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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  • 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.

    (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.

  • 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.

    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. 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 NFPjT|ZHfW6ldHnvckBie3OjeR?= MmTMSIl{eGyjY3Xt[Y51KG:oIGuzTH1TOTh6MTDmdo9uKEGUIHnuJIh2dWGwIF3ERU1OSi12NUOgZ4VtdHNuIFXDOVA:OzFibl2= MX[yN|cyOzV4Nx?=
LNCaP cells NGfuTVZHfW6ldHnvckBie3OjeR?= NXPVSWZnUW6qaXLpeIlwdiCxZjDbN2heNUSKVDDibY5lcW6pIITvJHQ5PzeDIHHu[JJw\2WwIILlZ4VxfG:{IH;mJGxPS2GSIHPlcIx{NCCNaU2zOUBvVQ>? NIr6[m4yPTZyM{m2NC=>
Freestyle293F cells NInSRVNHfW6ldHnvckBie3OjeR?= MWnJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCDbnTyc4dmdiC{ZXPldJRweiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDGdoVme3S7bHWyPVNHKGOnbHzzMEBKSzVyPUCuNFU1KM7:TR?= MWSyN|E6QTR5Nx?=
HEK293 cells Mn32SpVv[3Srb36gZZN{[Xl? NY[zSmdKOyCq NWm4Wo5yTGm|cHzhZ4Vu\W62IH;mJHsyPy2jbIDoZU1u\XSqeXytN2hedWmkb3zldo9v\SCocn;tJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZYZ1\XJiMzDodpMtKEmFNUC9OVQhdk1? MoTDNlI{QTFyM{O=
MDA453 cells M1nKbmZ2dmO2aX;uJIF{e2G7 NU\HdnRUTGm|cHzhZ4Vu\W62IH;mJHs{UF2GSGSg[pJwdSCqdX3hckBidmS{b3flckBz\WOncITvdkBqdiCPRFG0OVMh[2WubIOsJGtqRTZ2IH7N NUDIS5JROTh{OUG2OFQ>
human MDA-MB-453 cells MmDRSpVv[3Srb36gZZN{[Xl? NUnHc2dXTGm|cHzhZ4Vu\W62IH;mJHs{UF2GSGSg[pJwdSCDUjDpckBpfW2jbjDNSGEuVUJvNEWzJINmdGy|LDDJR|UxRTZ2IH7N M4fZOVIxPTh2NkGw
COS1 cells MlzISpVv[3Srb36gZZN{[Xl? M1HxNmFvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBxW0d3LYTh[4dm\CCqdX3hckBidmS{b3flckBz\WOncITvdkBmgHC{ZYPz[YQhcW5iQ1;TNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icnXj[ZB1d3JvbXXkbYF1\WRidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGK7IFHSMZJm\3WuYYTl[EBz[XRicILvZoF{cW5icILvcY91\XJiZoLh[41mdnRiZILpeoVvKG[rcnXmcJkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCjc4PhfUwhUUN3ME2wMlA5PjlizszN NVzZdmZKOjV4NE[2OFk>
HeLa cells M{LOZ2Z2dmO2aX;uJIF{e2G7 MVvBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiZHnofYRzd3Snc4Tvd5Rmem:wZTDpcoR2[2WmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCkeTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUCuNVQh|ryP MonUNVc5ODR{Mkm=
CV1 cells MoPrSpVv[3Srb36gZZN{[Xl? M1r2RmJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEOYMTDj[YxteyxiS3m9NE4yPTFizszN MWixO|I2Pzh|OB?=
monkey COS7 cells NUjrV4d7TnWwY4Tpc44h[XO|YYm= NXLaOItTSmmwZHnu[{Bi\m[rbnn0fUB1dyCqdX3hckBidmS{b3flckBz\WOncITvdkBmgHC{ZYPz[YQhcW5ibX;ub4V6KEORU{egZ4VtdHNiYomge4hwdGViY3XscEBjcW6maX7nJIF{e2G7LDDLbV0xNjF3MTFOwG0> NVLzTFZuOTh2NEK5NVI>
COS7 cells NEW5[|BHfW6ldHnvckBie3OjeR?= MWXB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IGe3OFFEKG23dHHueEBmgHC{ZYPz[YQhcW5iQ1;TO{Bk\WyuczDhd5Nme3OnZDDhd{BtfWOrZnXyZZNmKGGldHn2bZR6KGGodHXyJFI1KGi{czDifUBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvOThizszN MWGyNlA6PDJ5OR?=
CHO-K1 cells MonTSpVv[3Srb36gZZN{[Xl? NVr1O2FLOiCq NWHUbIJ2TGm|cHzhZ4Vu\W62IH;mJHs{UF2vaXLvcIVzd26nIH\yc40hcHWvYX6gRXIh\XiycnXzd4VlKGmwIFPIU{1MOSClZXzsd{Bi\nSncjCyJIhzeyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwQVAvOiEQvF2= NYXOTYFnOjB|OEGzOlE>
human HT-3 cell MmPhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MluzTY5pcWKrdHnvckBw\iCqdX3hckBJXC1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63N|E{PCEQvF2= MV\TRW5ITVJ?
human LNCAP cells MnnMVJJwdGmoZYLheIlwdiCjc4PhfS=> MlLDN{Bl[Xm| NYTnZZNUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNuIFnDOVA:OC55M{K3JO69VQ>? NWHiNmNNOjZyNE[zNVM>
human PC3 cells NECybJdHfW6ldHnvckBie3OjeR?= M2HieGRqe3CuYXPlcYVvfCCxZjDbN2heWjF6OEGg[pJwdSCjbnTyc4dmdiC{ZXPldJRweiCrbjDoeY1idiCSQ{OgZ4VtdHNuIFXDOVA:PC5|IN88US=> NFfxOWYzPTV7MUC2Oi=>
human 22Rv1 cells NW\Ic2hqTnWwY4Tpc44h[XO|YYm= NUfhfXpROyCmYYnz NWXTOnhbSW62YXfvcol{fCCjY4Tpeol1gSCjdDDhcoRzd2enbjDy[YNmeHSxcjDIPFc1YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hOjKUdkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCGSGStbY5lfWOnZDDj[YxtKGe{b4f0bEBi\nSncjCzJIRigXNiYomgW3NVNThiYYPzZZktKEmFNUC9OE43KM7:TR?= NHzRNmEzPDlyMEW4PC=>
human CCF-STTG1 cell NIrmco9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGNETi2VVGTHNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:PC57MkmyPUDPxE1? MlrRV2FPT0WU
human SCC-25 cell M1f0emdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKGi3bXHuJHNESy1{NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNFg3PTZizszN NWnDVpo6W0GQR1XS
human MKN45 cell Ml60S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX\RWFB7UW6qaXLpeIlwdiCxZjDoeY1idiCPS160OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvQTZyNTFOwG0> NV3vNJl3W0GQR1XS
human ES5 cell MlrIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4DadWlvcGmkaYTpc44hd2ZiaIXtZY4hTVN3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OD62NVE2PCEQvF2= MX7TRW5ITVJ?
human SK-MEL-3 cell MmnsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHfFWFlKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBwMEm2OEDPxE1? MV\TRW5ITVJ?
human PC-3 cell M4nvVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvJe3RKdmirYnn0bY9vKG:oIHj1cYFvKFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE4zPzlzIN88US=> MXLTRW5ITVJ?
human NOS-1 cell NYfOeoc1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWPV[XFyUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjJ7MUeg{txO M2e3ZnNCVkeHUh?=
human LB1047-RCC cell MlniS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFfjU4hKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj6yOVMh|ryP MUHTRW5ITVJ?
human CAMA-1 cell M3\ZSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoXtTY5pcWKrdHnvckBw\iCqdX3hckBESU2DLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk4{QTJ4IN88US=> NVPvS5VIW0GQR1XS
human SAS cell NWHXT3h2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\wZWRRUW6qaXLpeIlwdiCxZjDoeY1idiCVQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4{ODhzIN88US=> MoPUV2FPT0WU
human NCI-H2228 cell M13qcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGnDR2xKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlIzQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|Lke1N|Eh|ryP MnLWV2FPT0WU
human NCI-H187 cell M37WN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkjuTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG4O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3NjZ4MU[g{txO MXjTRW5ITVJ?
human BFTC-905 cell NYDjOlg{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXfyOG9xUW6qaXLpeIlwdiCxZjDoeY1idiCERmTDMVkxPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF5LkS4OVch|ryP MY\TRW5ITVJ?
human G-361 cell NYjlSmNJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYrJcohq[mm2aX;uJI9nKGi3bXHuJGcuOzZzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUeuPFI3KM7:TR?= NXnGUFNpW0GQR1XS
human DU145 cells NF7PPFFEgXSxdH;4bYPDqGG|c3H5 NXTVSVFqPzJiaB?= NH\xNItEgXSxdH;4bYNqfHliYXfhbY5{fCCHUnHsdIhiNWSnZnnjbYVvfCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFXSZoV1[SCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTF6IN88US=> MWjTRW5ITVJ?
human SW780 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mo\HTY5pcWKrdHnvckBw\iCqdX3hckBUXzd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5 M3jrNnNCVkeHUh?=
human BB49-HNC cell NFPCZXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEPJS2FKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwOUWzNkDPxE1? NH;RfWpUSU6JRWK=
human KALS-1 cell NFSzVG1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn3NTY5pcWKrdHnvckBw\iCqdX3hckBMSUyVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU43PjN3IN88US=> MoXCV2FPT0WU
human AU565 cell M{XSdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1i4c2lvcGmkaYTpc44hd2ZiaIXtZY4hSVV3NkWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU44PDB{IN88US=> MorIV2FPT0WU
human NCI-H2087 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFm0S5VKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJzLkC1PVEh|ryP MoH3V2FPT0WU
human RVH-421 cell M17RSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXfKS2tNUW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwNUe5OUDPxE1? MlzSV2FPT0WU
human SK-CO-1 cell M{PvN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnzlTY5pcWKrdHnvckBw\iCqdX3hckBUUy2FTz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvQDh5MjFOwG0> MV7TRW5ITVJ?
human KU-19-19 cell M3TPdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnnsTY5pcWKrdHnvckBw\iCqdX3hckBMXS1zOT2xPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIzNjB{NEKg{txO MVLTRW5ITVJ?
human NB6 cell NYTwfJBLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJG5DPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ{LkmxN|Uh|ryP MXjTRW5ITVJ?
human RO82-W-1 cell NVLSN|cxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWe2XXNSUW6qaXLpeIlwdiCxZjDoeY1idiCUT{iyMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ|LkGzNVgh|ryP NHHtWY5USU6JRWK=
human LNCAP cells MlG2R5l1d3SxeHnjxsBie3OjeR?= MoHBNkBl[Xm| NEnqPXlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkAzKGSjeYOgZpkh[2WubDDjc5VvfGmwZzDt[ZRpd2RuIFnDOVA:OjNwN{mg{txO NGXFTFczOzd{N{C0OC=>
human CTB-1 cell M4HJS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuOVU{PiEQvF2= M3;MOXNCVkeHUh?=
human SW48 cell NH23bJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYjBUoVMUW6qaXLpeIlwdiCxZjDoeY1idiCVV{S4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPjV2NjFOwG0> NHywTIVUSU6JRWK=
human TCCSUP cell NUn3PIl4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlLsTY5pcWKrdHnvckBw\iCqdX3hckBVS0OVVWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE44OjN{IN88US=> NIjDUIZUSU6JRWK=
human DK-MG cell NHy0ZoNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmfnTY5pcWKrdHnvckBw\iCqdX3hckBFUy2PRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0Mlg6OTdizszN NW\Fe25{W0GQR1XS
human ST486 cell M3zBcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWPJcohq[mm2aX;uJI9nKGi3bXHuJHNVPDh4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkWuO|Q3PCEQvF2= NGD5OnRUSU6JRWK=
human H4 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFvDeZhKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mk[uPVQ2QCEQvF2= NV7TNHJZW0GQR1XS
human SBC-1 cell M2XVUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUXMWHNYUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5NjN3MEeg{txO MX3TRW5ITVJ?
human CAS-1 cell M2mwOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFPsZ|FKdmirYnn0bY9vKG:oIHj1cYFvKEODUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPjJ7NDFOwG0> MmDLV2FPT0WU
human OAW-42 cell M4nuOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4LKTGlvcGmkaYTpc44hd2ZiaIXtZY4hV0GZLUSyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzF7NTFOwG0> NWPiSG9DW0GQR1XS
human HCC1954 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzF7NUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE44PTJ3IN88US=> M32wSnNCVkeHUh?=
human MDA-MB-453 cell M{\KOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20OVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQS57MEeg{txO NWXwVHZWW0GQR1XS
human MCF7 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYrESnJ1UW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvOzBzIN88US=> NH\Dd4dUSU6JRWK=
human PC3 cells M3XJeWZ2dmO2aX;uJIF{e2G7 NUfodldUOTBy45EA{txO MWe0PEBp M4TxemlvcGmkaYTpc44hd2ZiYXP0bY4h[mG|ZXSgdJNmfWSxcH;kbYEh\m:{bXH0bY9vKGmwIHHu[JJw\2WwLXTldIVv\GWwdDDoeY1idiCSQ{OgZ4VtdHNiYYSgNVAxKHWPIHHmeIVzKDR6IHjyd{BjgSCGQWDJJJN1[WmwaX7nJIJie2WmIH\seY9z\XOlZX7j[UBucWO{b4Pjc5B6KGG|c3H5 M2\qVlIzPjd{OUi0
human PC3 cells NF;LUFBHfW6ldHnvckBie3OjeR?= MYewMlEuOSEQvF2= MVrB[49vcXO2IHHjeIl3cXS7IHH0JIFv\HKxZ3XuJJJm[2WydH;yJHc4PDGFIH31eIFvfCCneIDy[ZN{\WRiaX6gbJVu[W5iUFOzJINmdGy|IHHzd4V{e2WmIHHzJJN1cW23bHH0bY9vKG:oIILlZ4VxfG:{IITyZY5{[WO2aY\heIlwdiCjdDCwMlEhfG9iMTD1UUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MUeyNlE4PTZ7NB?=

... 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]
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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
  • 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
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
NCT03043807 Not yet recruiting Prostate Cancer Sidney Kimmel Comprehensive Cancer Center February 2017 Phase 2
NCT02716974 Recruiting Prostate Cancer Sidney Kimmel Comprehensive Cancer Center June 2016 Phase 2
NCT02582749 Recruiting Prostate Cancer|Bone Metastases|Prostate Neoplasms Ajjai Alva, MD|Hoosier Cancer Research Network|Bayer Healthcare Pharmaceuticals, Inc./Bayer Schering Pharma April 2016 Phase 2
NCT02742675 Recruiting Prostate Cancer Fudan University March 2016 Phase 2
NCT02697032 Recruiting Breast Cancer University Medical Center Groningen February 2016 Phase 2
NCT02910050 Recruiting Breast Cancer Xu fei|Sun Yat-sen University January 2016 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