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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4 Customer Reviews

  • 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, 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 NHL0d3JHfW6ldHnvckBie3OjeR?= MV7EbZNxdGGlZX3lcpQhd2ZiW{PIYXIyQDhzIH\yc40hSVJiaX6gbJVu[W5iTVTBMW1DNTR3MzDj[YxteyxiRVO1NF0{OSCwTR?= NHHEfnAzOzdzM{W2Oy=>
LNCaP cells MlrhSpVv[3Srb36gZZN{[Xl? MWHJcohq[mm2aX;uJI9nKFt|SG2tSGhVKGKrbnTpcochfG9iVEi3O2Eh[W6mcn;n[Y4hemWlZYD0c5Ihd2ZiTF7DZXAh[2WubIOsJGtqRTN3IH7N M{S2OFE2PjB|OU[w
Freestyle293F cells MmPZSpVv[3Srb36gZZN{[Xl? MkDHTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViQX7kdo9o\W5icnXj[ZB1d3JiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gSpJm\XO2eXzlNlk{TiClZXzsd{whUUN3ME2wMlA2PCEQvF2= NYnwRnprOjNzOUm0O|c>
HEK293 cells NYLPWWhXTnWwY4Tpc44h[XO|YYm= M1nBU|MhcA>? NWXBO2Z1TGm|cHzhZ4Vu\W62IH;mJHsyPy2jbIDoZU1u\XSqeXytN2hedWmkb3zldo9v\SCocn;tJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZYZ1\XJiMzDodpMtKEmFNUC9OVQhdk1? MXmyNlM6OTB|Mx?=
MDA453 cells M4\5Z2Z2dmO2aX;uJIF{e2G7 NFv5bIxFcXOybHHj[Y1mdnRib3[gX|NJZUSKVDDmdo9uKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIlvKE2GQUS1N{Bk\WyuczygT4k:PjRibl2= NInsTXIyQDJ7MU[0OC=>
human MDA-MB-453 cells NVS2U5ZpTnWwY4Tpc44h[XO|YYm= MnTlSIl{eGyjY3Xt[Y51KG:oIGuzTH1FUFRiZoLvcUBCWiCrbjDoeY1idiCPRFGtUWIuPDV|IHPlcIx{NCCLQ{WwQVY1KG6P M1nXelIxPTh2NkGw
COS1 cells MUPGeY5kfGmxbjDhd5NigQ>? MmTURY51[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= NEC4d20zPTZ2Nk[0PS=>
HeLa cells MX;GeY5kfGmxbjDhd5NigQ>? M4HWbmFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDkbYh6\HKxdHXzeI9{fGW{b37lJIlv\HWlZXSgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHL5JJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NE4yPCEQvF2= MWSxO|gxPDJ{OR?=
CV1 cells NIPFeHJHfW6ldHnvckBie3OjeR?= MYnCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEXjFiY3XscJMtKEurPUCuNVUyKM7:TR?= M13yT|E4OjV5OEO4
monkey COS7 cells M{LFc2Z2dmO2aX;uJIF{e2G7 NHfaXHNDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCvb37r[ZkhS0:VNzDj[YxteyCkeTD3bI9t\SClZXzsJIJqdmSrbnegZZN{[XluIFvpQVAvOTVzIN88US=> MmfWNVg1PDJ7MUK=
COS7 cells MW\GeY5kfGmxbjDhd5NigQ>? MoXFRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDhcoRzd2enbjDy[YNmeHSxcjDXO|QySyCvdYThcpQh\XiycnXzd4VlKGmwIFPPV|ch[2WubIOgZZN{\XO|ZXSgZZMhdHWlaX\ldoF{\SCjY4Tpeol1gSCjZoTldkAzPCCqcoOgZpkhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjF6IN88US=> MVyyNlA6PDJ5OR?=
CHO-K1 cells MkPqSpVv[3Srb36gZZN{[Xl? M{PWVVIhcA>? NE[5XVhFcXOybHHj[Y1mdnRib3[gX|NJZW2rYn;s[ZJwdmViZoLvcUBpfW2jbjDBVkBmgHC{ZYPz[YQhcW5iQ1jPMWsyKGOnbHzzJIFnfGW{IEKgbJJ{KGK7IIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUC9NE4zKM7:TR?= MnP6NlA{QDF|NkG=
human HT-3 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGX0XWxKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc{OTN2IN88US=> M3HCXXNCVkeHUh?=
human LNCAP cells NGXsPVFRem:uaX\ldoF1cW:wIHHzd4F6 NYmzdGhzOyCmYYnz Mkj4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOTlPBVEBk\WyuczDh[pRmeiB|IHThfZMtKEmFNUC9NE44OzJ5IN88US=> MWiyOlA1PjNzMx?=
human PC3 cells NUnjVmhMTnWwY4Tpc44h[XO|YYm= NEDPU2VFcXOybHHj[Y1mdnRib3[gX|NJZVJzOEixJIZzd21iYX7kdo9o\W5icnXj[ZB1d3JiaX6gbJVu[W5iUFOzJINmdGy|LDDFR|UxRTRwMzFOwG0> MWOyOVU6OTB4Nh?=
human 22Rv1 cells MmmwSpVv[3Srb36gZZN{[Xl? NWjXU2hYOyCmYYnz NXX3[ItRSW62YXfvcol{fCCjY4Tpeol1gSCjdDDhcoRzd2enbjDy[YNmeHSxcjDIPFc1YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hOjKUdkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCGSGStbY5lfWOnZDDj[YxtKGe{b4f0bEBi\nSncjCzJIRigXNiYomgW3NVNThiYYPzZZktKEmFNUC9OE43KM7:TR?= NYnDcVNMOjR7MEC1PFg>
human CCF-STTG1 cell MnTrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUixZYtvUW6qaXLpeIlwdiCxZjDoeY1idiCFQ1[tV3RVTzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3Ojef-8kEBKSzVyPUSuPVI6OjlizszN M33JSXNCVkeHUh?=
human SCC-25 cell NI\QXXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUnJcohq[mm2aX;uJI9nKGi3bXHuJHNESy1{NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNFg3PTZizszN Mn7HV2FPT0WU
human MKN45 cell NELsVoVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHvGbHlKdmirYnn0bY9vKG:oIHj1cYFvKE2NTkS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok46PjB3IN88US=> NHTKcHlUSU6JRWK=
human ES5 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnCTY5pcWKrdHnvckBw\iCqdX3hckBGWzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16Lk[xNVU1KM7:TR?= M3nzbXNCVkeHUh?=
human SK-MEL-3 cell NYDWenlsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH\Zb3RKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBwMEm2OEDPxE1? NG\BfJlUSU6JRWK=
human PC-3 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH3lOmRKdmirYnn0bY9vKG:oIHj1cYFvKFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE4zPzlzIN88US=> NEXlcZBUSU6JRWK=
human NOS-1 cell NFqwbYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1KzR2lvcGmkaYTpc44hd2ZiaIXtZY4hVk:VLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU4zQTF5IN88US=> NFnRUVBUSU6JRWK=
human LB1047-RCC cell MoXtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkHzTY5pcWKrdHnvckBw\iCqdX3hckBNSjFyNEetVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwMkWzJO69VQ>? Mn\KV2FPT0WU
human CAMA-1 cell NY\yNHFLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoXHTY5pcWKrdHnvckBw\iCqdX3hckBESU2DLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk4{QTJ4IN88US=> NFnhd3hUSU6JRWK=
human SAS cell MnHkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MofkTY5pcWKrdHnvckBw\iCqdX3hckBUSVNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6zNFgyKM7:TR?= NXj6PGw5W0GQR1XS
human NCI-H2228 cell NGPzPFJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1XnfWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNlI5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwN{WzNUDPxE1? M13uNHNCVkeHUh?=
human NCI-H187 cell NVXGWXVpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlLUTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG4O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3NjZ4MU[g{txO MkjhV2FPT0WU
human BFTC-905 cell M1:3Omdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEXnT5JKdmirYnn0bY9vKG:oIHj1cYFvKEKIVFOtPVA2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTdwNEi1O{DPxE1? MkX0V2FPT0WU
human G-361 cell NYm4WnpbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmTWTY5pcWKrdHnvckBw\iCqdX3hckBINTN4MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG3MlgzPiEQvF2= MofhV2FPT0WU
human DU145 cells NYriSJpHS3m2b4TvfIlkyqCjc4PhfS=> MWO3NkBp MlrsR5l1d3SxeHnjbZR6KGGpYXnud5QhTVKjbIDoZU1l\W[rY3nlcpQhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCHUnLleIEh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yQCEQvF2= MknHV2FPT0WU
human SW780 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH\rUlZKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZk> NGLxXFRUSU6JRWK=
human BB49-HNC cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFu0UmJKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwOUWzNkDPxE1? NHf2S2tUSU6JRWK=
human KALS-1 cell MlLUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKGi3bXHuJGtCVFNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlY3OzVizszN MXzTRW5ITVJ?
human AU565 cell NVS3PIw6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NELXSpVKdmirYnn0bY9vKG:oIHj1cYFvKEGXNU[1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPzRyMjFOwG0> M{LncnNCVkeHUh?=
human NCI-H2087 cell MmHBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1K2PGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFg4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwMEW5NUDPxE1? NUfZWHlzW0GQR1XS
human RVH-421 cell MmLrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mo\LTY5pcWKrdHnvckBw\iCqdX3hckBTXkhvNEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTd7NTFOwG0> M2DlbnNCVkeHUh?=
human SK-CO-1 cell M1nofmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4r0bWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvQ1:tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjh6N{Kg{txO M3mycnNCVkeHUh?=
human KU-19-19 cell NH7mUnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3KxZ2lvcGmkaYTpc44hd2ZiaIXtZY4hU1VvMUmtNVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOi5yMkSyJO69VQ>? Mlj4V2FPT0WU
human NB6 cell NGXITWhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NE\DTG1KdmirYnn0bY9vKG:oIHj1cYFvKE6ENjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlkyOzVizszN MlLyV2FPT0WU
human RO82-W-1 cell NV:yNmlUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NI\jW5pKdmirYnn0bY9vKG:oIHj1cYFvKFKROEKtW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwMUOxPEDPxE1? M3LjcXNCVkeHUh?=
human LNCAP cells Ml61R5l1d3SxeHnjxsBie3OjeR?= M4nLR|Ih\GG7cx?= NF\KT2xEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkAzKGSjeYOgZpkh[2WubDDjc5VvfGmwZzDt[ZRpd2RuIFnDOVA:OjNwN{mg{txO MoLlNlM4OjdyNES=
human CTB-1 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuOVU{PiEQvF2= NHzFTHJUSU6JRWK=
human SW48 cell NFHHOZpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlLITY5pcWKrdHnvckBw\iCqdX3hckBUXzR6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSuOlU1PiEQvF2= MU\TRW5ITVJ?
human TCCSUP cell NFrzT4RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKGi3bXHuJHRES1OXUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlczOzJizszN NHzBRmNUSU6JRWK=
human DK-MG cell MlvLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;LTY5pcWKrdHnvckBw\iCqdX3hckBFUy2PRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0Mlg6OTdizszN Mn;pV2FPT0WU
human ST486 cell M4Pwb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIiwVJlKdmirYnn0bY9vKG:oIHj1cYFvKFOWNEi2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvPzR4NDFOwG0> NFuxVFFUSU6JRWK=
human H4 cell NU\jcXlUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjZwOUS1PEDPxE1? MXrTRW5ITVJ?
human SBC-1 cell Mk\4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGrvTZNKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvOzVyNzFOwG0> MmTzV2FPT0WU
human CAS-1 cell M{jSVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\M[GlvcGmkaYTpc44hd2ZiaIXtZY4hS0GVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE43Ojl2IN88US=> MmLLV2FPT0WU
human OAW-42 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4rq[mlvcGmkaYTpc44hd2ZiaIXtZY4hV0GZLUSyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPzF7NTFOwG0> NHL5SXpUSU6JRWK=
human HCC1954 cell Mlf6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HRcmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUm1OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5Njd3MkWg{txO MXrTRW5ITVJ?
human MDA-MB-453 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWjJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20OVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQS57MEeg{txO Mn\XV2FPT0WU
human MCF7 cell NWT4WI42T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVXkb2VwUW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvOzBzIN88US=> NIXNdHNUSU6JRWK=
human PC3 cells NYniT4pYTnWwY4Tpc44h[XO|YYm= M4XYflExOOPCgN88US=> M3nwPVQ5KGh? Mk[zTY5pcWKrdHnvckBw\iCjY4TpckBj[XOnZDDwd4V2\G:yb3TpZUBnd3KvYYTpc44hcW5iYX7kdo9o\W5vZHXw[Y5l\W62IHj1cYFvKFCFMzDj[YxteyCjdDCxNFAhfU1iYX\0[ZIhPDhiaILzJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJI1q[3Kxc3PvdJkh[XO|YYm= NEfIN2IzOjZ5Mkm4OC=>
human PC3 cells NEDCVWtHfW6ldHnvckBie3OjeR?= MX2wMlEuOSEQvF2= Ml7QRYdwdmm|dDDhZ5Rqfmm2eTDheEBidmS{b3flckBz\WOncITvdkBYPzRzQzDteZRidnRiZYjwdoV{e2WmIHnuJIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{B{fGmvdXzheIlwdiCxZjDy[YNmeHSxcjD0doFve2GldHn2ZZRqd25iYYSgNE4yKHSxIEGgeW0h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 MkKyNlIyPzV4OUS=

... 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
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    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