2OE[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOU44PDZ2IN88US=> NF\1fFBUSU6JRWK=
human H4 cell NYL5OYRiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXrJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjZwOUS1PEDPxE1? NGDqbZBUSU6JRWK=
human SBC-1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4PVZmlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE4{PTB5IN88US=> M{PSNHNCVkeHUh?=
human CAS-1 cell NG\YPHFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVzKenZSUW6qaXLpeIlwdiCxZjDoeY1idiCFQWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5NjZ{OUSg{txO NUTy[ZpRW0GQR1XS
human OAW-42 cell NFfvcpJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKGi3bXHuJG9CXy12MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlcyQTVizszN NYT2O4JyW0GQR1XS
human HCC1954 cell NXzxOGFHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NELxVFhKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G5OVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQC55NUK1JO69VQ>? MYPTRW5ITVJ?
human MDA-MB-453 cell M{LVWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWrNd3NsUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuPDV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkmuPVA4KM7:TR?= NGmxS49USU6JRWK=
human MCF7 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEDwdFRKdmirYnn0bY9vKG:oIHj1cYFvKE2FRkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPU4{ODFizszN M2PXNnNCVkeHUh?=
human PC3 cells NYrvNGlHTnWwY4Tpc44h[XO|YYm= M1W3U|ExOOPCgN88US=> MWe0PEBp NGD5cZhKdmirYnn0bY9vKG:oIHHjeIlvKGKjc3XkJJB{\XWmb4Dv[IliKG[xcn3heIlwdiCrbjDhcoRzd2enbj3k[ZBmdmSnboSgbJVu[W5iUFOzJINmdGy|IHH0JFExOCC3TTDh[pRmeiB2ODDodpMh[nliRFHQTUB{fGGrbnnu[{Bj[XOnZDDmcJVwemW|Y3XuZ4UhdWmlcn;zZ49xgSCjc4PhfS=> MXiyNlY4Ojl6NB?=
human PC3 cells NEDlPHlHfW6ldHnvckBie3OjeR?= M2H6OlAvOS1zIN88US=> MXnB[49vcXO2IHHjeIl3cXS7IHH0JIFv\HKxZ3XuJJJm[2WydH;yJHc4PDGFIH31eIFvfCCneIDy[ZN{\WRiaX6gbJVu[W5iUFOzJINmdGy|IHHzd4V{e2WmIHHzJJN1cW23bHH0bY9vKG:oIILlZ4VxfG:{IITyZY5{[WO2aY\heIlwdiCjdDCwMlEhfG9iMTD1UUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= NWH3VW1ZOjJzN{W2PVQ>

... 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
NCT01664923 Completed Prostate Cancer Pfizer|Astellas Pharma Inc|Medivation Inc. August 7 2012 Phase 2
NCT03147196 Recruiting Stage I Prostate Adenocarcinoma|Stage II Prostate Adenocarcinoma Mayo Clinic|National Cancer Institute (NCI) June 27 2017 Phase 2
NCT01251861 Active not recruiting Recurrent Prostate Carcinoma|Stage I Prostate Cancer AJCC v7|Stage IIA Prostate Cancer AJCC v7|Stage IIB Prostate Cancer AJCC v7|Stage III Prostate Cancer AJCC v7 National Cancer Institute (NCI) December 23 2010 Phase 2
NCT00094328 Completed Puberty Precocious AstraZeneca November 22 2004 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 2018 Phase 2
NCT03055312 Recruiting Metastatic Triple Negative Breast Cancer Sun Yat-sen University December 2016 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID