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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In DMSO USD 134 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

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 M1;PZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mni5TY5pcWKrdHnvckBw\iCqdX3hckBJW0NvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE{KG6P NWixRXhIW0GQR1XS
human L-363 cell NIrPZ4hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFrN[GxKdmirYnn0bY9vKG:oIHj1cYFvKExvM{[zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDJibl2= NGTiZppUSU6JRWK=
human Ramos-2G6-4C10 cell NV21OoFbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFLEUWNKdmirYnn0bY9vKG:oIHj1cYFvKFKjbX;zMVJIPi12Q{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PDJibl2= M4HJR3NCVkeHUh?=
human SBC-1 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TUbWlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= MV;TRW5ITVJ?
human MHH-PREB-1 cell M{nWdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUjjdWY6UW6qaXLpeIlwdiCxZjDoeY1idiCPSFitVHJGSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVUhdk1? NHPqWVVUSU6JRWK=
human LNCAP cells MmjxVJJwdGmoZYLheIlwdiCjc4PhfS=> MXOzJIRigXN? MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGOgZZN{[XluIFnDOVA:OC53IH7N NEn1TFMzOTR|OEW3PS=>
human HH cell Mnn3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54NkSgcm0> MlL1V2FPT0WU
human TYK-nu cell M3W2T2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXy3fINNUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd5ODDuUS=> NIWxelJUSU6JRWK=
human H4 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yNzDuUS=> M2q0ZnNCVkeHUh?=
human K5 cell M3LkUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NELWdnVKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zN{BvVQ>? NWDKS4V6W0GQR1XS
human PA-1 cell NEPWNmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYr5WYhEUW6qaXLpeIlwdiCxZjDoeY1idiCSQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41PyCwTR?= NF31fYJUSU6JRWK=
human SK-NEP-1 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNU6HUD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41QSCwTR?= M3e0cXNCVkeHUh?=
human 697 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV3QUGZXUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlchdk1? MV3TRW5ITVJ?
human CTB-1 cell MkfqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV7Ee|lwUW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTNibl2= M2G4[nNCVkeHUh?=
human DB cell NHjROY9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2jjTWlvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O M1P6bnNCVkeHUh?=
human MLMA cell MkHKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnPnTY5pcWKrdHnvckBw\iCqdX3hckBOVE2DIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6zNUBvVQ>? NVPhXHI5W0GQR1XS
human GAMG cell NGK1RphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUDYZm5yUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OiCwTR?= NID6[2xUSU6JRWK=
human JVM-3 cell MoWwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWH3fVh3UW6qaXLpeIlwdiCxZjDoeY1idiCMVl2tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTVibl2= NVTMSW1mW0GQR1XS
human LAMA-84 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlA{KG6P M37FUXNCVkeHUh?=
human RPMI-8226 cell NGrrNHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXjbHpzUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O NYXjPIxGW0GQR1XS
human MOLT-4 cell M1frVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTtVIdZUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjNzIH7N M4rTXHNCVkeHUh?=
human CAMA-1 cell Mn\OS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M124eGlvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44PyCwTR?= NXz2dJliW0GQR1XS
human NCI-SNU-1 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYXYdHhsUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkixJI5O MkW0V2FPT0WU
human SW780 cell M1\q[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFnZfm1KdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45OyCwTR?= MXLTRW5ITVJ?
human H9 cell NHT1T5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56ODDuUS=> NHLqfm5USU6JRWK=
human BE-13 cell NH7ucZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND65NUBvVQ>? MXzTRW5ITVJ?
human ES8 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmDaTY5pcWKrdHnvckBw\iCqdX3hckBGWzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkK3JI5O M17ld3NCVkeHUh?=
human DEL cell NUjSPVJKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvVTY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O M{fZenNCVkeHUh?=
human QIMR-WIL cell NFHoR4VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2fodGlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjdzIH7N Mn3jV2FPT0WU
human CGTH-W-1 cell M{\0OGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYnTRnJKUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Wgcm0> M4XNcXNCVkeHUh?=
human CHL-1 cell NGqwWplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3HRbGlvcGmkaYTpc44hd2ZiaIXtZY4hS0iOLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg3KG6P NH[ybJZUSU6JRWK=
human A2780 cell MoLZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKGi3bXHuJGEzPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64PEBvVQ>? MWHTRW5ITVJ?
human VA-ES-BJ cell NYjuOWE5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXL1XGozUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> M17WXnNCVkeHUh?=
human BB65-RCC cell M{TIXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2fXOWlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ4NT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04KG6P Mk\KV2FPT0WU
human D-566MG cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJGQuPTZ4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23MlE3KG6P Mn7yV2FPT0WU
human MDA468 cells NEX3enhRem:uaX\ldoF1cW:wIHHzd4F6 NULGXnlYOyCmYYnz MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQUS2PEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRThibl2= MUSyNVQ{QDV5OR?=
human HO-1-N-1 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWnQR2JsUW6qaXLpeIlwdiCxZjDoeY1idiCKTz2xMW4uOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;OD6yJI5O MljvV2FPT0WU
human RS4-11 cell NX\pSFJqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOFUhdk1? NVzudJF5W0GQR1XS
human PC-3 cell NV;WN2RST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVmwelB2UW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU4yPCCwTR?= NXT1UGxxW0GQR1XS
human NB69 cell MknrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEPBS3NKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ3KG6P MV\TRW5ITVJ?
human HGC-27 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGhISy1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOkBvVQ>? NYfCbY11W0GQR1XS
human NCI-H720 cell Mlf5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{KwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU43OiCwTR?= NVGwdHFsW0GQR1XS
human NCI-H292 cell Mn72S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFHtfndKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS56NDDuUS=> NIDxR5JUSU6JRWK=
human A3-KAW cell NUj4XlRbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGE{NUuDVzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlQ{KG6P M2G0SXNCVkeHUh?=
human DU-4475 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHzTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPzNibl2= NWLFd49iW0GQR1XS
human HuH-7 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Moe1TY5pcWKrdHnvckBw\iCqdX3hckBJfUhvNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlMzKG6P NU\1Z|hrW0GQR1XS
human J-RT3-T3-5 cell NHPsWIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnFem86UW6qaXLpeIlwdiCxZjDoeY1idiCMLWLUN{1VOy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|ghdk1? M1zGVnNCVkeHUh?=
human VM-CUB-1 cell M{L4VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEP2S5pKdmirYnn0bY9vKG:oIHj1cYFvKF[PLVPVRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkegcm0> MV3TRW5ITVJ?
human MOLT-16 cell NUfCUYJRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3Sw[mlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjh2IH7N M4H0UXNCVkeHUh?=
human KG-1 cell M3nrOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MULJcohq[mm2aX;uJI9nKGi3bXHuJGtINTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj65JI5O MnfvV2FPT0WU
human P12-ICHIKAWA cell M{XVXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDmTY5pcWKrdHnvckBw\iCqdX3hckBROTJvSVPITWtCX0FiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNUBvVQ>? M2DGfXNCVkeHUh?=
human ACN cell NWjtSGlRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4W1U2lvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFIhdk1? MW\TRW5ITVJ?
human COLO-684 cell NW\XVFNuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF3rcIFKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwM{Ggcm0> MVrTRW5ITVJ?
human T-24 cell NUXPWWxzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlGwTY5pcWKrdHnvckBw\iCqdX3hckBVNTJ2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuPFYhdk1? NIXFO3VUSU6JRWK=
human AGS cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHPpZ5RKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P MnvZV2FPT0WU
human EW-13 cell NEXnWlNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnue29tUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV2IH7N NYrCV2syW0GQR1XS
human SW962 cell NF3MWYxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWDMWmJKUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjV7IH7N MX\TRW5ITVJ?
human EW-11 cell M2nQTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFHKdpFKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPiCwTR?= NFrkXWRUSU6JRWK=
human RXF393 cell M1XmWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn;iTY5pcWKrdHnvckBw\iCqdX3hckBTYEZ|OUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU43PiCwTR?= MX7TRW5ITVJ?
human EoL-1-cell cell M4K3PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NInHOVlKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNj6xJI5O MUnTRW5ITVJ?

... 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