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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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 NHXZ[GRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnXsTY5pcWKrdHnvckBw\iCqdX3hckBJW0NvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE{KG6P M1TNdXNCVkeHUh?=
human L-363 cell Ml;TS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWDCOmZFUW6qaXLpeIlwdiCxZjDoeY1idiCOLUO2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjR{IH7N NX\1dJZ7W0GQR1XS
human Ramos-2G6-4C10 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFj4bmJKdmirYnn0bY9vKG:oIHj1cYFvKFKjbX;zMVJIPi12Q{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PDJibl2= MU\TRW5ITVJ?
human SBC-1 cell NU\0SVhQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHLFc3NKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PDRibl2= NEXaOHJUSU6JRWK=
human MHH-PREB-1 cell M2fLemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml7TTY5pcWKrdHnvckBw\iCqdX3hckBOUEhvUGLFRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OUWgcm0> M{HpS3NCVkeHUh?=
human LNCAP cells MXjQdo9tcW[ncnH0bY9vKGG|c3H5 Mk\sN{Bl[Xm| MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGOgZZN{[XluIFnDOVA:OC53IH7N NEHYWG4zOTR|OEW3PS=>
human HH cell M1rzT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkPITY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNk[0JI5O MXzTRW5ITVJ?
human TYK-nu cell NH;xe5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHPYOG1KdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzd6IH7N MX\TRW5ITVJ?
human H4 cell MoTNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{\LemlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC3JI5O NHGyeoZUSU6JRWK=
human K5 cell Mn3LS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYfRc|RoUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Mhdk1? NFHx[5ZUSU6JRWK=
human PA-1 cell Mo[1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoPBTY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? M4HF[HNCVkeHUh?=
human SK-NEP-1 cell MoSxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFrMWnFKdmirYnn0bY9vKG:oIHj1cYFvKFONLV7FVE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52OTDuUS=> M2T3WnNCVkeHUh?=
human 697 cell M4facmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWrjTlFHUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlchdk1? M{XGe3NCVkeHUh?=
human CTB-1 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnzITY5pcWKrdHnvckBw\iCqdX3hckBEXEJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVMhdk1? M{jQUXNCVkeHUh?=
human DB cell NUfNOYtWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3GxdWlvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O MkXtV2FPT0WU
human MLMA cell NW\1RXpxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlzkTY5pcWKrdHnvckBw\iCqdX3hckBOVE2DIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6zNUBvVQ>? M33CdXNCVkeHUh?=
human GAMG cell NEPzNlNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJGdCVUdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkiyJI5O NHvaOYdUSU6JRWK=
human JVM-3 cell NX7nb3B[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkfoTY5pcWKrdHnvckBw\iCqdX3hckBLXk1vMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVUhdk1? MWDTRW5ITVJ?
human LAMA-84 cell NIHWRmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIK2PHpKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB|IH7N MXLTRW5ITVJ?
human RPMI-8226 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmjETY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUiyNlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjF3IH7N NHnJVWlUSU6JRWK=
human MOLT-4 cell MnPvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkjCTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlMyKG6P NFL4SlJUSU6JRWK=
human CAMA-1 cell M2P3bWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1PrWGlvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44PyCwTR?= MmLQV2FPT0WU
human NCI-SNU-1 cell NWCyRZl5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGLGZndKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEGgcm0> NVrvVFF5W0GQR1XS
human SW780 cell M{nY[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIPqO3pKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45OyCwTR?= NVrQTJN1W0GQR1XS
human H9 cell M1OxPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnxfJF1UW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFghdk1? MXzTRW5ITVJ?
human BE-13 cell MojoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHNTY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVEhdk1? NIPaeZVUSU6JRWK=
human ES8 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEPJPHJKdmirYnn0bY9vKG:oIHj1cYFvKEWVODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNlchdk1? MkXKV2FPT0WU
human DEL cell NVLRcYs6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn20TY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O MYfTRW5ITVJ?
human QIMR-WIL cell MnLuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{D4S2lvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjdzIH7N NWe4[lhzW0GQR1XS
human CGTH-W-1 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWewdWRwUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Wgcm0> NVLGPFFZW0GQR1XS
human CHL-1 cell NWnld5dYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmSxTY5pcWKrdHnvckBw\iCqdX3hckBEUExvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFYhdk1? M3;vPXNCVkeHUh?=
human A2780 cell NHzHWmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWfke3VuUW6qaXLpeIlwdiCxZjDoeY1idiCDMke4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDhibl2= M1HxWHNCVkeHUh?=
human VA-ES-BJ cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoDXTY5pcWKrdHnvckBw\iCqdX3hckBXSS2HUz3CTkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQSCwTR?= NHfuZXVUSU6JRWK=
human BB65-RCC cell M3LW[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVX0fmZOUW6qaXLpeIlwdiCxZjDoeY1idiCEQk[1MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdibl2= MmfLV2FPT0WU
human D-566MG cell M1npUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHz0dpBKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjF4IH7N NEnqNlFUSU6JRWK=
human MDA468 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 M{fXbVMh\GG7cx?= M1y3NGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBOFY5KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;ODDuUS=> M2XRU|IyPDN6NUe5
human HO-1-N-1 cell M3zrfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUXJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF05NjJibl2= MmrsV2FPT0WU
human RS4-11 cell M2raZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOFUhdk1? MmTjV2FPT0WU
human PC-3 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEHEVIpKdmirYnn0bY9vKG:oIHj1cYFvKFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlE1KG6P M371OnNCVkeHUh?=
human NB69 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFTRbXZKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ3KG6P M3eyXXNCVkeHUh?=
human HGC-27 cell MoXnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M37WW2lvcGmkaYTpc44hd2ZiaIXtZY4hUEeFLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU43KG6P NFn5XppUSU6JRWK=
human NCI-H720 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVzJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{KwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU43OiCwTR?= MmnlV2FPT0WU
human NCI-H292 cell NGfHZYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3jlTGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N MW\TRW5ITVJ?
human A3-KAW cell M1LkOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn\uTY5pcWKrdHnvckBw\iCqdX3hckBCOy2NQWegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE41OyCwTR?= MX3TRW5ITVJ?
human DU-4475 cell M{XqPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mmm1TY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPzNibl2= NVvTWGk5W0GQR1XS
human HuH-7 cell NELOd2JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFm1dmtKdmirYnn0bY9vKG:oIHj1cYFvKEi3SD23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvOzJibl2= NV33UZRoW0GQR1XS
human J-RT3-T3-5 cell NEe1T25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGTrR3VKdmirYnn0bY9vKG:oIHj1cYFvKEpvUmSzMXQ{NTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj6zPEBvVQ>? NFPlZnRUSU6JRWK=
human VM-CUB-1 cell MljvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFTzd25KdmirYnn0bY9vKG:oIHj1cYFvKF[PLVPVRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkegcm0> M2LFUnNCVkeHUh?=
human MOLT-16 cell NIi5d4JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{O3VmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjh2IH7N M2C4RXNCVkeHUh?=
human KG-1 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1Hn[GlvcGmkaYTpc44hd2ZiaIXtZY4hU0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlkhdk1? MUPTRW5ITVJ?
human P12-ICHIKAWA cell MkDLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYPNZ4RXUW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOSCwTR?= NFSyU3BUSU6JRWK=
human ACN cell NGPUOVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVfJcohq[mm2aX;uJI9nKGi3bXHuJGFEViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCyJI5O Mnr6V2FPT0WU
human COLO-684 cell NFHZeXVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkjNTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjNzIH7N NUPkOHZVW0GQR1XS
human T-24 cell NX;DPG04T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3HpSWlvcGmkaYTpc44hd2ZiaIXtZY4hXC1{NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlg3KG6P MU\TRW5ITVJ?
human AGS cell NFfsVHVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnLKTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND6xNUBvVQ>? MYTTRW5ITVJ?
human EW-13 cell NYmxN3JXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1:xeGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PCCwTR?= MUnTRW5ITVJ?
human SW962 cell MlrSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVnaNoVkUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjV7IH7N MXvTRW5ITVJ?
human EW-11 cell NUHlXmduT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkHOTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlYhdk1? MkT0V2FPT0WU
human RXF393 cell M3Lme2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWLabolLUW6qaXLpeIlwdiCxZjDoeY1idiCUWF[zPVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS54NjDuUS=> MU\TRW5ITVJ?
human EoL-1-cell cell M{TW[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWPJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi5zIH7N NFvh[pJUSU6JRWK=

... 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(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01010126 Completed Adult Hepatocellular Carcinoma|Advanced Adult Hepatocellular Carcinoma|Endometrial Serous Adenocarcinoma|Localized Non-Resectable Adult Liver Carcinoma|Lung Carcinoid Tumor|Malignant Pancreatic Gastrinoma|Malignant Pancreatic Glucagonoma|Malignant Pancreatic Insulinoma|Malignant Pancreatic Somatostatinoma|Metastatic Digestive System Neuroendocrine Tumor G1|Ovarian Carcinosarcoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Surface Papillary Adenocarcinoma|Pancreatic Alpha Cell Adenoma|Pancreatic Beta Cell Adenoma|Pancreatic Delta Cell Adenoma|Pancreatic G-Cell Adenoma|Pancreatic Polypeptide Tumor|Recurrent Adult Liver Carcinoma|Recurrent Digestive System Neuroendocrine Tumor G1|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Pancreatic Neuroendocrine Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma|Regional Digestive System Neuroendocrine Tumor G1|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Primary Peritoneal Cancer|Stage IIIA Uterine Corpus Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Primary Peritoneal Cancer|Stage IIIB Uterine Corpus Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Cancer|Stage IIIC Primary Peritoneal Cancer|Stage IIIC Uterine Corpus Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer|Stage IVA Uterine Corpus Cancer|Stage IVB Uterine Corpus Cancer|Uterine Carcinosarcoma National Cancer Institute (NCI) September 8 2009 Phase 2
NCT00703625 Completed Resistant Solid Malignancies Washington University School of Medicine March 8 2008 Phase 1
NCT02389309 Recruiting Solid Tumors M.D. Anderson Cancer Center October 5 2015 Phase 1
NCT01687673 Active not recruiting Hepatocellular Carcinoma University of California San Francisco|Robert H. Lurie Cancer Center|Pfizer October 5 2012 Phase 2
NCT00700258 Recruiting Carcinoma Renal Cell Advanced|Lymphoma Mantle-Cell|Gastrointestinal Stroma Tumors Pfizer January 4 2008 --
NCT00699491 Completed Male Breast Carcinoma|Recurrent Breast Carcinoma|Stage IV Breast Cancer AJCC v6 and v7 National Cancer Institute (NCI) October 31 2008 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID