Temsirolimus (CCI-779)

For research use only.

Licensed by Pfizer Catalog No.S1044 Synonyms: NSC 683864

48 publications

Temsirolimus (CCI-779) 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. Temsirolimus induces autophagy and apoptosis.

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Selleck's Temsirolimus (CCI-779) has been cited by 48 publications

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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. 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 MnuwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHnWfmJKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTNibl2= MnvOV2FPT0WU
human L-363 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TZO2lvcGmkaYTpc44hd2ZiaIXtZY4hVC1|NkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1OiCwTR?= MlvjV2FPT0WU
human Ramos-2G6-4C10 cell M4PsU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH7kdYRKdmirYnn0bY9vKG:oIHj1cYFvKFKjbX;zMVJIPi12Q{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PDJibl2= MX\TRW5ITVJ?
human SBC-1 cell NH:4PJpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3n6UmlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= MnzKV2FPT0WU
human MHH-PREB-1 cell M1XMTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnzSTY5pcWKrdHnvckBw\iCqdX3hckBOUEhvUGLFRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OUWgcm0> NIjXcVRUSU6JRWK=
human LNCAP cells MmXaVJJwdGmoZYLheIlwdiCjc4PhfS=> MVGzJIRigXN? MnraRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOTlPBVEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRTBwNTDuUS=> M{PlUFIyPDN6NUe5
human HH cell NEWxWpBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54NkSgcm0> MV3TRW5ITVJ?
human TYK-nu cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHLrdmtKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzd6IH7N MkPtV2FPT0WU
human H4 cell MlzRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVLhWJdNUW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFchdk1? M{L3VnNCVkeHUh?=
human K5 cell NYPNbIhUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXK2T2xwUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Mhdk1? MYHTRW5ITVJ?
human PA-1 cell MleyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlPpTY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? NHfNemxUSU6JRWK=
human SK-NEP-1 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWXJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU6HUD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41QSCwTR?= MXvTRW5ITVJ?
human 697 cell Mm\JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;BWpZ{UW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlchdk1? MUPTRW5ITVJ?
human CTB-1 cell MlvqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65N{BvVQ>? MnThV2FPT0WU
human DB cell NF3ZVJdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3nH[WlvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O MnTMV2FPT0WU
human MLMA cell NFfqOHZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV3xeotwUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= NUDs[49GW0GQR1XS
human GAMG cell M4TkPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkPxTY5pcWKrdHnvckBw\iCqdX3hckBISU2JIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz64NkBvVQ>? M3ryZnNCVkeHUh?=
human JVM-3 cell M4rZSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHvtVGRKdmirYnn0bY9vKG:oIHj1cYFvKEqYTT2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTR?= MkH0V2FPT0WU
human LAMA-84 cell Mnu3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHXGOoNKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB|IH7N M4mwWXNCVkeHUh?=
human RPMI-8226 cell NVzZSJFJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWHJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvOEKyOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTVibl2= Mnz4V2FPT0WU
human MOLT-4 cell NIK1eZJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{DybGlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{OSCwTR?= MmjoV2FPT0WU
human CAMA-1 cell M3rzV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGNCVUFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|chdk1? M{PQVXNCVkeHUh?=
human NCI-SNU-1 cell M32zSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYeyPIcxUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkixJI5O NGr4cIpUSU6JRWK=
human SW780 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2[3PGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{KG6P NGfpNHNUSU6JRWK=
human H9 cell MnrqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVnJcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56ODDuUS=> MorxV2FPT0WU
human BE-13 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGHsSGRKdmirYnn0bY9vKG:oIHj1cYFvKEKHLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46OSCwTR?= MnThV2FPT0WU
human ES8 cell Mlu3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIHwTWJKdmirYnn0bY9vKG:oIHj1cYFvKEWVODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNlchdk1? MX7TRW5ITVJ?
human DEL cell NEDNZpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGRGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNE[gcm0> MUTTRW5ITVJ?
human QIMR-WIL cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1rGWWlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjdzIH7N MX;TRW5ITVJ?
human CGTH-W-1 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWnnXXlnUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Wgcm0> NVHsbFhlW0GQR1XS
human CHL-1 cell M1LMVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? MXLTRW5ITVJ?
human A2780 cell M4LrTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJGEzPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64PEBvVQ>? NEfLRZZUSU6JRWK=
human VA-ES-BJ cell NF\6b4ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXO4TFFYUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> NGjxT|RUSU6JRWK=
human BB65-RCC cell NXyyeXRCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHzmSolKdmirYnn0bY9vKG:oIHj1cYFvKEKENkWtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PyCwTR?= NI\NdpFUSU6JRWK=
human D-566MG cell MoDnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVLJcohq[mm2aX;uJI9nKGi3bXHuJGQuPTZ4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23MlE3KG6P MlrSV2FPT0WU
human MDA468 cells M4XpdHBzd2yrZnXyZZRqd25iYYPzZZk> NHn6SFk{KGSjeYO= MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQUS2PEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRThibl2= MYGyNVQ{QDV5OR?=
human HO-1-N-1 cell MnT4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIPISnBKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> MXzTRW5ITVJ?
human RS4-11 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2jPeGlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE41PSCwTR?= NVPXTFRHW0GQR1XS
human PC-3 cell NHvhUHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHBENTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkG0JI5O M3GzUnNCVkeHUh?=
human NB69 cell MmO3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkS2JI5O NVX2XYtRW0GQR1XS
human HGC-27 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWPQN4dxUW6qaXLpeIlwdiCxZjDoeY1idiCKR1OtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZibl2= NGjweo1USU6JRWK=
human NCI-H720 cell M4XiN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUXBXHlTUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFczOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwNkKgcm0> M332[XNCVkeHUh?=
human NCI-H292 cell MojwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEfjfFBKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS56NDDuUS=> M37kXnNCVkeHUh?=
human A3-KAW cell NHWyc|lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGE{NUuDVzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlQ{KG6P MYPTRW5ITVJ?
human DU-4475 cell NWfZNoFqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoPjTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPzNibl2= Ml;hV2FPT0WU
human HuH-7 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUn0WJRxUW6qaXLpeIlwdiCxZjDoeY1idiCKdVitO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjN{IH7N M1niSnNCVkeHUh?=
human J-RT3-T3-5 cell NWPXWo5nT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXvJcohq[mm2aX;uJI9nKGi3bXHuJGouWlR|LWSzMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|ODDuUS=> NX3UPWkyW0GQR1XS
human VM-CUB-1 cell M3PJeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVfYco82UW6qaXLpeIlwdiCxZjDoeY1idiCYTT3DWWIuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lk[3JI5O MkDOV2FPT0WU
human MOLT-16 cell NH\SO5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1TPd2lvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjh2IH7N NHrYclVUSU6JRWK=
human KG-1 cell NETrWHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYPJcohq[mm2aX;uJI9nKGi3bXHuJGtINTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj65JI5O MmP0V2FPT0WU
human P12-ICHIKAWA cell M17ye2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXT6S3BCUW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOSCwTR?= M2\mcHNCVkeHUh?=
human ACN cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofOTY5pcWKrdHnvckBw\iCqdX3hckBCS05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNkBvVQ>? NHPSfIFUSU6JRWK=
human COLO-684 cell NEi3[nJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFLPZYhKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwM{Ggcm0> MnflV2FPT0WU
human T-24 cell M1jGV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHzCN2lKdmirYnn0bY9vKG:oIHj1cYFvKFRvMkSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{45PiCwTR?= M4D5cXNCVkeHUh?=
human AGS cell M4PQNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYrJcohq[mm2aX;uJI9nKGi3bXHuJGFIWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2LkGxJI5O NWe3T3pDW0GQR1XS
human EW-13 cell MkDhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkHMTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlU1KG6P MoPkV2FPT0WU
human SW962 cell NGrRfIFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUTvTGl1UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjV7IH7N M4j6R3NCVkeHUh?=
human EW-11 cell Mn7JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV73UpVQUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZibl2= MWjTRW5ITVJ?
human RXF393 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYfJcohq[mm2aX;uJI9nKGi3bXHuJHJZTjN7MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlY3KG6P Mm\nV2FPT0WU
human EoL-1-cell cell M3rrSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3Htb2lvcGmkaYTpc44hd2ZiaIXtZY4hTW:OLUGtZ4VtdCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4LkGgcm0> NV\WUIlZW0GQR1XS

... 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 COC1CC(CCC1OC(=O)C(C)(CO)CO)CC(C)C2CC(=O)C(C)\C=C(C)\C(O)C(OC)C(=O)C(C)CC(C)/C=C/C=C/C=C(C)/C(CC3CCC(C)C(O)(O3)C(=O)C(=O)N4CCCCC4C(=O)O2)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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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)

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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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* 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):
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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID