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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Cited by 13 Publications

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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.

  • 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.

  • Cancer Res, 2018, doi:10.1158/0008-5472.CAN-17-3728. 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.

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 MXLGeY5kfGmxbjDhd5NigQ>? M{nCPGRqe3CuYXPlcYVvfCCxZjDbN2heWjF6OEGg[pJwdSCDUjDpckBpfW2jbjDNSGEuVUJvNEWzJINmdGy|LDDFR|UxRTNzIH7N M3zxTVI{PzF|NU[3
LNCaP cells MXrGeY5kfGmxbjDhd5NigQ>? MXnJcohq[mm2aX;uJI9nKFt|SG2tSGhVKGKrbnTpcochfG9iVEi3O2Eh[W6mcn;n[Y4hemWlZYD0c5Ihd2ZiTF7DZXAh[2WubIOsJGtqRTN3IH7N MVmxOVYxOzl4MB?=
Freestyle293F cells NI\Z[VdHfW6ldHnvckBie3OjeR?= MWTJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCDbnTyc4dmdiC{ZXPldJRweiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDGdoVme3S7bHWyPVNHKGOnbHzzMEBKSzVyPUCuNFU1KM7:TR?= M1\zelI{OTl7NEe3
HEK293 cells NWDMdGIxTnWwY4Tpc44h[XO|YYm= MU[zJIg> M1[3R2Rqe3CuYXPlcYVvfCCxZjDbNVcu[WyyaHGtcYV1cHmuLUPIYY1q[m:uZYLvcoUh\nKxbTDhcoRzd2enbjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHmeIVzKDNiaILzMEBKSzVyPUW0JI5O NXXPfmpPOjJ|OUGwN|M>
MDA453 cells MWXGeY5kfGmxbjDhd5NigQ>? MX;EbZNxdGGlZX3lcpQhd2ZiW{PIYWRJXCCocn;tJIh2dWGwIHHu[JJw\2WwIILlZ4VxfG:{IHnuJG1FSTR3MzDj[YxteyxiS3m9OlQhdk1? M3PsO|E5OjlzNkS0
human MDA-MB-453 cells MVXGeY5kfGmxbjDhd5NigQ>? NVjo[G9NTGm|cHzhZ4Vu\W62IH;mJHs{UF2GSGSg[pJwdSCDUjDpckBpfW2jbjDNSGEuVUJvNEWzJINmdGy|LDDJR|UxRTZ2IH7N NIDTc5QzODV6NE[xNC=>
COS1 cells NFfF[FVHfW6ldHnvckBie3OjeR?= M3H2[mFvfGGpb37pd5Qh[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 M3PMXFI2PjR4NkS5
HeLa cells NUnsUIZ[TnWwY4Tpc44h[XO|YYm= NHzQfoVCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKGGwZILv[4VvKHKnY3XweI9zKGW6cILld5Nm\CCrbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[g[IlpgWS{b4Tld5Rwe3Sncn;u[UBqdmS3Y3XkJJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eTDifUBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVAvOTRizszN NUewU5pyOTd6MESyNlk>
CV1 cells NYS2V4tETnWwY4Tpc44h[XO|YYm= NUT1b45wSmmwZHnu[{Bi\m[rbnn0fUB1dyCqdX3hckBidmS{b3flckBz\WOncITvdkBmgHC{ZYPz[YQhcW5iQ2[xJINmdGy|LDDLbV0xNjF3MTFOwG0> MUOxO|I2Pzh|OB?=
monkey COS7 cells MmPJSpVv[3Srb36gZZN{[Xl? MonSRolv\GmwZzDh[oZqdmm2eTD0c{BpfW2jbjDhcoRzd2enbjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hdW:wa3X5JGNQWzdiY3XscJMh[nlid3jvcIUh[2WubDDibY5lcW6pIHHzd4F6NCCNaU2wMlE2OSEQvF2= NV3kfmgxOTh2NEK5NVI>
COS7 cells NULZdZpSTnWwY4Tpc44h[XO|YYm= M{\XWWFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgW|c1OUNibYX0ZY51KGW6cILld5Nm\CCrbjDDU3M4KGOnbHzzJIF{e2W|c3XkJIF{KGy3Y3nm[ZJie2ViYXP0bZZqfHliYX\0[ZIhOjRiaILzJIJ6KHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5zODFOwG0> MXKyNlA6PDJ5OR?=
CHO-K1 cells NVv4cWNVTnWwY4Tpc44h[XO|YYm= M2\pcVIhcA>? M2fjZ2Rqe3CuYXPlcYVvfCCxZjDbN2hedWmkb3zldo9v\SCocn;tJIh2dWGwIFHSJIV5eHKnc4Pl[EBqdiCFSF:tT|Eh[2WubIOgZYZ1\XJiMjDodpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3ME2wMlIh|ryP MXSyNFM5OTN4MR?=
human HT-3 cell MlXPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUHvUmpuUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OzF|NDFOwG0> NFu0ZYRUSU6JRWK=
human LNCAP cells NHO1WJVRem:uaX\ldoF1cW:wIHHzd4F6 NGPZPGg{KGSjeYO= NEXNS4FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyxiSVO1NF0xNjd|Mkeg{txO MnvYNlYxPDZ|MUO=
human PC3 cells MlrDSpVv[3Srb36gZZN{[Xl? MVLEbZNxdGGlZX3lcpQhd2ZiW{PIYXIyQDhzIH\yc40h[W6mcn;n[Y4hemWlZYD0c5IhcW5iaIXtZY4hWEN|IHPlcIx{NCCHQ{WwQVQvOyEQvF2= MYWyOVU6OTB4Nh?=
human 22Rv1 cells MnL1SpVv[3Srb36gZZN{[Xl? NFzmdII{KGSjeYO= M1jSWGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiYX7kdo9o\W5icnXj[ZB1d3JiSEi3OHkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKGi3bXHuJFIzWnZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTEiWLXnu[JVk\WRiY3XscEBoem:5dHigZYZ1\XJiMzDkZZl{KGK7IGfTWE05KGG|c3H5MEBKSzVyPUSuOkDPxE1? NX;POldnOjR7MEC1PFg>
human CCF-STTG1 cell NHzOWo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHHjR3RKdmirYnn0bY9vKG:oIHj1cYFvKEOFRj3TWHRIOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;ND65NlkzQSEQvF2= MYXTRW5ITVJ?
human SCC-25 cell NYG5[ldCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkjuTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvMkWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlA5PjV4IN88US=> NVHxU|NHW0GQR1XS
human MKN45 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXT5VZlrUW6qaXLpeIlwdiCxZjDoeY1idiCPS160OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvQTZyNTFOwG0> M4jJTXNCVkeHUh?=
human ES5 cell NH7MdZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXfkWHd4UW6qaXLpeIlwdiCxZjDoeY1idiCHU{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlYyOTV2IN88US=> MVfTRW5ITVJ?
human SK-MEL-3 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmG3TY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjB7NkSg{txO M3y5ZnNCVkeHUh?=
human PC-3 cell NF7Mc5NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWDkNII2UW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvOjd7MTFOwG0> M1jWcnNCVkeHUh?=
human NOS-1 cell M3jFeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn22TY5pcWKrdHnvckBw\iCqdX3hckBPV1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlI6OTdizszN NYjmfGpjW0GQR1XS
human LB1047-RCC cell NHjxcWdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLSRWxKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj6yOVMh|ryP MYrTRW5ITVJ?
human CAMA-1 cell M{DSO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEf4VItKdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjN7Mk[g{txO NV:5OpRoW0GQR1XS
human SAS cell NVLvVoNCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXPjS3JxUW6qaXLpeIlwdiCxZjDoeY1idiCVQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4{ODhzIN88US=> NYfHZ2FNW0GQR1XS
human NCI-H2228 cell NFTTWGZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFWyclZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlIzQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|Lke1N|Eh|ryP MmLVV2FPT0WU
human NCI-H187 cell NXLpZZpOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1XSemlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi54NkG2JO69VQ>? M2m0eHNCVkeHUh?=
human BFTC-905 cell MlPaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M32xXWlvcGmkaYTpc44hd2ZiaIXtZY4hSk[WQz25NFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy52OEW3JO69VQ>? M1L1ZXNCVkeHUh?=
human G-361 cell MkjsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKGi3bXHuJGcuOzZzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUeuPFI3KM7:TR?= MonuV2FPT0WU
human DU145 cells MlvqR5l1d3SxeHnjxsBie3OjeR?= NXzJWohQPzJiaB?= M4PG[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEWUYXzwbIEu\GWoaXPp[Y51KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiRWLi[ZRiKGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OThizszN M3\DNXNCVkeHUh?=
human SW780 cell Mn;ES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIKyd3lKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZk> NU\ZRZBlW0GQR1XS
human BB49-HNC cell MojES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MojMTY5pcWKrdHnvckBw\iCqdX3hckBDSjR7LVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE5Njl3M{Kg{txO MorhV2FPT0WU
human KALS-1 cell M1fCc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVvsc2FyUW6qaXLpeIlwdiCxZjDoeY1idiCNQVzTMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQS54NkO1JO69VQ>? NEHLU5pUSU6JRWK=
human AU565 cell NFvUfW5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGrOVoVKdmirYnn0bY9vKG:oIHj1cYFvKEGXNU[1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPzRyMjFOwG0> MYPTRW5ITVJ?
human NCI-H2087 cell NYP1RYR{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX36bm5HUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxQDdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{MT6wOVkyKM7:TR?= MmjRV2FPT0WU
human RVH-421 cell Mo\US5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnHtTY5pcWKrdHnvckBw\iCqdX3hckBTXkhvNEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvPTd7NTFOwG0> M1ez[XNCVkeHUh?=
human SK-CO-1 cell MmHYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NICyVWNKdmirYnn0bY9vKG:oIHj1cYFvKFONLVPPMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS56OEeyJO69VQ>? MnjnV2FPT0WU
human KU-19-19 cell MlnQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKGi3bXHuJGtWNTF7LUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvODJ2MjFOwG0> MWrTRW5ITVJ?
human NB6 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHixcpdKdmirYnn0bY9vKG:oIHj1cYFvKE6ENjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlkyOzVizszN MlnNV2FPT0WU
human RO82-W-1 cell NYf0doRFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHfucnpKdmirYnn0bY9vKG:oIHj1cYFvKFKROEKtW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjNwMUOxPEDPxE1? MlvjV2FPT0WU
human LNCAP cells NXLjfGliS3m2b4TvfIlkyqCjc4PhfS=> NFzFZ24zKGSjeYO= MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjCyJIRigXNiYomgZ4VtdCClb4XueIlv\yCvZYToc4QtKEmFNUC9NlMvPzlizszN Mor3NlM4OjdyNES=
human CTB-1 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mmi0TY5pcWKrdHnvckBw\iCqdX3hckBEXEJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlU2OzZizszN NUPP[pB2W0GQR1XS
human SW48 cell MnPXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGi0RnVKdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE43PTR4IN88US=> MYLTRW5ITVJ?
human TCCSUP cell M4r6VWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXzTY5pcWKrdHnvckBw\iCqdX3hckBVS0OVVWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE44OjN{IN88US=> MVzTRW5ITVJ?
human DK-MG cell M{WzPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIrNdZFKdmirYnn0bY9vKG:oIHj1cYFvKESNLV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvQDlzNzFOwG0> Mm\RV2FPT0WU
human ST486 cell M4PUWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHjvTYFKdmirYnn0bY9vKG:oIHj1cYFvKFOWNEi2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvPzR4NDFOwG0> NELMbGtUSU6JRWK=
human H4 cell NYPhWGZHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVnP[|dUUW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK2Mlk1PThizszN MV7TRW5ITVJ?
human SBC-1 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NU\wUHU2UW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5NjN3MEeg{txO NUnXWIlNW0GQR1XS
human CAS-1 cell M3OzeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlnqTY5pcWKrdHnvckBw\iCqdX3hckBESVNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlYzQTRizszN NVvwSlZXW0GQR1XS
human OAW-42 cell MkPRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUnJcohq[mm2aX;uJI9nKGi3bXHuJG9CXy12MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlcyQTVizszN NXj4c3RYW0GQR1XS
human HCC1954 cell M4XyNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVLJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF7NUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE44PTJ3IN88US=> NVK4dFBnW0GQR1XS
human MDA-MB-453 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20OVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQS57MEeg{txO NYTwTId1W0GQR1XS
human MCF7 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2T0XmlvcGmkaYTpc44hd2ZiaIXtZY4hVUOINzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO5MlMxOSEQvF2= MknzV2FPT0WU
human PC3 cells M1;pcGZ2dmO2aX;uJIF{e2G7 M1;oXVExOOPCgN88US=> M3W4VVQ5KGh? MlnsTY5pcWKrdHnvckBw\iCjY4TpckBj[XOnZDDwd4V2\G:yb3TpZUBnd3KvYYTpc44hcW5iYX7kdo9o\W5vZHXw[Y5l\W62IHj1cYFvKFCFMzDj[YxteyCjdDCxNFAhfU1iYX\0[ZIhPDhiaILzJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJI1q[3Kxc3PvdJkh[XO|YYm= NYjrTGQxOjJ4N{K5PFQ>
human PC3 cells MkTkSpVv[3Srb36gZZN{[Xl? NHjmTFIxNjFvMTFOwG0> MYPB[49vcXO2IHHjeIl3cXS7IHH0JIFv\HKxZ3XuJJJm[2WydH;yJHc4PDGFIH31eIFvfCCneIDy[ZN{\WRiaX6gbJVu[W5iUFOzJINmdGy|IHHzd4V{e2WmIHHzJJN1cW23bHH0bY9vKG:oIILlZ4VxfG:{IITyZY5{[WO2aY\heIlwdiCjdDCwMlEhfG9iMTD1UUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MXSyNlE4PTZ7NB?=

... 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
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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
    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
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 2019 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 2019 Phase 2
NCT03809000 Not yet recruiting Prostate Cancer RTOG Foundation Inc.|Pfizer|Astellas Pharma Inc February 15 2019 Phase 2
NCT03809000 Not yet recruiting Prostate Cancer RTOG Foundation Inc.|Pfizer|Astellas Pharma Inc February 15 2019 Phase 2
NCT03678025 Recruiting Castration Levels of Testosterone|Metastatic Prostatic Adenocarcinoma|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8 Southwest Oncology Group|National Cancer Institute (NCI) September 17 2018 Phase 3
NCT03678025 Recruiting Castration Levels of Testosterone|Metastatic Prostatic Adenocarcinoma|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8 Southwest Oncology Group|National Cancer Institute (NCI) September 17 2018 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

If you have any other enquiries, please leave a message.

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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID