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 39 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 Mo\oS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHvKWVZKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTNibl2= NWPnWIVnW0GQR1XS
human L-363 cell NVjzUWw4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1nBbGlvcGmkaYTpc44hd2ZiaIXtZY4hVC1|NkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1OiCwTR?= MX\TRW5ITVJ?
human Ramos-2G6-4C10 cell M{TJU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWDVN3FiUW6qaXLpeIlwdiCxZjDoeY1idiCUYX3vd{0zTzZvNFOxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzR{IH7N NGHre4dUSU6JRWK=
human SBC-1 cell MlrZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmLwTY5pcWKrdHnvckBw\iCqdX3hckBUSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ1KG6P MXHTRW5ITVJ?
human MHH-PREB-1 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2POemlvcGmkaYTpc44hd2ZiaIXtZY4hVUiKLWDSSWIuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEm1JI5O MVvTRW5ITVJ?
human LNCAP cells NGrNcnhRem:uaX\ldoF1cW:wIHHzd4F6 M3PYc|Mh\GG7cx?= NVW4NWY5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUCuOUBvVQ>? NFvOb3ozOTR|OEW3PS=>
human HH cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX;NbnJIUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlY1KG6P M1G0bnNCVkeHUh?=
human TYK-nu cell NV7sbmRRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGCyfnlKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzd6IH7N M2XjcHNCVkeHUh?=
human H4 cell NXnPNHFoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYjJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yNzDuUS=> MkDKV2FPT0WU
human K5 cell M2Hs[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVjqZ282UW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Mhdk1? NILhb|dUSU6JRWK=
human PA-1 cell M3rJTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4X2PWlvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOFchdk1? NX;IdGUyW0GQR1XS
human SK-NEP-1 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYfJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU6HUD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41QSCwTR?= MXrTRW5ITVJ?
human 697 cell MkHuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHHkRYVKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO{BvVQ>? M3HwO3NCVkeHUh?=
human CTB-1 cell NUjWUVluT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGj1NYlKdmirYnn0bY9vKG:oIHj1cYFvKEOWQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk46OyCwTR?= MlrEV2FPT0WU
human DB cell M{\GSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVvySnBrUW6qaXLpeIlwdiCxZjDoeY1idiCGQjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVIhdk1? M3ftdXNCVkeHUh?=
human MLMA cell M3K3UGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\udmlvcGmkaYTpc44hd2ZiaIXtZY4hVUyPQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|Ehdk1? NHXLeZFUSU6JRWK=
human GAMG cell M3e2dWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVvzVm1xUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OiCwTR?= MoTFV2FPT0WU
human JVM-3 cell NHfZNFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn3vTY5pcWKrdHnvckBw\iCqdX3hckBLXk1vMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVUhdk1? MYDTRW5ITVJ?
human LAMA-84 cell M1Xld2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYLJcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlA{KG6P MXHTRW5ITVJ?
human RPMI-8226 cell MmC5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYDFTHJOUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O NIDCdWlUSU6JRWK=
human MOLT-4 cell NUXGW41vT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M13kWmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{OSCwTR?= M4[weXNCVkeHUh?=
human CAMA-1 cell M4jBRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTBSlJSUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd5IH7N MV3TRW5ITVJ?
human NCI-SNU-1 cell M4O3N2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFrCS5lKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEGgcm0> MmTpV2FPT0WU
human SW780 cell NHPkR|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFzvVllKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45OyCwTR?= NVvQXG0zW0GQR1XS
human H9 cell NG\POmtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUXOWWlkUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFghdk1? NED5NZJUSU6JRWK=
human BE-13 cell Mn[2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVrsemdUUW6qaXLpeIlwdiCxZjDoeY1idiCERT2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTFibl2= MYfTRW5ITVJ?
human ES8 cell M4XxdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3rCUmlvcGmkaYTpc44hd2ZiaIXtZY4hTVN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6yO{BvVQ>? NF\WSFFUSU6JRWK=
human DEL cell NHqxRY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnTzTY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O NVTSNWRqW0GQR1XS
human QIMR-WIL cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mke5TY5pcWKrdHnvckBw\iCqdX3hckBSUU2ULWfJUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzFibl2= NFTkVo5USU6JRWK=
human CGTH-W-1 cell NIewNmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4LtN2lvcGmkaYTpc44hd2ZiaIXtZY4hS0eWSD3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njd3IH7N MWjTRW5ITVJ?
human CHL-1 cell NGO0cndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUe4e5Q3UW6qaXLpeIlwdiCxZjDoeY1idiCFSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDZibl2= M4LPXXNCVkeHUh?=
human A2780 cell NYTEXXd{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV;mS21FUW6qaXLpeIlwdiCxZjDoeY1idiCDMke4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDhibl2= MW\TRW5ITVJ?
human VA-ES-BJ cell MoP6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF;BfJlKdmirYnn0bY9vKG:oIHj1cYFvKF[DLVXTMWJLKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57IH7N NEfyb4NUSU6JRWK=
human BB65-RCC cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIr2cppKdmirYnn0bY9vKG:oIHj1cYFvKEKENkWtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PyCwTR?= MlrPV2FPT0WU
human D-566MG cell NF65TZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUHBOY9EUW6qaXLpeIlwdiCxZjDoeY1idiCGLUW2Om1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py5zNjDuUS=> M3PQSnNCVkeHUh?=
human MDA468 cells NWqw[|UyWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXG4RohMOyCmYYnz NXL4NpBLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGE1PjhiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VWyCjc4PhfUwhUUN3ME24JI5O M1jYPFIyPDN6NUe5
human HO-1-N-1 cell NGrhUJdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF05NjJibl2= Mk\xV2FPT0WU
human RS4-11 cell NEnybJBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fDN2lvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE41PSCwTR?= M4XYNXNCVkeHUh?=
human PC-3 cell M1jaR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYfocYhWUW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU4yPCCwTR?= M{fESnNCVkeHUh?=
human NB69 cell M3LT[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTpUGtJUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PiCwTR?= M4nZUnNCVkeHUh?=
human HGC-27 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M37zdGlvcGmkaYTpc44hd2ZiaIXtZY4hUEeFLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU43KG6P NVTXXHFmW0GQR1XS
human NCI-H720 cell Ml35S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{KwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU43OiCwTR?= NXfHPIJPW0GQR1XS
human NCI-H292 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYDJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU45PCCwTR?= MkXFV2FPT0WU
human A3-KAW cell NHnPdZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWjJcohq[mm2aX;uJI9nKGi3bXHuJGE{NUuDVzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlQ{KG6P MVLTRW5ITVJ?
human DU-4475 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfYOoZKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS55MzDuUS=> M1rDRnNCVkeHUh?=
human HuH-7 cell M4rC[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVXJcohq[mm2aX;uJI9nKGi3bXHuJGh2UC15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|Ihdk1? MWDTRW5ITVJ?
human J-RT3-T3-5 cell M4ezdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJGouWlR|LWSzMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|ODDuUS=> NIHNbJFUSU6JRWK=
human VM-CUB-1 cell NXzPVYxsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF7Ne4hKdmirYnn0bY9vKG:oIHj1cYFvKF[PLVPVRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkegcm0> MXTTRW5ITVJ?
human MOLT-16 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGjTPINKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi56NDDuUS=> MoLwV2FPT0WU
human KG-1 cell NWjL[YhNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3:zcmlvcGmkaYTpc44hd2ZiaIXtZY4hU0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlkhdk1? NXHqcW9RW0GQR1XS
human P12-ICHIKAWA cell M1PqTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnPTTY5pcWKrdHnvckBw\iCqdX3hckBROTJvSVPITWtCX0FiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNUBvVQ>? NIH0XHZUSU6JRWK=
human ACN cell NXnrNHhYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYrJcohq[mm2aX;uJI9nKGi3bXHuJGFEViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCyJI5O M1HPZnNCVkeHUh?=
human COLO-684 cell MlLFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUf2U5ZCUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY5PCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkOxJI5O NEfnSYFUSU6JRWK=
human T-24 cell M{joeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkW4TY5pcWKrdHnvckBw\iCqdX3hckBVNTJ2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuPFYhdk1? MXTTRW5ITVJ?
human AGS cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH3SdmVKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P MormV2FPT0WU
human EW-13 cell NFKzdndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2GzUWlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PCCwTR?= M2D2e3NCVkeHUh?=
human SW962 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEXyPYtKdmirYnn0bY9vKG:oIHj1cYFvKFOZOU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPTlibl2= NXLxUm9yW0GQR1XS
human EW-11 cell Mn\IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUf6c5VUUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZibl2= MmnGV2FPT0WU
human RXF393 cell MlSwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1z3fGlvcGmkaYTpc44hd2ZiaIXtZY4hWliIM{mzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPjZibl2= M{jwT3NCVkeHUh?=
human EoL-1-cell cell MoPMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFX0cXhKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNj6xJI5O NWCyO2RVW0GQR1XS

... 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:

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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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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