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 33 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 NFz3b3FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mke5TY5pcWKrdHnvckBw\iCqdX3hckBJW0NvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE{KG6P NXvwepF7W0GQR1XS
human L-363 cell NVv2Uoo2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXzDOZJvUW6qaXLpeIlwdiCxZjDoeY1idiCOLUO2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjR{IH7N Mn;jV2FPT0WU
human Ramos-2G6-4C10 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXG3dVE3UW6qaXLpeIlwdiCxZjDoeY1idiCUYX3vd{0zTzZvNFOxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzR{IH7N M3HMZnNCVkeHUh?=
human SBC-1 cell NWDTO2syT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{TNemlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= MUDTRW5ITVJ?
human MHH-PREB-1 cell NI\TUY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX3aOYtvUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitVHJGSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVUhdk1? MVTTRW5ITVJ?
human LNCAP cells NGjRb2JRem:uaX\ldoF1cW:wIHHzd4F6 NWLvZpJxOyCmYYnz MlnVRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOTlPBVEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRTBwNTDuUS=> NFXhfXgzOTR|OEW3PS=>
human HH cell NUDOZmVlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmrFTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNk[0JI5O MoDGV2FPT0WU
human TYK-nu cell NEW0UHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXexUFJQUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd5ODDuUS=> M2TQU3NCVkeHUh?=
human H4 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2Tmb2lvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC3JI5O NYOweYtWW0GQR1XS
human K5 cell M37wbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWTJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|MzDuUS=> NU\aS5R[W0GQR1XS
human PA-1 cell M3PNeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX;SVWJiUW6qaXLpeIlwdiCxZjDoeY1idiCSQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41PyCwTR?= NHToN5lUSU6JRWK=
human SK-NEP-1 cell NVrRbm5zT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYf3VVlPUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OSXAuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEmgcm0> NHHtWJlUSU6JRWK=
human 697 cell NYHWU3B{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXXJcohq[mm2aX;uJI9nKGi3bXHuJFY6PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNzDuUS=> NEXhT2VUSU6JRWK=
human CTB-1 cell M{\kTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65N{BvVQ>? NWXHT4MxW0GQR1XS
human DB cell M1jGfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVvQR3k4UW6qaXLpeIlwdiCxZjDoeY1idiCGQjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVIhdk1? MkTIV2FPT0WU
human MLMA cell NYTsSHNPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH2yPZJKdmirYnn0bY9vKG:oIHj1cYFvKE2OTVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlMyKG6P M3v1cXNCVkeHUh?=
human GAMG cell NHnSbWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3rLbWlvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPFIhdk1? MXnTRW5ITVJ?
human JVM-3 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2D1NmlvcGmkaYTpc44hd2ZiaIXtZY4hUl[PLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2KG6P MUPTRW5ITVJ?
human LAMA-84 cell M3fobWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1LieWlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODNibl2= NWHTXJo{W0GQR1XS
human RPMI-8226 cell NV7zd2hKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoDjTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUiyNlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjF3IH7N NXP4W2RpW0GQR1XS
human MOLT-4 cell M{HOSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkfoTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlMyKG6P M1LKR3NCVkeHUh?=
human CAMA-1 cell M33pcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXjHRZdFUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd5IH7N MUjTRW5ITVJ?
human NCI-SNU-1 cell Ml36S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVr6bo5UUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkixJI5O M1TyUnNCVkeHUh?=
human SW780 cell NVLEZnZXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2L1eWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{KG6P MknJV2FPT0WU
human H9 cell NYDxSpR6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFrIcYZKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64PEBvVQ>? MVHTRW5ITVJ?
human BE-13 cell NILqZZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MorFTY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVEhdk1? MVnTRW5ITVJ?
human ES8 cell NXrpe5BjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkfsTY5pcWKrdHnvckBw\iCqdX3hckBGWzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkK3JI5O NVfpfHVlW0GQR1XS
human DEL cell M{[0TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoTiTY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O MXnTRW5ITVJ?
human QIMR-WIL cell MknMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIns[3hKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS55MTDuUS=> MWHTRW5ITVJ?
human CGTH-W-1 cell NFnqeWNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX65VFQyUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Wgcm0> M2TaSXNCVkeHUh?=
human CHL-1 cell NFfXOIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVPreJBEUW6qaXLpeIlwdiCxZjDoeY1idiCFSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDZibl2= NVWxR2p3W0GQR1XS
human A2780 cell M17BVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGEzPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64PEBvVQ>? NWDVeWs4W0GQR1XS
human VA-ES-BJ cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1e5UWlvcGmkaYTpc44hd2ZiaIXtZY4hXkFvRWOtRmoh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njlibl2= NHzPXY5USU6JRWK=
human BB65-RCC cell M2jKOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4XSPGlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ4NT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04KG6P M4LNUHNCVkeHUh?=
human D-566MG cell M3nTXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlfETY5pcWKrdHnvckBw\iCqdX3hckBFNTV4Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{4yPiCwTR?= M4LEfnNCVkeHUh?=
human MDA468 cells NH6yVIZRem:uaX\ldoF1cW:wIHHzd4F6 MlP6N{Bl[Xm| MljPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFG0Olgh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD16IH7N NGDZNoUzOTR|OEW3PS=>
human HO-1-N-1 cell NYWwOGdFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHf6WVVKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> MY\TRW5ITVJ?
human RS4-11 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOFUhdk1? NITYUHpUSU6JRWK=
human PC-3 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml7hTY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OT6xOEBvVQ>? M1P1XnNCVkeHUh?=
human NB69 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYXjO245UW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PiCwTR?= NFW0SHFUSU6JRWK=
human HGC-27 cell M3f0N2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVvUeYl3UW6qaXLpeIlwdiCxZjDoeY1idiCKR1OtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZibl2= NGX2SVZUSU6JRWK=
human NCI-H720 cell NUjlWJdZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkXITY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEeyNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPjJibl2= MmLPV2FPT0WU
human NCI-H292 cell NV7kUWlNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUfJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU45PCCwTR?= Mk\BV2FPT0WU
human A3-KAW cell M2P2Vmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml\DTY5pcWKrdHnvckBw\iCqdX3hckBCOy2NQWegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE41OyCwTR?= NVLGS5FpW0GQR1XS
human DU-4475 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1fhbmlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjd|IH7N MV;TRW5ITVJ?
human HuH-7 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkHNTY5pcWKrdHnvckBw\iCqdX3hckBJfUhvNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlMzKG6P NW\pSo1uW0GQR1XS
human J-RT3-T3-5 cell NVzKbFg3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFr3PWdKdmirYnn0bY9vKG:oIHj1cYFvKEpvUmSzMXQ{NTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj6zPEBvVQ>? MX;TRW5ITVJ?
human VM-CUB-1 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NW\DUoNvUW6qaXLpeIlwdiCxZjDoeY1idiCYTT3DWWIuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lk[3JI5O M2XVSnNCVkeHUh?=
human MOLT-16 cell NXPYbmRMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUHJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk45PCCwTR?= MnvzV2FPT0WU
human KG-1 cell M2LUWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXXkcGRGUW6qaXLpeIlwdiCxZjDoeY1idiCNRz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvQSCwTR?= NWjQ[GI6W0GQR1XS
human P12-ICHIKAWA cell M{XD[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\PTY5pcWKrdHnvckBw\iCqdX3hckBROTJvSVPITWtCX0FiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNUBvVQ>? M1rIZ3NCVkeHUh?=
human ACN cell MlLVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoDqTY5pcWKrdHnvckBw\iCqdX3hckBCS05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNkBvVQ>? NW[3Sm16W0GQR1XS
human COLO-684 cell MoLjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoW5TY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjNzIH7N NFnjZVVUSU6JRWK=
human T-24 cell MkLxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHHNTI1KdmirYnn0bY9vKG:oIHj1cYFvKFRvMkSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{45PiCwTR?= MlTFV2FPT0WU
human AGS cell NHHSVJBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEmwfJZKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P M2Ly[HNCVkeHUh?=
human EW-13 cell NFvuTnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnjDTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlU1KG6P MmfjV2FPT0WU
human SW962 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkDLTY5pcWKrdHnvckBw\iCqdX3hckBUXzl4MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlU6KG6P NVPrV283W0GQR1XS
human EW-11 cell M2[5TWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVnJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOkBvVQ>? MWTTRW5ITVJ?
human RXF393 cell NIT5PYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3fYUWlvcGmkaYTpc44hd2ZiaIXtZY4hWliIM{mzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPjZibl2= Mn7rV2FPT0WU
human EoL-1-cell cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofqTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwMTDuUS=> NVzZcopQW0GQR1XS

... 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 N/A

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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Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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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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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