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.

Size Price Stock Quantity  
In DMSO USD 134 In stock
USD 117 In stock
USD 247 In stock
USD 370 In stock
USD 870 In stock

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4 Customer Reviews

  • mTOR inhibitors attenuate ganetespib-driven elevation of HSPs in multiple tumor cell types. A375 melanoma cells were treated with vehicle, ganetespib (25 nmol/L), BEZ235 (500 nmol/L), or temsirolimus (500 nmol/L), either alone or in combination, for 24 hours. The levels of HSP90α, HSP70, HSP27, and GAPDH were determined by immunoblotting.

    Mol Cancer Res 2014 12, 703-13. Temsirolimus (CCI-779, NSC 683864) purchased from Selleck.

    SCID mice with PC-9/Vec or PC-9/HGF tumors were administered as described in Figure. Four hours after final administration of erlotinib, tumors were harvested, and tumor cell angiogenesis (CD31) were determined by immunohistochemistry.

    PLoS One 2013 8, e62104. Temsirolimus (CCI-779, NSC 683864) purchased from Selleck.

  • SCID mice with PC-9/Vec or PC-9/HGF tumors were administered 25 mg/kg erlotinib once daily for 4 days or 50 mg/kg temsirolimus once from day 8. Four hours after final erlotinib administration, tumors were harvested, and the relative levels of proteins in the tumor lysates were determined by western blotting.

    PLoS One 2013 8, e62104. Temsirolimus (CCI-779, NSC 683864) purchased from Selleck.

    Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Temsirolimus for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. Temsirolimus (CCI-779, NSC 683864) purchased from Selleck.

Purity & Quality Control

Choose Selective mTOR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NULqSndzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MonNTY5pcWKrdHnvckBw\iCqdX3hckBJW0NvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE{KG6P NWOzd3pDW0GQR1XS
human L-363 cell MonKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWDDdJo4UW6qaXLpeIlwdiCxZjDoeY1idiCOLUO2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjR{IH7N MojOV2FPT0WU
human Ramos-2G6-4C10 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLxTY5pcWKrdHnvckBw\iCqdX3hckBT[W2xcz2yS|YuPENzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|QzKG6P NUT3XIQ2W0GQR1XS
human SBC-1 cell Ml\zS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXO0VWFbUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDR2IH7N MlTBV2FPT0WU
human MHH-PREB-1 cell NFzKeWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NETZRmNKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3QVmVDNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5OUBvVQ>? MXjTRW5ITVJ?
human LNCAP cells NUHOVG1ZWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHiyOlY{KGSjeYO= MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGOgZZN{[XluIFnDOVA:OC53IH7N MVeyNVQ{QDV5OR?=
human HH cell NVvRZ4ppT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWfNW4gzUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlY1KG6P M4\0UXNCVkeHUh?=
human TYK-nu cell M{\D[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3m0ZWlvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44Pzhibl2= NYG4T5BDW0GQR1XS
human H4 cell M4LnSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{PheGlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC3JI5O MkHGV2FPT0WU
human K5 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MljTTY5pcWKrdHnvckBw\iCqdX3hckBMPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwM{Ogcm0> MXXTRW5ITVJ?
human PA-1 cell NVjWZ2dWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX\UOo15UW6qaXLpeIlwdiCxZjDoeY1idiCSQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41PyCwTR?= NXL1WZNkW0GQR1XS
human SK-NEP-1 cell Mm[3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M17sO2lvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTlXQMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR7IH7N MUXTRW5ITVJ?
human 697 cell NH7JNZJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{HsdWlvcGmkaYTpc44hd2ZiaIXtZY4hPjl5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63JI5O MmrUV2FPT0WU
human CTB-1 cell NWrvPIlET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWHJcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65N{BvVQ>? M1\EXnNCVkeHUh?=
human DB cell NEjmXW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGRDKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5zMjDuUS=> M2TWTXNCVkeHUh?=
human MLMA cell NX\ZVlZmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXPmZoFRUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= MVrTRW5ITVJ?
human GAMG cell NI\aZlFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fqNGlvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPFIhdk1? MoXHV2FPT0WU
human JVM-3 cell MmPmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGpXVS1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OUBvVQ>? NYHpe20{W0GQR1XS
human LAMA-84 cell NIfGeoZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFTIeXlKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB|IH7N MXHTRW5ITVJ?
human RPMI-8226 cell MljYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVrwVWlzUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O M4HabnNCVkeHUh?=
human MOLT-4 cell NHTDO3VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuN|Ehdk1? NYDUPXpDW0GQR1XS
human CAMA-1 cell NXWwS4JZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYjkS3V4UW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd5IH7N M4faTHNCVkeHUh?=
human NCI-SNU-1 cell Mni3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4HPUWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLWPOWU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56MTDuUS=> M4jXW3NCVkeHUh?=
human SW780 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64N{BvVQ>? M4\Uc3NCVkeHUh?=
human H9 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56ODDuUS=> M4HsV3NCVkeHUh?=
human BE-13 cell NFv5R4NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MorxTY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVEhdk1? M2PES3NCVkeHUh?=
human ES8 cell MkjYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGVUQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwMkegcm0> M1fv[3NCVkeHUh?=
human DEL cell MmLwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoLhTY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O M1WxenNCVkeHUh?=
human QIMR-WIL cell MmruS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoLrTY5pcWKrdHnvckBw\iCqdX3hckBSUU2ULWfJUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzFibl2= NWD3bVVTW0GQR1XS
human CGTH-W-1 cell MlqwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIXOWIZKdmirYnn0bY9vKG:oIHj1cYFvKEOJVFitW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS55NTDuUS=> NWPLWHo2W0GQR1XS
human CHL-1 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mm\MTY5pcWKrdHnvckBw\iCqdX3hckBEUExvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFYhdk1? MXjTRW5ITVJ?
human A2780 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mlv2TY5pcWKrdHnvckBw\iCqdX3hckBCOjd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFghdk1? M{O4dHNCVkeHUh?=
human VA-ES-BJ cell M2PBTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWHMUms4UW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> NInkOXBUSU6JRWK=
human BB65-RCC cell NYn2Sm1QT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnH4TY5pcWKrdHnvckBw\iCqdX3hckBDSjZ3LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVchdk1? MWfTRW5ITVJ?
human D-566MG cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVLJcohq[mm2aX;uJI9nKGi3bXHuJGQuPTZ4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23MlE3KG6P M2LJRnNCVkeHUh?=
human MDA468 cells MonwVJJwdGmoZYLheIlwdiCjc4PhfS=> MXizJIRigXN? M3;wVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBOFY5KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;ODDuUS=> NYrMflllOjF2M{i1O|k>
human HO-1-N-1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV7UXJFTUW6qaXLpeIlwdiCxZjDoeY1idiCKTz2xMW4uOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;OD6yJI5O MX7TRW5ITVJ?
human RS4-11 cell NFjtfZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOFUhdk1? NUPWPY8yW0GQR1XS
human PC-3 cell NE\Mb4JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlLtTY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OT6xOEBvVQ>? NUDud4xpW0GQR1XS
human NB69 cell MlzLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NITZO4hKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ3KG6P NWX2WWNyW0GQR1XS
human HGC-27 cell NHr3V4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVG0U|VtUW6qaXLpeIlwdiCxZjDoeY1idiCKR1OtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZibl2= MYLTRW5ITVJ?
human NCI-H720 cell Mme5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVrFVZJVUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFczOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwNkKgcm0> NHTkPWpUSU6JRWK=
human NCI-H292 cell Ml3JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1fKSGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N MlL5V2FPT0WU
human A3-KAW cell Mk\oS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NULjO4lbUW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC52MzDuUS=> NGexZ2xUSU6JRWK=
human DU-4475 cell NITnOJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVK3N|FXUW6qaXLpeIlwdiCxZjDoeY1idiCGVT20OFc2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwN{Ogcm0> MU\TRW5ITVJ?
human HuH-7 cell MonLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mmr1TY5pcWKrdHnvckBw\iCqdX3hckBJfUhvNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlMzKG6P M2TWTXNCVkeHUh?=
human J-RT3-T3-5 cell NYKzXXF6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mm\YTY5pcWKrdHnvckBw\iCqdX3hckBLNVKWMz3UN{02KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwM{igcm0> MVrTRW5ITVJ?
human VM-CUB-1 cell M33JO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYTKV2JHUW6qaXLpeIlwdiCxZjDoeY1idiCYTT3DWWIuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lk[3JI5O M1zMWnNCVkeHUh?=
human MOLT-16 cell Mn2xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXHWOXI4UW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwOESgcm0> M3S3U3NCVkeHUh?=
human KG-1 cell MnnJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGtINTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj65JI5O M3ThTXNCVkeHUh?=
human P12-ICHIKAWA cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mnf3TY5pcWKrdHnvckBw\iCqdX3hckBROTJvSVPITWtCX0FiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNUBvVQ>? NUj4UYpuW0GQR1XS
human ACN cell M2PmVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXfGc|g5UW6qaXLpeIlwdiCxZjDoeY1idiCDQ16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOiCwTR?= MU\TRW5ITVJ?
human COLO-684 cell M4nL[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn3BTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjNzIH7N MkXzV2FPT0WU
human T-24 cell NY\kR5A6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4TzRWlvcGmkaYTpc44hd2ZiaIXtZY4hXC1{NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlg3KG6P MWPTRW5ITVJ?
human AGS cell Mnm5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGFIWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2LkGxJI5O Ml7zV2FPT0WU
human EW-13 cell NFH5eo5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUfldnU5UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV2IH7N NVL4WWNbW0GQR1XS
human SW962 cell NXHkXG9ST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOVkhdk1? M1LZPXNCVkeHUh?=
human EW-11 cell MmfSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml;GTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlYhdk1? NVy2XVlSW0GQR1XS
human RXF393 cell M3fHcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2\ob2lvcGmkaYTpc44hd2ZiaIXtZY4hWliIM{mzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPjZibl2= NUHoO3VbW0GQR1XS
human EoL-1-cell cell NVvPd29kT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4DUVWlvcGmkaYTpc44hd2ZiaIXtZY4hTW:OLUGtZ4VtdCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF4LkGgcm0> MXjTRW5ITVJ?

... 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]

+ 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 DMSO 75 mg/mL (72.79 mM)
Ethanol 75 mg/mL (72.79 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 10 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 Conditions Sponsor/Collaborators Start Date Phases
NCT01182883 Withdrawn Brain Stem Neoplasms|Glioma|Pinealoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 28, 2010 Phase 1
NCT02908035 Not yet recruiting Chronic Limb Ischemia Mercator MedSystems, Inc. January 2017 Phase 2
NCT02567435 Suspended Alveolar Rhabdomyosarcoma|Botryoid-Type Embryonal Rhabdomyosarcoma|Embryonal Rhabdomyosarcoma|Rhabdomyosarcoma|Sclerosing Rhabdomyosarcoma|Spindle Cell Rhabdomyosarcoma|Untreated Childhood Rhabdomyosarcoma National Cancer Institute (NCI) May 2016 Phase 3
NCT02693535 Recruiting Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer March 2016 Phase 2
NCT02560012 Recruiting Carcinoma, Renal Cell The University of Texas Health Science Center, Houston December 2015 Phase 2
NCT02420613 Recruiting Diffuse Intrinsic Pontine Glioma M.D. Anderson Cancer Center October 2015 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID