Temsirolimus (CCI-779)

For research use only. Not for use in humans.

Licensed by Pfizer Catalog No.S1044 Synonyms: NSC 683864

39 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.

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Selleck's Temsirolimus (CCI-779) has been cited by 39 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.
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 NV3kR4M3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rpV2lvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyOyCwTR?= NF;Xc3dUSU6JRWK=
human L-363 cell NF3hfpRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmP1TY5pcWKrdHnvckBw\iCqdX3hckBNNTN4MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQzKG6P MU\TRW5ITVJ?
human Ramos-2G6-4C10 cell NUjCW|VyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlnZTY5pcWKrdHnvckBw\iCqdX3hckBT[W2xcz2yS|YuPENzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|QzKG6P Ml2yV2FPT0WU
human SBC-1 cell NV7ZfmxWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXTwV|VWUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDR2IH7N M2rad3NCVkeHUh?=
human MHH-PREB-1 cell NGXXbmZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUDJcohq[mm2aX;uJI9nKGi3bXHuJG1JUC2SUlXCMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR7NTDuUS=> NUPiSYVzW0GQR1XS
human LNCAP cells MkCyVJJwdGmoZYLheIlwdiCjc4PhfS=> M1z2elMh\GG7cx?= NFfufZJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;MD61JI5O MoTmNlE1Ozh3N{m=
human HH cell NEfDV4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGPOdohKdmirYnn0bY9vKG:oIHj1cYFvKEiKIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD62OlQhdk1? M2myd3NCVkeHUh?=
human TYK-nu cell MlfGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYqwenpuUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd5ODDuUS=> M2HjO3NCVkeHUh?=
human H4 cell MkfvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVm1bFd3UW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFchdk1? NWLRcXhtW0GQR1XS
human K5 cell NUXxXpNQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M12xNGlvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOzJI5O M3;s[XNCVkeHUh?=
human PA-1 cell M3Xs[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M12wSWlvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOFchdk1? NWL0R3h[W0GQR1XS
human SK-NEP-1 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXe5[5QxUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OSXAuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEmgcm0> M2r6enNCVkeHUh?=
human 697 cell MnnzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWPJcohq[mm2aX;uJI9nKGi3bXHuJFY6PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNzDuUS=> NGqzU|BUSU6JRWK=
human CTB-1 cell NIHoblJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NILMbldKdmirYnn0bY9vKG:oIHj1cYFvKEOWQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk46OyCwTR?= M{X6NXNCVkeHUh?=
human DB cell NYDGV5M2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWHIdmFYUW6qaXLpeIlwdiCxZjDoeY1idiCGQjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVIhdk1? NVzYbXQ4W0GQR1XS
human MLMA cell M{HZTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUn1V2ZHUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= MUnTRW5ITVJ?
human GAMG cell M13Kemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUHJcohq[mm2aX;uJI9nKGi3bXHuJGdCVUdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkiyJI5O NXLzO49lW0GQR1XS
human JVM-3 cell M3TpO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF65WVVKdmirYnn0bY9vKG:oIHj1cYFvKEqYTT2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTR?= NFj5cYhUSU6JRWK=
human LAMA-84 cell MmDxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MknkTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xOyCwTR?= MnTDV2FPT0WU
human RPMI-8226 cell NHfFR3BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEDIe2FKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtPFIzPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMUWgcm0> NHWzNmlUSU6JRWK=
human MOLT-4 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1v5RWlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{OSCwTR?= NHP5d4dUSU6JRWK=
human CAMA-1 cell MlnCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4TuTGlvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44PyCwTR?= Ml\iV2FPT0WU
human NCI-SNU-1 cell NEXRfW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVPCSpBNUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkixJI5O Mkf5V2FPT0WU
human SW780 cell NYHJdm9uT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXLJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64N{BvVQ>? M1\z[HNCVkeHUh?=
human H9 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHHPOZNKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64PEBvVQ>? NFrZZ29USU6JRWK=
human BE-13 cell NVThVZR4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND65NUBvVQ>? NHSwN5pUSU6JRWK=
human ES8 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXnENFVEUW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlI4KG6P NWmze2ZWW0GQR1XS
human DEL cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoTXTY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O Ml3DV2FPT0WU
human QIMR-WIL cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoTRTY5pcWKrdHnvckBw\iCqdX3hckBSUU2ULWfJUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzFibl2= NH\oO5VUSU6JRWK=
human CGTH-W-1 cell Ml\DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmrwTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzVibl2= MkD2V2FPT0WU
human CHL-1 cell NHHLRnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV;LXXVGUW6qaXLpeIlwdiCxZjDoeY1idiCFSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDZibl2= NF\ISJpUSU6JRWK=
human A2780 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnvFTY5pcWKrdHnvckBw\iCqdX3hckBCOjd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFghdk1? M3TwU3NCVkeHUh?=
human VA-ES-BJ cell NFG1PWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnruTY5pcWKrdHnvckBw\iCqdX3hckBXSS2HUz3CTkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQSCwTR?= MUTTRW5ITVJ?
human BB65-RCC cell NWOzSFVZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGJDPjVvUlPDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{BvVQ>? M3PUc3NCVkeHUh?=
human D-566MG cell MofmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETMOnZKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjF4IH7N NFPHbXZUSU6JRWK=
human MDA468 cells M4fJe3Bzd2yrZnXyZZRqd25iYYPzZZk> MYWzJIRigXN? M3TXU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBOFY5KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;ODDuUS=> M{HSSVIyPDN6NUe5
human HO-1-N-1 cell M2i2fmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWnJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF05NjJibl2= MkDUV2FPT0WU
human RS4-11 cell M2DDTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnnITY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlQ2KG6P NHX6WnRUSU6JRWK=
human PC-3 cell NVPSZ4o4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX70NIYxUW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU4yPCCwTR?= NULHcYZTW0GQR1XS
human NB69 cell Mlr1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVvJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkS2JI5O M1;TV3NCVkeHUh?=
human HGC-27 cell NIDXS5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHLsVVlKdmirYnn0bY9vKG:oIHj1cYFvKEiJQz2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPiCwTR?= NEC0R4lUSU6JRWK=
human NCI-H720 cell M3T6U2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVvJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{KwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU43OiCwTR?= MlfoV2FPT0WU
human NCI-H292 cell NV[0SFZ5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1nIemlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N NUHwZVZZW0GQR1XS
human A3-KAW cell M{[2Wmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGE{NUuDVzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlQ{KG6P NEnpd2ZUSU6JRWK=
human DU-4475 cell NYjLSpdyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnrrTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPzNibl2= NIS3TW9USU6JRWK=
human HuH-7 cell NVL4bHhxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGh2UC15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|Ihdk1? NH\kU5VUSU6JRWK=
human J-RT3-T3-5 cell M4\jZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVLJcohq[mm2aX;uJI9nKGi3bXHuJGouWlR|LWSzMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|ODDuUS=> MVXTRW5ITVJ?
human VM-CUB-1 cell MmjBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M37CbGlvcGmkaYTpc44hd2ZiaIXtZY4hXk1vQ2XCMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi54NzDuUS=> NY[0XpVFW0GQR1XS
human MOLT-16 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnITY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvQDRibl2= NIr6fYpUSU6JRWK=
human KG-1 cell NHz2Z|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYO5bYt6UW6qaXLpeIlwdiCxZjDoeY1idiCNRz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvQSCwTR?= MoPuV2FPT0WU
human P12-ICHIKAWA cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4HP[GlvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFEhdk1? M2PGSnNCVkeHUh?=
human ACN cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIDk[lNKdmirYnn0bY9vKG:oIHj1cYFvKEGFTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlAzKG6P MnvXV2FPT0WU
human COLO-684 cell Mnj3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNki0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvOzFibl2= MkPzV2FPT0WU
human T-24 cell M2Phfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz64OkBvVQ>? MnrKV2FPT0WU
human AGS cell M2\CT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmizTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND6xNUBvVQ>? Mnv5V2FPT0WU
human EW-13 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1HsdmlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PCCwTR?= M2HGeHNCVkeHUh?=
human SW962 cell MkPUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUPJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOVkhdk1? NITHNG5USU6JRWK=
human EW-11 cell NFzISY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX\XUG1XUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZibl2= M3LLNXNCVkeHUh?=
human RXF393 cell NUnLV29JT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoTSTY5pcWKrdHnvckBw\iCqdX3hckBTYEZ|OUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU43PiCwTR?= MnzpV2FPT0WU
human EoL-1-cell cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4j0ZmlvcGmkaYTpc44hd2ZiaIXtZY4hTW:OLUGtZ4VtdCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4LkGgcm0> M37Ie3NCVkeHUh?=

... 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
  • 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 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

Bio Calculators

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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

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  • Computed Result

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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)
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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID