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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  • 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 NH;3OWFHfW6ldHnvckBie3OjeR?= NYnlUnZZTGm|cHzhZ4Vu\W62IH;mJHs{UF2UMUi4NUBnem:vIFHSJIlvKGi3bXHuJG1FSS2PQj20OVMh[2WubIOsJGVEPTB;M{Ggcm0> NETwTpYzOzdzM{W2Oy=>
LNCaP cells MnjUSpVv[3Srb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKFt|SG2tSGhVKGKrbnTpcochfG9iVEi3O2Eh[W6mcn;n[Y4hemWlZYD0c5Ihd2ZiTF7DZXAh[2WubIOsJGtqRTN3IH7N NIX5coMyPTZyM{m2NC=>
Freestyle293F cells MVXGeY5kfGmxbjDhd5NigQ>? NUntVld{UW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgRY5lem:pZX6gdoVk\XC2b4KgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hTnKnZYP0fYxmOjl|RjDj[YxteyxiSVO1NF0xNjB3NDFOwG0> M{XlcFI{OTl7NEe3
HEK293 cells MWnGeY5kfGmxbjDhd5NigQ>? NUixW4hkOyCq MVzEbZNxdGGlZX3lcpQhd2ZiW{G3MYFteGijLX3leIh6dC1|SG3tbYJwdGW{b37lJIZzd21iYX7kdo9o\W5icnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjZoTldkA{KGi{czygTWM2OD13NDDuUS=> M4Htb|IzOzlzMEOz
MDA453 cells MlLCSpVv[3Srb36gZZN{[Xl? NHi2eZFFcXOybHHj[Y1mdnRib3[gX|NJZUSKVDDmdo9uKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIlvKE2GQUS1N{Bk\WyuczygT4k:PjRibl2= NEnJOFcyQDJ7MU[0OC=>
human MDA-MB-453 cells MmXCSpVv[3Srb36gZZN{[Xl? M{fDZ2Rqe3CuYXPlcYVvfCCxZjDbN2heTEiWIH\yc40hSVJiaX6gbJVu[W5iTVTBMW1DNTR3MzDj[YxteyxiSVO1NF03PCCwTR?= NHH3eIUzODV6NE[xNC=>
COS1 cells MYPGeY5kfGmxbjDhd5NigQ>? MWPBcpRi\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?= NYTsbnY2OjV4NE[2OFk>
HeLa cells MWnGeY5kfGmxbjDhd5NigQ>? M{PyRWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4h[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDkbYh6\HKxdHXzeI9{fGW{b37lJIlv\HWlZXSgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHL5JJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NE4yPCEQvF2= Mn\DNVc5ODR{Mkm=
CV1 cells NXntRXZ6TnWwY4Tpc44h[XO|YYm= NH7sPVhDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCFVkGgZ4VtdHNuIFvpQVAvOTVzIN88US=> MVuxO|I2Pzh|OB?=
monkey COS7 cells M1KxR2Z2dmO2aX;uJIF{e2G7 M1XudGJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gZY5lem:pZX6gdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKG2xbnvlfUBEV1N5IHPlcIx{KGK7IIfoc4xmKGOnbHygZolv\GmwZzDhd5NigSxiS3m9NE4yPTFizszN NFXSUZkyQDR2MkmxNi=>
COS7 cells NGT4SFRHfW6ldHnvckBie3OjeR?= NUXYWllXSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBidmS{b3flckBz\WOncITvdkBYPzRzQzDteZRidnRiZYjwdoV{e2WmIHnuJGNQWzdiY3XscJMh[XO|ZYPz[YQh[XNibIXjbYZmemG|ZTDhZ5Rqfmm2eTDh[pRmeiB{NDDodpMh[nlicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkG4JO69VQ>? NGDCZZIzOjB7NEK3PS=>
CHO-K1 cells MnnuSpVv[3Srb36gZZN{[Xl? M2fwTFIhcA>? MljXSIl{eGyjY3Xt[Y51KG:oIGuzTH1ucWKxbHXyc45mKG[{b32gbJVu[W5iQWKg[ZhxemW|c3XkJIlvKEOKTz3LNUBk\WyuczDh[pRmeiB{IHjyd{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyPUCuNkDPxE1? MXWyNFM5OTN4MR?=
human HT-3 cell NInxUHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmqwTY5pcWKrdHnvckBw\iCqdX3hckBJXC1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63N|E{PCEQvF2= MkLkV2FPT0WU
human LNCAP cells MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 NX[zfG83OyCmYYnz NWrpUHoySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNuIFnDOVA:OC55M{K3JO69VQ>? MWOyOlA1PjNzMx?=
human PC3 cells M3HmNWZ2dmO2aX;uJIF{e2G7 NHv3cZpFcXOybHHj[Y1mdnRib3[gX|NJZVJzOEixJIZzd21iYX7kdo9o\W5icnXj[ZB1d3JiaX6gbJVu[W5iUFOzJINmdGy|LDDFR|UxRTRwMzFOwG0> NIWxU|QzPTV7MUC2Oi=>
human 22Rv1 cells MX;GeY5kfGmxbjDhd5NigQ>? MWOzJIRigXN? NYD4W2NLSW62YXfvcol{fCCjY4Tpeol1gSCjdDDhcoRzd2enbjDy[YNmeHSxcjDIPFc1YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaIXtZY4hOjKUdkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCGSGStbY5lfWOnZDDj[YxtKGe{b4f0bEBi\nSncjCzJIRigXNiYomgW3NVNThiYYPzZZktKEmFNUC9OE43KM7:TR?= M3PMNlI1QTByNUi4
human CCF-STTG1 cell NFvueWtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGNETi2VVGTHNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:PC57MkmyPUDPxE1? Moq0V2FPT0WU
human SCC-25 cell NYq0S4FWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlLtTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvMkWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlA5PjV4IN88US=> NV33XoNvW0GQR1XS
human MKN45 cell M4rBRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXu2TItvUW6qaXLpeIlwdiCxZjDoeY1idiCPS160OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvQTZyNTFOwG0> MoDnV2FPT0WU
human ES5 cell M4T5O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnzwTY5pcWKrdHnvckBw\iCqdX3hckBGWzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16Lk[xNVU1KM7:TR?= MX;TRW5ITVJ?
human SK-MEL-3 cell NGf2UYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlHzTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjB7NkSg{txO NXfXcYhkW0GQR1XS
human PC-3 cell NUfyVotMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkK1TY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNlc6OSEQvF2= NXfablZ{W0GQR1XS
human NOS-1 cell NXj6NZFrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXXSPI9TUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjJ7MUeg{txO M1jYPHNCVkeHUh?=
human LB1047-RCC cell MmfBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkP2TY5pcWKrdHnvckBw\iCqdX3hckBNSjFyNEetVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwMkWzJO69VQ>? MmnzV2FPT0WU
human CAMA-1 cell NGTibHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2P2[2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvOzl{NjFOwG0> NIXqRlFUSU6JRWK=
human SAS cell NWjHb5FKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUXO[WY{UW6qaXLpeIlwdiCxZjDoeY1idiCVQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4{ODhzIN88US=> MUDTRW5ITVJ?
human NCI-H2228 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVfubHlpUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzOjhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz63OVMyKM7:TR?= MUnTRW5ITVJ?
human NCI-H187 cell MoPQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml7NTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG4O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3NjZ4MU[g{txO MmjUV2FPT0WU
human BFTC-905 cell NXX2N2oxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWLJcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvPDh3NzFOwG0> MUXTRW5ITVJ?
human G-361 cell M17HSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NETXNmJKdmirYnn0bY9vKG:oIHj1cYFvKEdvM{[xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvQDJ4IN88US=> NXmwdYZLW0GQR1XS
human DU145 cells NH2zSpJEgXSxdH;4bYPDqGG|c3H5 MX[3NkBp MkeyR5l1d3SxeHnjbZR6KGGpYXnud5QhTVKjbIDoZU1l\W[rY3nlcpQhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCHUnLleIEh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yQCEQvF2= MmPCV2FPT0WU
human SW780 cell NVO0Tot5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= NVj5eWVxW0GQR1XS
human BB49-HNC cell NVvXNGZrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXHJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVgvQTV|MjFOwG0> MXjTRW5ITVJ?
human KALS-1 cell NHK5NlJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{\lbWlvcGmkaYTpc44hd2ZiaIXtZY4hU0GOUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPjZ|NTFOwG0> M3P1[HNCVkeHUh?=
human AU565 cell M{XB[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\JfGlvcGmkaYTpc44hd2ZiaIXtZY4hSVV3NkWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU44PDB{IN88US=> MYPTRW5ITVJ?
human NCI-H2087 cell Mkf2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVLDWWg3UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxQDdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{MT6wOVkyKM7:TR?= NXPwOZFkW0GQR1XS
human RVH-421 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWLwNWg6UW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwNUe5OUDPxE1? MoLyV2FPT0WU
human SK-CO-1 cell NGPMeWdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYD2Um1mUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3DU{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwOEi3NkDPxE1? NYXpcYJCW0GQR1XS
human KU-19-19 cell M2G1[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXaTY5pcWKrdHnvckBw\iCqdX3hckBMXS1zOT2xPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIzNjB{NEKg{txO NEe2dY9USU6JRWK=
human NB6 cell MnjBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MojmTY5pcWKrdHnvckBw\iCqdX3hckBPSjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Mj65NVM2KM7:TR?= NGDYUoRUSU6JRWK=
human RO82-W-1 cell NFzxTIlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKGi3bXHuJHJQQDJvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvOTNzODFOwG0> NXnSXIdYW0GQR1XS
human LNCAP cells Mnr4R5l1d3SxeHnjxsBie3OjeR?= NGfUNI4zKGSjeYO= MkPpR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5ESVBiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgNkBl[Xm|IHL5JINmdGxiY3;1cpRqdmdibXX0bI9lNCCLQ{WwQVI{Njd7IN88US=> MWWyN|czPzB2NB?=
human CTB-1 cell M33nXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlPQTY5pcWKrdHnvckBw\iCqdX3hckBEXEJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlU2OzZizszN M37hcnNCVkeHUh?=
human SW48 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV\QXZM2UW6qaXLpeIlwdiCxZjDoeY1idiCVV{S4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPjV2NjFOwG0> NWD2VGpJW0GQR1XS
human TCCSUP cell M1jEOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFzFbIRKdmirYnn0bY9vKG:oIHj1cYFvKFSFQ2PVVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1Njd{M{Kg{txO NFjpVHZUSU6JRWK=
human DK-MG cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkCxTY5pcWKrdHnvckBw\iCqdX3hckBFUy2PRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0Mlg6OTdizszN Ml7LV2FPT0WU
human ST486 cell NF;DcIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MljCTY5pcWKrdHnvckBw\iCqdX3hckBUXDR6NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK1Mlc1PjRizszN M4\qV3NCVkeHUh?=
human H4 cell MnrvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHTEOGlKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mk[uPVQ2QCEQvF2= M1fBcnNCVkeHUh?=
human SBC-1 cell M1Ozcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3fGV2lvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE4{PTB5IN88US=> MlvmV2FPT0WU
human CAS-1 cell NX\uVIJRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NI\2U3dKdmirYnn0bY9vKG:oIHj1cYFvKEODUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPjJ7NDFOwG0> MXPTRW5ITVJ?
human OAW-42 cell MoC4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKGi3bXHuJG9CXy12MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlcyQTVizszN MnfWV2FPT0WU
human HCC1954 cell Mly1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1;BcGlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUm1OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5Njd3MkWg{txO MXnTRW5ITVJ?
human MDA-MB-453 cell NFLnb4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{jsV2lvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQ2OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ7LkmwO{DPxE1? Mlr3V2FPT0WU
human MCF7 cell MlXKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkD6TY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{muN|AyKM7:TR?= M4LCW3NCVkeHUh?=
human PC3 cells NXq5UmVyTnWwY4Tpc44h[XO|YYm= MXexNFDkiIEQvF2= M{HQfVQ5KGh? MnvyTY5pcWKrdHnvckBw\iCjY4TpckBj[XOnZDDwd4V2\G:yb3TpZUBnd3KvYYTpc44hcW5iYX7kdo9o\W5vZHXw[Y5l\W62IHj1cYFvKFCFMzDj[YxteyCjdDCxNFAhfU1iYX\0[ZIhPDhiaILzJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJI1q[3Kxc3PvdJkh[XO|YYm= NGXsbZMzOjZ5Mkm4OC=>
human PC3 cells MUTGeY5kfGmxbjDhd5NigQ>? NFK2NmkxNjFvMTFOwG0> M1T4VGFod26rc4SgZYN1cX[rdImgZZQh[W6mcn;n[Y4hemWlZYD0c5IhXzd2MVOgcZV1[W62IHX4dJJme3OnZDDpckBpfW2jbjDQR|Mh[2WubIOgZZN{\XO|ZXSgZZMhe3SrbYXsZZRqd25ib3[gdoVk\XC2b4KgeJJidnOjY4TpeoF1cW:wIHH0JFAvOSC2bzCxJJVOKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> MmP5NlIyPzV4OUS=

... 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]
+ 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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*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
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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 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