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 MkPaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFvQNWxKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTNibl2= NYnoPGNlW0GQR1XS
human L-363 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofZTY5pcWKrdHnvckBw\iCqdX3hckBNNTN4MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQzKG6P M3fueXNCVkeHUh?=
human Ramos-2G6-4C10 cell MnPNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2nF[mlvcGmkaYTpc44hd2ZiaIXtZY4hWmGvb4OtNmc3NTSFMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM1OiCwTR?= NIrIVYVUSU6JRWK=
human SBC-1 cell M4jSdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEft[nNKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PDRibl2= NIDze3pUSU6JRWK=
human MHH-PREB-1 cell MmrjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYLWd5NqUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitVHJGSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVUhdk1? MX7TRW5ITVJ?
human LNCAP cells NUHJOVdEWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn;jN{Bl[Xm| NI\NNolCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;MD61JI5O M1i3dlIyPDN6NUe5
human HH cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXTOcllsUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlY1KG6P M3r3TnNCVkeHUh?=
human TYK-nu cell M{\3R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{fhcWlvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44Pzhibl2= MYXTRW5ITVJ?
human H4 cell MoDLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUfTT3o{UW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFchdk1? M{\Ne3NCVkeHUh?=
human K5 cell NE\HTYJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVzZeJpuUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Mhdk1? NGLReZFUSU6JRWK=
human PA-1 cell M3fUO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmPjTY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? M4f5O3NCVkeHUh?=
human SK-NEP-1 cell NX3aO5BlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmDUTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QRWCtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDlibl2= Ml[xV2FPT0WU
human 697 cell M13oVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFf3PVVKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO{BvVQ>? NF:1fWpUSU6JRWK=
human CTB-1 cell M1XURmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFzZdHlKdmirYnn0bY9vKG:oIHj1cYFvKEOWQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk46OyCwTR?= NF62bpVUSU6JRWK=
human DB cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NILodHVKdmirYnn0bY9vKG:oIHj1cYFvKESEIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6xNkBvVQ>? Mn3TV2FPT0WU
human MLMA cell NITGd|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NET3NG1KdmirYnn0bY9vKG:oIHj1cYFvKE2OTVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlMyKG6P NXS5[WFzW0GQR1XS
human GAMG cell NEmyWJRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJGdCVUdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkiyJI5O Ml;5V2FPT0WU
human JVM-3 cell NXnqSJp6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2LnTGlvcGmkaYTpc44hd2ZiaIXtZY4hUl[PLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2KG6P MY\TRW5ITVJ?
human LAMA-84 cell NGK5fm9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF\XWXBKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB|IH7N MWfTRW5ITVJ?
human RPMI-8226 cell NUDYOFhsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV34VGFHUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O NX[ydoVIW0GQR1XS
human MOLT-4 cell MoXNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PwXGlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{OSCwTR?= Mmq3V2FPT0WU
human CAMA-1 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIPxWndKdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzdibl2= M3HXT3NCVkeHUh?=
human NCI-SNU-1 cell NIT6cGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFLHfHJKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEGgcm0> NFHWOoFUSU6JRWK=
human SW780 cell M33GVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4\obWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{KG6P MY\TRW5ITVJ?
human H9 cell NUThVm9pT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnK3TY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEigcm0> M2fmWHNCVkeHUh?=
human BE-13 cell MmTuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFe5O2lKdmirYnn0bY9vKG:oIHj1cYFvKEKHLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46OSCwTR?= NEnJ[2FUSU6JRWK=
human ES8 cell M{n3OGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1W5bWlvcGmkaYTpc44hd2ZiaIXtZY4hTVN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6yO{BvVQ>? M4TrTXNCVkeHUh?=
human DEL cell NInOVYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MorETY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O MWnTRW5ITVJ?
human QIMR-WIL cell M2[2T2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44OSCwTR?= NFzIUHZUSU6JRWK=
human CGTH-W-1 cell NGDC[IdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWT6c3lSUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Wgcm0> NUTXT2R7W0GQR1XS
human CHL-1 cell NULUfWI{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUnJcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? MVnTRW5ITVJ?
human A2780 cell M3rIT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnHzTY5pcWKrdHnvckBw\iCqdX3hckBCOjd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFghdk1? MVjTRW5ITVJ?
human VA-ES-BJ cell NYjQb2RGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NE\DTWJKdmirYnn0bY9vKG:oIHj1cYFvKF[DLVXTMWJLKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57IH7N MYfTRW5ITVJ?
human BB65-RCC cell NEW5NlRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2HiVWlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ4NT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04KG6P M4f5THNCVkeHUh?=
human D-566MG cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnHPTY5pcWKrdHnvckBw\iCqdX3hckBFNTV4Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{4yPiCwTR?= MXHTRW5ITVJ?
human MDA468 cells NFvYSGRRem:uaX\ldoF1cW:wIHHzd4F6 MX2zJIRigXN? M4K4ZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBOFY5KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;ODDuUS=> MWmyNVQ{QDV5OR?=
human HO-1-N-1 cell MonjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF05NjJibl2= NFLJdXZUSU6JRWK=
human RS4-11 cell NWrxeVA2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTkTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlQ2KG6P NYLqZZdiW0GQR1XS
human PC-3 cell M3O4Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoDFTY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OT6xOEBvVQ>? MlywV2FPT0WU
human NB69 cell NFvyeGhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M130N2lvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOFYhdk1? NUO5SpBkW0GQR1XS
human HGC-27 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHlTY5pcWKrdHnvckBw\iCqdX3hckBJT0NvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlYhdk1? MnK3V2FPT0WU
human NCI-H720 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVnmV4w3UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFczOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwNkKgcm0> MnnMV2FPT0WU
human NCI-H292 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2Pad2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N NX;COpo4W0GQR1XS
human A3-KAW cell M1;X[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Moi3TY5pcWKrdHnvckBw\iCqdX3hckBCOy2NQWegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE41OyCwTR?= NGPtbGlUSU6JRWK=
human DU-4475 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkT6TY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPzNibl2= MmHxV2FPT0WU
human HuH-7 cell Mmq2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1\Zc2lvcGmkaYTpc44hd2ZiaIXtZY4hUHWKLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk4{OiCwTR?= MnO2V2FPT0WU
human J-RT3-T3-5 cell NX3x[5hXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX3T[lhmUW6qaXLpeIlwdiCxZjDoeY1idiCMLWLUN{1VOy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|ghdk1? MlGyV2FPT0WU
human VM-CUB-1 cell NYXCTI5tT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX\6NVN4UW6qaXLpeIlwdiCxZjDoeY1idiCYTT3DWWIuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lk[3JI5O NXPYTllEW0GQR1XS
human MOLT-16 cell MlnsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3;E[GlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjh2IH7N NFfxZXlUSU6JRWK=
human KG-1 cell M13KTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHi4b4JKdmirYnn0bY9vKG:oIHj1cYFvKEuJLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk46KG6P MVXTRW5ITVJ?
human P12-ICHIKAWA cell NXjkW4FnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHAyOi2LQ1jJT2FYSSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCxJI5O MlHwV2FPT0WU
human ACN cell M{Hw[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1PaU2lvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFIhdk1? NESye|RUSU6JRWK=
human COLO-684 cell M1;yd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFuzcJBKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwM{Ggcm0> Ml;DV2FPT0WU
human T-24 cell NWrXWGRXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUnodYpVUW6qaXLpeIlwdiCxZjDoeY1idiCWLUK0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvQDZibl2= M1XTRXNCVkeHUh?=
human AGS cell NVLKe|R[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFHSXGdKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P MlfIV2FPT0WU
human EW-13 cell Mlq1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3jWU2lvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PCCwTR?= NFvUZ5VUSU6JRWK=
human SW962 cell MoixS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2\GUmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU42QSCwTR?= NIDjdoNUSU6JRWK=
human EW-11 cell M{\GWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUnJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOkBvVQ>? MV;TRW5ITVJ?
human RXF393 cell M{KwUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{[4W2lvcGmkaYTpc44hd2ZiaIXtZY4hWliIM{mzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPjZibl2= M4PJWnNCVkeHUh?=
human EoL-1-cell cell NITieYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmrITY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwMTDuUS=> NV2wbXc1W0GQR1XS

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
10 mg/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
in solvent
Synonyms N/A

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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