Temsirolimus (CCI-779)

For research use only.

Licensed by Pfizer Catalog No.S1044 Synonyms: NSC 683864

56 publications

Temsirolimus (CCI-779) Chemical Structure

CAS No. 162635-04-3

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

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Selleck's Temsirolimus (CCI-779) has been cited by 56 publications

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Biological Activity

Description Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
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 NUL3Z4tQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4HyfGlvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyOyCwTR?= M1X1WHNCVkeHUh?=
human L-363 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1rNZmlvcGmkaYTpc44hd2ZiaIXtZY4hVC1|NkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1OiCwTR?= NV;1bVluW0GQR1XS
human Ramos-2G6-4C10 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnfpTY5pcWKrdHnvckBw\iCqdX3hckBT[W2xcz2yS|YuPENzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|QzKG6P MojJV2FPT0WU
human SBC-1 cell MnrXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3X5cWlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= M13XUnNCVkeHUh?=
human MHH-PREB-1 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUnUSJlxUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitVHJGSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVUhdk1? M2rOfHNCVkeHUh?=
human LNCAP cells M{eycHBzd2yrZnXyZZRqd25iYYPzZZk> NV\HR3hHOyCmYYnz NGLpd5hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;MD61JI5O NVLOeoVPOjF2M{i1O|k>
human HH cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54NkSgcm0> M3HtR3NCVkeHUh?=
human TYK-nu cell M3jqcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\2TY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc4QCCwTR?= MkHiV2FPT0WU
human H4 cell NUfuWFBPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF3KPY9KdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wO{BvVQ>? Mlu4V2FPT0WU
human K5 cell M{H5bGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHfiXHBKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zN{BvVQ>? NX;sNnVkW0GQR1XS
human PA-1 cell MorzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnrpTY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? M3fidXNCVkeHUh?=
human SK-NEP-1 cell M1TSPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlTqTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QRWCtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDlibl2= M1zl[XNCVkeHUh?=
human 697 cell M3rvZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jqfGlvcGmkaYTpc44hd2ZiaIXtZY4hPjl5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63JI5O MonXV2FPT0WU
human CTB-1 cell M4\BdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWDJcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65N{BvVQ>? MknLV2FPT0WU
human DB cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2XDOWlvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O MYrTRW5ITVJ?
human MLMA cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYLlVFdEUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= NF;jUmRUSU6JRWK=
human GAMG cell NVHISVJiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH21dYFKdmirYnn0bY9vKG:oIHj1cYFvKEeDTVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlgzKG6P NGTJTlBUSU6JRWK=
human JVM-3 cell NVfaUZJ4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX3OO25iUW6qaXLpeIlwdiCxZjDoeY1idiCMVl2tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTVibl2= MlPmV2FPT0WU
human LAMA-84 cell Ml3VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HZRmlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODNibl2= MVHTRW5ITVJ?
human RPMI-8226 cell NIn5fHZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1PBO2lvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST24NlI3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5zNTDuUS=> MoXyV2FPT0WU
human MOLT-4 cell M3nGdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUHJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuN|Ehdk1? NWO1O|ZQW0GQR1XS
human CAMA-1 cell MoW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnXhTY5pcWKrdHnvckBw\iCqdX3hckBESU2DLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc4KG6P NUHvUGxlW0GQR1XS
human NCI-SNU-1 cell M4Tlbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHizUnFKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEGgcm0> NFXUXWhUSU6JRWK=
human SW780 cell NIrjRmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVjJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64N{BvVQ>? M4mzPXNCVkeHUh?=
human H9 cell NHXuXHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnXLTY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEigcm0> Ml7oV2FPT0WU
human BE-13 cell NFu1OmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkfFTY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVEhdk1? M1G0W3NCVkeHUh?=
human ES8 cell MoDSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGVUQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwMkegcm0> Mli3V2FPT0WU
human DEL cell NFTrUYJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoL1TY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O NXLZUXFoW0GQR1XS
human QIMR-WIL cell M{T2TWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LV[mlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjdzIH7N M3Tq[XNCVkeHUh?=
human CGTH-W-1 cell NXLEUXRzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWLJcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44PSCwTR?= MVLTRW5ITVJ?
human CHL-1 cell M3jCbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnmxTY5pcWKrdHnvckBw\iCqdX3hckBEUExvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFYhdk1? NHHCOJVUSU6JRWK=
human A2780 cell NIPSV|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{G0TGlvcGmkaYTpc44hd2ZiaIXtZY4hSTJ5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg5KG6P MoLZV2FPT0WU
human VA-ES-BJ cell M1TLfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NU[we21TUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> M2CzVXNCVkeHUh?=
human BB65-RCC cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MljXTY5pcWKrdHnvckBw\iCqdX3hckBDSjZ3LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVchdk1? M1fFPXNCVkeHUh?=
human D-566MG cell M2LBfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\VTY5pcWKrdHnvckBw\iCqdX3hckBFNTV4Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{4yPiCwTR?= MU\TRW5ITVJ?
human MDA468 cells MojRVJJwdGmoZYLheIlwdiCjc4PhfS=> NInveGQ{KGSjeYO= MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQUS2PEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRThibl2= MlX4NlE1Ozh3N{m=
human HO-1-N-1 cell MkXTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFnufGNKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> NEO4SnNUSU6JRWK=
human RS4-11 cell M1Hjb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYG1V5FRUW6qaXLpeIlwdiCxZjDoeY1idiCUU{StNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR3IH7N M1HvenNCVkeHUh?=
human PC-3 cell M{jwTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MorETY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OT6xOEBvVQ>? MV\TRW5ITVJ?
human NB69 cell MmC0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NECyR|BKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ3KG6P M3S2OnNCVkeHUh?=
human HGC-27 cell NVX0ZmJoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkHNTY5pcWKrdHnvckBw\iCqdX3hckBJT0NvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlYhdk1? M2jQdHNCVkeHUh?=
human NCI-H720 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIn0NY1KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|IxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS54MjDuUS=> MnLuV2FPT0WU
human NCI-H292 cell NWq1U4g4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\IXVB2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwOESgcm0> MonFV2FPT0WU
human A3-KAW cell MoHXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKGi3bXHuJGE{NUuDVzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlQ{KG6P NXrDcpprW0GQR1XS
human DU-4475 cell M1;ZWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHvLTGVKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS55MzDuUS=> NYrHNodyW0GQR1XS
human HuH-7 cell NFzXS3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{TBUmlvcGmkaYTpc44hd2ZiaIXtZY4hUHWKLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk4{OiCwTR?= MVLTRW5ITVJ?
human J-RT3-T3-5 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M33NWGlvcGmkaYTpc44hd2ZiaIXtZY4hUi2UVEOtWFMuPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{LkO4JI5O M1THPHNCVkeHUh?=
human VM-CUB-1 cell NGTiR2pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFflb|RKdmirYnn0bY9vKG:oIHj1cYFvKF[PLVPVRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkegcm0> M4\VOXNCVkeHUh?=
human MOLT-16 cell NWnRblV3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkLITY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvQDRibl2= MX3TRW5ITVJ?
human KG-1 cell NXTX[Ih{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2TxeGlvcGmkaYTpc44hd2ZiaIXtZY4hU0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlkhdk1? NVPibHhVW0GQR1XS
human P12-ICHIKAWA cell Mm\IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJHAyOi2LQ1jJT2FYSSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCxJI5O MXrTRW5ITVJ?
human ACN cell M2i3[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWP4WHpiUW6qaXLpeIlwdiCxZjDoeY1idiCDQ16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOiCwTR?= NHXaO3hUSU6JRWK=
human COLO-684 cell NWrRdXJWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2fGfmlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22PFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy5|MTDuUS=> M{nFUnNCVkeHUh?=
human T-24 cell NXf3cIVPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHTpe5NKdmirYnn0bY9vKG:oIHj1cYFvKFRvMkSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{45PiCwTR?= NVHZXVdPW0GQR1XS
human AGS cell NXfV[HhTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF\4XFVKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P MXTTRW5ITVJ?
human EW-13 cell MonFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2S0WGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PCCwTR?= NVrWNZBlW0GQR1XS
human SW962 cell Ml7tS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOVkhdk1? NG\W[VJUSU6JRWK=
human EW-11 cell MlTrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOkBvVQ>? NFztTI9USU6JRWK=
human RXF393 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmLFTY5pcWKrdHnvckBw\iCqdX3hckBTYEZ|OUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU43PiCwTR?= NHHsN2ZUSU6JRWK=
human EoL-1-cell cell NX\vT5JlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX\ydFJsUW6qaXLpeIlwdiCxZjDoeY1idiCHb1ytNU1k\WyuIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MU[uNUBvVQ>? NWr0OmVkW0GQR1XS

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-mTOR / mTOR / p-S6 / S6 / p-4E-BP1 / 4E-BP1 ; 

PubMed: 23291985     


The mTOR inhibitor temsirolimus inhibits the activation of mTOR and its downstream molecules in esophageal cancer cells. Three esophageal cancer cell lines (TE-1, TE-8, and TE-10) were treated with different concentrations of temsirolimus (0–1000nM) and western blot was performed with appropriate antibodies to detect the expression of mTOR and its downstream effectors. β-actin was served as an internal control.

p-rS6 / rS6 / p-AKT /AKT ; 

PubMed: 22039466     


C, D, Phosphorylation of rS6 (P-rS6) and Akt (P-Akt T308 and P-Akt S473) after treatment with indicated doses of temsirolimus for 72 hrs in temsirolimus-sensitive (C) or temsirolimus-resistant (D) cells was determined by Western blotting. Expression of total rS6 and Akt protein serves as loading controls.

23291985 22039466
Immunofluorescence
NRF2; 

PubMed: 22848625     


Ectopic expression of Nrf2 (red) and nuclear staining with Dapi (blue) after a 6 hour drug incubation. Yellow numbers represent the percent of cells with nuclear Nrf2 +/− the standard deviation. Scale bar = 10 µM.

22848625
Growth inhibition assay
Cell growth (HGC-3 cells) ; 

PubMed: 30866995     


Effect of temsirolimus on the growth of HGC-3 and -20 cells in primary culture. 

Cell viability ; 

PubMed: 22039466     


A, B, Endometrial cancer cells were treated with increasing doses of temsirolimus for 72 hrs. Results are separated by (A) sensitivity or (B) resistance as determined by cell viability. 

30866995 22039466
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
  • Dosages: 20 mg/kg
  • Administration: Injection daily 5 times per week
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 67 mg/mL (65.03 mM)
Water Insoluble
Ethanol '75 mg/mL
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 NSC 683864
Smiles CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OC(=O)C(C)(CO)CO)C)C)O)OC)C)C)C)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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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 )

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    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):
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    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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01653067 Unknown status Drug: Rituximab Temsirolimus DHAP intravenous Diffuse Large B-Cell Lymphoma Mathias Witzens-Harig|Johannes Gutenberg University Mainz|Technische Universität München|Ludwig-Maximilians - University of Munich|University Hospital Ulm|University Hospital Erlangen|Charite University Berlin Germany|University Hospital Freiburg|Johann Wolfgang Goethe University Hospital|University Hospital Heidelberg September 2012 Phase 2
NCT02093598 Completed Drug: Temsirolimus Carcinoma Endometrioid|mTOR Protein MedSIR May 2012 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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID