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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Cited by 24 Publications

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 Ml;US5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGLmTmVKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTNibl2= NHTtXFhUSU6JRWK=
human L-363 cell MnL2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV[1U3BRUW6qaXLpeIlwdiCxZjDoeY1idiCOLUO2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjR{IH7N MX3TRW5ITVJ?
human Ramos-2G6-4C10 cell MknHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4LmV2lvcGmkaYTpc44hd2ZiaIXtZY4hWmGvb4OtNmc3NTSFMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM1OiCwTR?= MYrTRW5ITVJ?
human SBC-1 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1;1eWlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= MYjTRW5ITVJ?
human MHH-PREB-1 cell MmHvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmDzTY5pcWKrdHnvckBw\iCqdX3hckBOUEhvUGLFRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OUWgcm0> NIHsOI9USU6JRWK=
human LNCAP cells M3\WSHBzd2yrZnXyZZRqd25iYYPzZZk> NVzGc5BQOyCmYYnz MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGOgZZN{[XluIFnDOVA:OC53IH7N NYK0W2xvOjF2M{i1O|k>
human HH cell NFzxWXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1TY[WlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[2OEBvVQ>? MWXTRW5ITVJ?
human TYK-nu cell NWXGZVJUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mm\kTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc4QCCwTR?= Ml\HV2FPT0WU
human H4 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3PTUWlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC3JI5O M3y4NnNCVkeHUh?=
human K5 cell NXTuUIRkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1vGXmlvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOzJI5O M{nIVnNCVkeHUh?=
human PA-1 cell MlvSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHqTY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? MWHTRW5ITVJ?
human SK-NEP-1 cell MoX3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3zFNmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTlXQMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR7IH7N MXLTRW5ITVJ?
human 697 cell NWDwOXgyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFHxfpNKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO{BvVQ>? MmW3V2FPT0WU
human CTB-1 cell MmXRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlfUTY5pcWKrdHnvckBw\iCqdX3hckBEXEJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVMhdk1? MlLzV2FPT0WU
human DB cell MnTsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{exTmlvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O M4HyN3NCVkeHUh?=
human MLMA cell NY\nZpBtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJG1NVUFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkOxJI5O MoCzV2FPT0WU
human GAMG cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml24TY5pcWKrdHnvckBw\iCqdX3hckBISU2JIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz64NkBvVQ>? NHHWbIVUSU6JRWK=
human JVM-3 cell NVXJfWRoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NITp[GlKdmirYnn0bY9vKG:oIHj1cYFvKEqYTT2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTR?= NFnZenZUSU6JRWK=
human LAMA-84 cell NG\PSIpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{LF[mlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODNibl2= NETt[IJUSU6JRWK=
human RPMI-8226 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Moj6TY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUiyNlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjF3IH7N NFu1S41USU6JRWK=
human MOLT-4 cell NVThUW5tT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXvUN5FjUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjNzIH7N NF63SI9USU6JRWK=
human CAMA-1 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml;BTY5pcWKrdHnvckBw\iCqdX3hckBESU2DLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc4KG6P M2nIOnNCVkeHUh?=
human NCI-SNU-1 cell NUXuPYdTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH:0NJNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEGgcm0> NW\N[Fh1W0GQR1XS
human SW780 cell M4HMNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVTQTHlMUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDNibl2= NUPDeoZ6W0GQR1XS
human H9 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEja[ldKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64PEBvVQ>? NX[4XYdmW0GQR1XS
human BE-13 cell Mmr5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkHtTY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVEhdk1? NUX0eWVSW0GQR1XS
human ES8 cell MmjRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWrobIFZUW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlI4KG6P MUDTRW5ITVJ?
human DEL cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnzNTY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O Mmj5V2FPT0WU
human QIMR-WIL cell NHLt[nlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWrlfW5ZUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Ggcm0> MWHTRW5ITVJ?
human CGTH-W-1 cell MkDLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUD3[YVPUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Wgcm0> Mn\BV2FPT0WU
human CHL-1 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? NHzaZmNUSU6JRWK=
human A2780 cell NYm2fHBxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnT2TY5pcWKrdHnvckBw\iCqdX3hckBCOjd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFghdk1? NFXuc3pUSU6JRWK=
human VA-ES-BJ cell MkHuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUK5eHhNUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> NHO1SYhUSU6JRWK=
human BB65-RCC cell NHW2e5hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnfYTY5pcWKrdHnvckBw\iCqdX3hckBDSjZ3LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVchdk1? NUfvWWFUW0GQR1XS
human D-566MG cell MoT1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH35codKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjF4IH7N MWnTRW5ITVJ?
human MDA468 cells M1HaVXBzd2yrZnXyZZRqd25iYYPzZZk> MX:zJIRigXN? MoLlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFG0Olgh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD16IH7N M3XR[VIyPDN6NUe5
human HO-1-N-1 cell M{K2Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFfVb5BKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> MlrpV2FPT0WU
human RS4-11 cell NHzvR2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLMZ3A4UW6qaXLpeIlwdiCxZjDoeY1idiCUU{StNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR3IH7N M2e3OHNCVkeHUh?=
human PC-3 cell NVzuSG1tT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2S4UmlvcGmkaYTpc44hd2ZiaIXtZY4hWENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuNVQhdk1? MUnTRW5ITVJ?
human NB69 cell Ml;rS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkS2JI5O M1jyTnNCVkeHUh?=
human HGC-27 cell NYHmPZp2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWLJcohq[mm2aX;uJI9nKGi3bXHuJGhISy1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOkBvVQ>? MUnTRW5ITVJ?
human NCI-H720 cell M3XDcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV;Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{KwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU43OiCwTR?= Mnf6V2FPT0WU
human NCI-H292 cell NX;oWIZCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU45PCCwTR?= MYHTRW5ITVJ?
human A3-KAW cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoriTY5pcWKrdHnvckBw\iCqdX3hckBCOy2NQWegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE41OyCwTR?= Mn3LV2FPT0WU
human DU-4475 cell MmWxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MULJcohq[mm2aX;uJI9nKGi3bXHuJGRWNTR2N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU44OyCwTR?= NETleY5USU6JRWK=
human HuH-7 cell NU\5bYpuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVjJcohq[mm2aX;uJI9nKGi3bXHuJGh2UC15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|Ihdk1? NVnxWlZqW0GQR1XS
human J-RT3-T3-5 cell NIPST3pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoWxTY5pcWKrdHnvckBw\iCqdX3hckBLNVKWMz3UN{02KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwM{igcm0> M{nmRnNCVkeHUh?=
human VM-CUB-1 cell NFHmTJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlLvTY5pcWKrdHnvckBw\iCqdX3hckBXVS2FVVKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjZ5IH7N MWDTRW5ITVJ?
human MOLT-16 cell NFr1dZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXvJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk45PCCwTR?= NHzmSJpUSU6JRWK=
human KG-1 cell MkLDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEW3b2pKdmirYnn0bY9vKG:oIHj1cYFvKEuJLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk46KG6P NXfJbHlIW0GQR1XS
human P12-ICHIKAWA cell M1\IbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYrJcohq[mm2aX;uJI9nKGi3bXHuJHAyOi2LQ1jJT2FYSSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCxJI5O NHTPNWhUSU6JRWK=
human ACN cell NUjhbo5oT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1HQ[mlvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFIhdk1? MXLTRW5ITVJ?
human COLO-684 cell NH\nSXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYLPUGN6UW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY5PCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkOxJI5O M2jMN3NCVkeHUh?=
human T-24 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NW\kTWN3UW6qaXLpeIlwdiCxZjDoeY1idiCWLUK0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvQDZibl2= NETmOlZUSU6JRWK=
human AGS cell M1fUfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NU\xPFg5UW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE4yOSCwTR?= NVmxR3ZIW0GQR1XS
human EW-13 cell M1\WW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{H0XGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PCCwTR?= NUfUOFZOW0GQR1XS
human SW962 cell NXjhN2V1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUnJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOVkhdk1? M3fs[3NCVkeHUh?=
human EW-11 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXLJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOkBvVQ>? NHj6V4ZUSU6JRWK=
human RXF393 cell M33zTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUnBPXo{UW6qaXLpeIlwdiCxZjDoeY1idiCUWF[zPVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS54NjDuUS=> MYPTRW5ITVJ?
human EoL-1-cell cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnrhTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwMTDuUS=> M3;JNnNCVkeHUh?=

... 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]

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  • 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]

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  • 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
NCT03203525 Not yet recruiting Liver Cancer M.D. Anderson Cancer Center|NovoCure Ltd. February 2019 Phase 1
NCT03203525 Not yet recruiting Liver Cancer M.D. Anderson Cancer Center|NovoCure Ltd. February 2019 Phase 1
NCT03158389 Recruiting Glioblastoma Adult University Hospital Heidelberg|German Cancer Aid|German Cancer Research Center|National Center for Tumor Diseases Heidelberg May 7 2018 Phase 1|Phase 2
NCT03158389 Recruiting Glioblastoma Adult University Hospital Heidelberg|German Cancer Aid|German Cancer Research Center|National Center for Tumor Diseases Heidelberg May 7 2018 Phase 1|Phase 2
NCT03571438 Recruiting Kidney Cancer University Hospital Grenoble October 16 2017 Not Applicable
NCT03297606 Recruiting Lymphoma Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors Canadian Cancer Trials Group|AstraZeneca|Bristol-Myers Squibb|Hoffmann-La Roche|Pfizer October 6 2017 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID