Temsirolimus (CCI-779, NSC 683864)

Licensed by Pfizer Catalog No.S1044

Temsirolimus (CCI-779, NSC 683864) Chemical Structure

Molecular Weight(MW): 1030.29

Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay.

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In DMSO USD 134 In stock
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4 Customer Reviews

  • mTOR inhibitors attenuate ganetespib-driven elevation of HSPs in multiple tumor cell types. A375 melanoma cells were treated with vehicle, ganetespib (25 nmol/L), BEZ235 (500 nmol/L), or temsirolimus (500 nmol/L), either alone or in combination, for 24 hours. The levels of HSP90α, HSP70, HSP27, and GAPDH were determined by immunoblotting.

    Mol Cancer Res 2014 12, 703-13. Temsirolimus (CCI-779, NSC 683864) purchased from Selleck.

    SCID mice with PC-9/Vec or PC-9/HGF tumors were administered as described in Figure. Four hours after final administration of erlotinib, tumors were harvested, and tumor cell angiogenesis (CD31) were determined by immunohistochemistry.

    PLoS One 2013 8, e62104. Temsirolimus (CCI-779, NSC 683864) purchased from Selleck.

  • SCID mice with PC-9/Vec or PC-9/HGF tumors were administered 25 mg/kg erlotinib once daily for 4 days or 50 mg/kg temsirolimus once from day 8. Four hours after final erlotinib administration, tumors were harvested, and the relative levels of proteins in the tumor lysates were determined by western blotting.

    PLoS One 2013 8, e62104. Temsirolimus (CCI-779, NSC 683864) purchased from Selleck.

    Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Temsirolimus for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. Temsirolimus (CCI-779, NSC 683864) purchased from Selleck.

Purity & Quality Control

Choose Selective mTOR Inhibitors

Biological Activity

Description Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay.
Targets
mTOR [1]
(Cell-free assay)
1.76 μM
In vitro

In the absence of FKBP12, Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM. Temsirolimus treatment at nanomolar concentrations (10 nM to <5 μM) displays a modest and selective antiproliferative activity via FKBP12-dependent mechanism, but can completely inhibit the proliferation of a broad panel of tumor cells at low micromolar concentrations (5-15 μM), involving FKBP12-independent suppression of mTOR signaling. Temsirolimus treatment at micromolar but not nanomolar concentrations (20 μM) causes a marked decline in global protein synthesis and disassembly of polyribosomes, accompanied by rapid increase in the phosphorylation of translation elongation factor eEF2 and the translation initiation factor eIF2A. [1] Temsirolimus inhibits the phosphorylation of ribosomal protein S6, more potently in PTEN-positive DU145 cells than in PTEN-negative PC-3 cells, and inhibits cell growth and clonogenic survival of both cells in a concentration-dependent manner. [2] Temsirolimus (100 ng/mL) potently inhibits proliferation and induces apoptosis in primary human lymphoblastic leukemia (ALL) cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HSC-4 cell M33JW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmD1TY5pcWKrdHnvckBw\iCqdX3hckBJW0NvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE{KG6P MkD5V2FPT0WU
human L-363 cell NF;kXoZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2j0VWlvcGmkaYTpc44hd2ZiaIXtZY4hVC1|NkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1OiCwTR?= NUnTU2dnW0GQR1XS
human Ramos-2G6-4C10 cell M3O3d2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjsTY5pcWKrdHnvckBw\iCqdX3hckBT[W2xcz2yS|YuPENzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|QzKG6P MknGV2FPT0WU
human SBC-1 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLITY5pcWKrdHnvckBw\iCqdX3hckBUSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ1KG6P NVzYV5U4W0GQR1XS
human MHH-PREB-1 cell M4faXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG1JUC2SUlXCMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR7NTDuUS=> M1vrbXNCVkeHUh?=
human LNCAP cells NYS0NWZbWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXnaWpFlOyCmYYnz Mn;XRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOTlPBVEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRTBwNTDuUS=> M4TUZlIyPDN6NUe5
human HH cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYLJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54NkSgcm0> M1PrNHNCVkeHUh?=
human TYK-nu cell NX3rbGNLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|c5KG6P MX\TRW5ITVJ?
human H4 cell NIjBOlJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37HcGlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC3JI5O NHe4cotUSU6JRWK=
human K5 cell M1u3WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4TocGlvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOzJI5O NW[xSllLW0GQR1XS
human PA-1 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHTTY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? NVrBRXI{W0GQR1XS
human SK-NEP-1 cell M1fncWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXfCVolYUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OSXAuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEmgcm0> M2HFdnNCVkeHUh?=
human 697 cell NIPuXm9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGnuOGFKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO{BvVQ>? MYrTRW5ITVJ?
human CTB-1 cell M2W3eWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlH4TY5pcWKrdHnvckBw\iCqdX3hckBEXEJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVMhdk1? NWC1VWtzW0GQR1XS
human DB cell NEjKXm5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2HYNWlvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O MYfTRW5ITVJ?
human MLMA cell NFzWU3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIe0[XBKdmirYnn0bY9vKG:oIHj1cYFvKE2OTVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlMyKG6P NIfJdndUSU6JRWK=
human GAMG cell NXXW[GhtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M17V[GlvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPFIhdk1? M1LrOHNCVkeHUh?=
human JVM-3 cell NG[wR5NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml7YTY5pcWKrdHnvckBw\iCqdX3hckBLXk1vMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVUhdk1? NFXF[JhUSU6JRWK=
human LAMA-84 cell NUDheVA4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlA{KG6P MYPTRW5ITVJ?
human RPMI-8226 cell NYTwOYp[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUDUNYNCUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O NYnZRXY4W0GQR1XS
human MOLT-4 cell M3XkZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVjJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuN|Ehdk1? NFfUNINUSU6JRWK=
human CAMA-1 cell NUT1TXl3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHW1d3hKdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzdibl2= MU\TRW5ITVJ?
human NCI-SNU-1 cell NV\BWZJFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWr1N2VyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkixJI5O MVnTRW5ITVJ?
human SW780 cell NUfnTW43T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1\5SGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{KG6P MYrTRW5ITVJ?
human H9 cell NFjCS2JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Moi0TY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEigcm0> M364NXNCVkeHUh?=
human BE-13 cell M2i0TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND65NUBvVQ>? NFr1OGVUSU6JRWK=
human ES8 cell M{jncmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJGVUQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwMkegcm0> M4\lenNCVkeHUh?=
human DEL cell NILNb3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGRGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNE[gcm0> M2LZV3NCVkeHUh?=
human QIMR-WIL cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2GyWGlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjdzIH7N MoPaV2FPT0WU
human CGTH-W-1 cell M3rOWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jOdGlvcGmkaYTpc44hd2ZiaIXtZY4hS0eWSD3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njd3IH7N NEjX[FNUSU6JRWK=
human CHL-1 cell NFPISndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1e4N2lvcGmkaYTpc44hd2ZiaIXtZY4hS0iOLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg3KG6P MXTTRW5ITVJ?
human A2780 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkTRTY5pcWKrdHnvckBw\iCqdX3hckBCOjd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFghdk1? MlvhV2FPT0WU
human VA-ES-BJ cell NULHNW83T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYnxbFJTUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> MV3TRW5ITVJ?
human BB65-RCC cell NFftSmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnTNTY5pcWKrdHnvckBw\iCqdX3hckBDSjZ3LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVchdk1? MnPxV2FPT0WU
human D-566MG cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUe3dHJwUW6qaXLpeIlwdiCxZjDoeY1idiCGLUW2Om1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py5zNjDuUS=> MmjHV2FPT0WU
human MDA468 cells MmnKVJJwdGmoZYLheIlwdiCjc4PhfS=> MnO2N{Bl[Xm| NIezfXdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERVQ3QCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUigcm0> MV:yNVQ{QDV5OR?=
human HO-1-N-1 cell NIK2SW5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{Hwe2lvcGmkaYTpc44hd2ZiaIXtZY4hUE9vMT3OMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRThwMjDuUS=> NGrxZnpUSU6JRWK=
human RS4-11 cell MonoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2XRT2lvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE41PSCwTR?= NHWxc2lUSU6JRWK=
human PC-3 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYPDNJdZUW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU4yPCCwTR?= MVfTRW5ITVJ?
human NB69 cell NV\JVpRDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXe1S3pTUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PiCwTR?= MkO4V2FPT0WU
human HGC-27 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGLoeJdKdmirYnn0bY9vKG:oIHj1cYFvKEiJQz2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPiCwTR?= MUXTRW5ITVJ?
human NCI-H720 cell NHP5bnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHfZS5VKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|IxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS54MjDuUS=> NF;uVIJUSU6JRWK=
human NCI-H292 cell MnrJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVjET29YUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwOESgcm0> NVvjXoh6W0GQR1XS
human A3-KAW cell NIXrendIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{jGTmlvcGmkaYTpc44hd2ZiaIXtZY4hSTNvS1HXJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvPDNibl2= NYLsbW46W0GQR1XS
human DU-4475 cell Mn;jS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUW4fmtLUW6qaXLpeIlwdiCxZjDoeY1idiCGVT20OFc2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwN{Ogcm0> NVjDXFVXW0GQR1XS
human HuH-7 cell NUDnSIhtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1r6PGlvcGmkaYTpc44hd2ZiaIXtZY4hUHWKLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk4{OiCwTR?= NW[3blF4W0GQR1XS
human J-RT3-T3-5 cell NYTKb3h{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUK5[4RjUW6qaXLpeIlwdiCxZjDoeY1idiCMLWLUN{1VOy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|ghdk1? MlzIV2FPT0WU
human VM-CUB-1 cell NFu5dHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX[0fItZUW6qaXLpeIlwdiCxZjDoeY1idiCYTT3DWWIuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lk[3JI5O M2PJUnNCVkeHUh?=
human MOLT-16 cell M3WzSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml\XTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvQDRibl2= M2DmcnNCVkeHUh?=
human KG-1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnO5TY5pcWKrdHnvckBw\iCqdX3hckBMTy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuPUBvVQ>? Mkj2V2FPT0WU
human P12-ICHIKAWA cell NYDQZVB[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFf6bmZKdmirYnn0bY9vKG:oIHj1cYFvKFBzMj3JR2hKU0GZQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlAyKG6P NFH0ZWtUSU6JRWK=
human ACN cell NFLpdnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmnVTY5pcWKrdHnvckBw\iCqdX3hckBCS05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNkBvVQ>? NEHwOmxUSU6JRWK=
human COLO-684 cell NXPDPYpHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV\NTlljUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY5PCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkOxJI5O NUHhU5R1W0GQR1XS
human T-24 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUjJcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz64OkBvVQ>? NXTPPVc{W0GQR1XS
human AGS cell MlL6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmTXTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND6xNUBvVQ>? MV;TRW5ITVJ?
human EW-13 cell NV\pToFHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGTsfVZKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTRibl2= Mn70V2FPT0WU
human SW962 cell NYHmeZF1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2jrS2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU42QSCwTR?= M3;YcHNCVkeHUh?=
human EW-11 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLTTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlYhdk1? MV3TRW5ITVJ?
human RXF393 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlrlTY5pcWKrdHnvckBw\iCqdX3hckBTYEZ|OUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU43PiCwTR?= M3zHeXNCVkeHUh?=
human EoL-1-cell cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHLYN4NKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNj6xJI5O M4judnNCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo In the NOD/SCID xenograft models with human ALL, Temsirolimus treatment at 10 mg/kg/day produces a decrease in peripheral blood blasts and in splenomegaly [3] Administration of Temsirolimus (20 mg/kg i.p. 5 days/week) significantly delays the growth of DAOY xenografts by 160% after 1 week and 240% after 2 weeks, compared with controls. Single high-dose of Temsirolimus (100 mg/kg i.p) treatment induces 37% regression of tumor volume within 1 week. Temsirolimus treatment for 2 weeks also delays the growth of rapamycin-resistant U251 xenografts by 148%. [4] Inhibition of mTOR by Temsirolimus improves performance on four different behavioral tasks and decreases aggregate formation in a mouse model of Huntington disease. [5] Administration of Temsirolimus induces significant dose-dependent, antitumor responses against subcutaneous growth of 8226, OPM-2, and U266 xenografts with ED50 of 20 mg/kg and 2 mg/kg for 8226 and OPM-2, respectively, which are associated with inhibited proliferation and angiogenesis, induction of apoptosis, and reduction in tumor cell size. [6]

Protocol

Kinase Assay:

[1]

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In vitro assay of mTOR catalytic activity:

The Flag-tagged wild-type human mTOR (Flag-mTOR) DNA constructs are transiently transfected into HEK293 cells. Protein extraction and purification of Flag-mTOR are carried out 48 hours later. In vitro kinase assays of purified Flag-mTOR in the presence of various concentrations of Temsirolimus without FKBP12 are performed in 96-well plate and detected by dissociation-enhanced lanthanide fluorescent immunoassay (DELFIA) using His6-S6K1 as the substrate. Enzymes is first diluted in kinase assay buffer (10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, 10 mM MnCl2, 0.5 mM DTT, 0.25 μM microcystin LR, and 100 μg/mL BSA). To each well, 12 μL of the diluted enzyme is mixed briefly with 0.5 μL Temsirolimus. The kinase reaction is initiated by adding 12.5 μL kinase assay buffer containing ATP and His6-S6K to give a final reaction volume of 25 μL containing 800 ng/mL FLAG-mTOR, 100 μM ATP, and 1.25 μM His6-S6K. The reaction plate is incubated for 2 hours (linear at 1-6 hours) at room temperature with gentle shaking and then terminated by adding 25 μL Stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA). The DELFIA detection of the phosphorylated (Thr-389) His6-S6K is performed at room temperature using a monoclonal anti-P(T389)-p70S6K antibody labeled with Europium-N1-ITC (Eu) (10.4 Eu per antibody). 45 μL of the terminated kinase reaction mixture is transferred to a MaxiSorp plate containing 55 μL PBS. The His6-S6K is allowed to attach for 2 hours after which the wells are aspirated and washed once with PBS. 100 μL of DELFIA buffer with 40 ng/mL Eu-P(T389)-S6K antibody is added. The antibody binding is continued for 1 hour with gentle agitation. The wells are then aspirated and washed four times with PBS containing 0.05% Tween 20 (PBST). 100 μL of DELFIA Enhancement solution is added to each well and the plates are read in a PerkinElmer Victor model plate reader.
Cell Research:

[1]

+ Expand
  • Cell lines: A549, H157, H460, H446, HCT116, HT29, SW480, DLD1, Caco2, LNCap, DU145, MDA468, MDA231, HEK293, and PC3-MM2
  • Concentrations: Dissolved in DMSO, final concentrations ~20 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are exposed to various concentrations of Temsirolimus for 72 hours. After treatment, viable cell densities are determined by MTS dye conversion using CellTiter AQ assay kit.


    (Only for Reference)
Animal Research:

[4]

+ Expand
  • Animal Models: Female athymic nude mice injected s.c. with DAOY, or U251 cells
  • Formulation: Prepared in 100% EtOH as a 50 mg/mL stock solution, and diluted in 5% Tween 80 and 5% polyethylene glycol 400
  • Dosages: 20 mg/kg
  • Administration: Injection daily 5 times per week
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 75 mg/mL (72.79 mM)
DMSO 67 mg/mL (65.03 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300 +2% Tween 80+ddH2O
For best results, use promptly after mixing.
7mg/mL

* 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 1030.29
Formula

C56H87NO16

CAS No. 162635-04-3
Storage powder
Synonyms N/A

Bio Calculators

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Molarity Calculator

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01182883 Withdrawn Brain Stem Neoplasms|Glioma|Pinealoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 28, 2010 Phase 1
NCT02908035 Not yet recruiting Chronic Limb Ischemia Mercator MedSystems, Inc. January 2017 Phase 2
NCT02567435 Suspended Alveolar Rhabdomyosarcoma|Botryoid-Type Embryonal Rhabdomyosarcoma|Embryonal Rhabdomyosarcoma|Rhabdomyosarcoma|Sclerosing Rhabdomyosarcoma|Spindle Cell Rhabdomyosarcoma|Untreated Childhood Rhabdomyosarcoma National Cancer Institute (NCI) May 2016 Phase 3
NCT02693535 Recruiting Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer March 2016 Phase 2
NCT02560012 Recruiting Carcinoma, Renal Cell The University of Texas Health Science Center, Houston December 2015 Phase 2
NCT02420613 Recruiting Diffuse Intrinsic Pontine Glioma M.D. Anderson Cancer Center October 2015 Phase 1

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