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 32 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 MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIfwZWdKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTNibl2= NET1W2lUSU6JRWK=
human L-363 cell NEXqTJdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXWRmV5UW6qaXLpeIlwdiCxZjDoeY1idiCOLUO2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjR{IH7N NVGyVHdrW0GQR1XS
human Ramos-2G6-4C10 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1T4e2lvcGmkaYTpc44hd2ZiaIXtZY4hWmGvb4OtNmc3NTSFMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM1OiCwTR?= NID5W3ZUSU6JRWK=
human SBC-1 cell NIPYSIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2rtd2lvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= MnXQV2FPT0WU
human MHH-PREB-1 cell M3jM[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEPvbnFKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3QVmVDNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5OUBvVQ>? NGriflBUSU6JRWK=
human LNCAP cells M1foTnBzd2yrZnXyZZRqd25iYYPzZZk> M4r0XlMh\GG7cx?= NIS1[|RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;MD61JI5O MlvRNlE1Ozh3N{m=
human HH cell NGHI[VVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEOwWlhKdmirYnn0bY9vKG:oIHj1cYFvKEiKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62OlQhdk1? NGj2OopUSU6JRWK=
human TYK-nu cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEDwN2RKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzd6IH7N MX7TRW5ITVJ?
human H4 cell NU\IR242T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NITp[WFKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wO{BvVQ>? NEDCPJFUSU6JRWK=
human K5 cell NHSxT2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH;pd3BKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zN{BvVQ>? NVvtdVdbW0GQR1XS
human PA-1 cell M{\ZfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M13zWmlvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOFchdk1? NY\2RoVCW0GQR1XS
human SK-NEP-1 cell NETJd|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3\WdWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTlXQMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR7IH7N M3zuVHNCVkeHUh?=
human 697 cell NXfvbWlQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWPMdZBzUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlchdk1? NI\DU2xUSU6JRWK=
human CTB-1 cell NVnpe|IyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYC1dWNpUW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTNibl2= MnLjV2FPT0WU
human DB cell NFuw[5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH;iPXhKdmirYnn0bY9vKG:oIHj1cYFvKESEIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6xNkBvVQ>? NWHtRVhiW0GQR1XS
human MLMA cell M3;jdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH3GXmdKdmirYnn0bY9vKG:oIHj1cYFvKE2OTVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlMyKG6P MnPEV2FPT0WU
human GAMG cell M1XnSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoTOTY5pcWKrdHnvckBw\iCqdX3hckBISU2JIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz64NkBvVQ>? NIX6eZlUSU6JRWK=
human JVM-3 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHe4bGNKdmirYnn0bY9vKG:oIHj1cYFvKEqYTT2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTR?= MkHnV2FPT0WU
human LAMA-84 cell NI\5WWtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn;wTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xOyCwTR?= Mo[0V2FPT0WU
human RPMI-8226 cell Mn;iS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXHJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvOEKyOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTVibl2= NVvtPWRvW0GQR1XS
human MOLT-4 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuN|Ehdk1? NYnwR|h6W0GQR1XS
human CAMA-1 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{jEUGlvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44PyCwTR?= NVnTNYVYW0GQR1XS
human NCI-SNU-1 cell NX3wSY5nT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFHEVHVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEGgcm0> Ml7jV2FPT0WU
human SW780 cell M1XY[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnrQTY5pcWKrdHnvckBw\iCqdX3hckBUXzd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFMhdk1? Ml\zV2FPT0WU
human H9 cell NWHMXlQ1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHruWm9KdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64PEBvVQ>? NH24NVFUSU6JRWK=
human BE-13 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmDQTY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVEhdk1? Mlz2V2FPT0WU
human ES8 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWTtO5hUUW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlI4KG6P MlrqV2FPT0WU
human DEL cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NULJfIN6UW6qaXLpeIlwdiCxZjDoeY1idiCGRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ3KG6P M4jNOXNCVkeHUh?=
human QIMR-WIL cell M4fM[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44OSCwTR?= MYDTRW5ITVJ?
human CGTH-W-1 cell M175OGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoXhTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzVibl2= NFrPc3RUSU6JRWK=
human CHL-1 cell NWTCdZVIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1H2U2lvcGmkaYTpc44hd2ZiaIXtZY4hS0iOLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg3KG6P NYGwVZBiW0GQR1XS
human A2780 cell NVHpOVJST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGEzPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64PEBvVQ>? Mn7nV2FPT0WU
human VA-ES-BJ cell NWfuPWN2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV;uNIoxUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> M{fxZ3NCVkeHUh?=
human BB65-RCC cell MlLlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;G[IxOUW6qaXLpeIlwdiCxZjDoeY1idiCEQk[1MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdibl2= MkTQV2FPT0WU
human D-566MG cell NH3yU4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2LpdWlvcGmkaYTpc44hd2ZiaIXtZY4hTC13Nk\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOTZibl2= NEO1R5VUSU6JRWK=
human MDA468 cells MnnVVJJwdGmoZYLheIlwdiCjc4PhfS=> MoXCN{Bl[Xm| MlfYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFG0Olgh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD16IH7N MmOwNlE1Ozh3N{m=
human HO-1-N-1 cell M1rv[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2\IeGlvcGmkaYTpc44hd2ZiaIXtZY4hUE9vMT3OMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRThwMjDuUS=> NWfhe29{W0GQR1XS
human RS4-11 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV3JbXdvUW6qaXLpeIlwdiCxZjDoeY1idiCUU{StNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR3IH7N NWHzT|NOW0GQR1XS
human PC-3 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{LNWGlvcGmkaYTpc44hd2ZiaIXtZY4hWENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuNVQhdk1? NGm0T2tUSU6JRWK=
human NB69 cell MlnrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXjJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkS2JI5O NU\lUWxbW0GQR1XS
human HGC-27 cell Mmm0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFPqbJZKdmirYnn0bY9vKG:oIHj1cYFvKEiJQz2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPiCwTR?= MWnTRW5ITVJ?
human NCI-H720 cell NV3PenNMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEHGN3VKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|IxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS54MjDuUS=> MoKxV2FPT0WU
human NCI-H292 cell Ml7mS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX;IUm13UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwOESgcm0> NGDhOG5USU6JRWK=
human A3-KAW cell MlWxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLjeJA6UW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC52MzDuUS=> NHnaW45USU6JRWK=
human DU-4475 cell NYT3fW9mT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3z0XmlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjd|IH7N M{DVUHNCVkeHUh?=
human HuH-7 cell NYXyVIhzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVmxfWlzUW6qaXLpeIlwdiCxZjDoeY1idiCKdVitO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjN{IH7N NVrtUmVxW0GQR1XS
human J-RT3-T3-5 cell M3ftPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUnUbFlFUW6qaXLpeIlwdiCxZjDoeY1idiCMLWLUN{1VOy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|ghdk1? MnLqV2FPT0WU
human VM-CUB-1 cell MmDhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFTLSlhKdmirYnn0bY9vKG:oIHj1cYFvKF[PLVPVRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkegcm0> MoL3V2FPT0WU
human MOLT-16 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHvRUXlKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi56NDDuUS=> M3;IWHNCVkeHUh?=
human KG-1 cell MlXDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUnJcohq[mm2aX;uJI9nKGi3bXHuJGtINTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj65JI5O NHHNbmRUSU6JRWK=
human P12-ICHIKAWA cell NGfIZZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFGw[ItKdmirYnn0bY9vKG:oIHj1cYFvKFBzMj3JR2hKU0GZQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlAyKG6P MnPOV2FPT0WU
human ACN cell NUCz[|M5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn7wTY5pcWKrdHnvckBw\iCqdX3hckBCS05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNkBvVQ>? NUDoVY9FW0GQR1XS
human COLO-684 cell NYe4fVRtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNki0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvOzFibl2= MWHTRW5ITVJ?
human T-24 cell NHf4NHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnMXJRMUW6qaXLpeIlwdiCxZjDoeY1idiCWLUK0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvQDZibl2= NWLaTpRiW0GQR1XS
human AGS cell M{Htd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkLnTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND6xNUBvVQ>? MXXTRW5ITVJ?
human EW-13 cell M{G1Zmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4XWdmlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PCCwTR?= M4HTOnNCVkeHUh?=
human SW962 cell NIHqfVRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLDfpBKdmirYnn0bY9vKG:oIHj1cYFvKFOZOU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPTlibl2= NEjyTW1USU6JRWK=
human EW-11 cell NY\zUWN3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoPjTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlYhdk1? NGLjXFdUSU6JRWK=
human RXF393 cell NIfkdmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MonzTY5pcWKrdHnvckBw\iCqdX3hckBTYEZ|OUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU43PiCwTR?= NEjabZFUSU6JRWK=
human EoL-1-cell cell MlnvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEfLV|FKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNj6xJI5O M2HvdHNCVkeHUh?=

... 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]

+ Expand

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

Bio Calculators

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID