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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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 MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHvI[2RKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTNibl2= MlfoV2FPT0WU
human L-363 cell NVfLTlVoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NULE[FZSUW6qaXLpeIlwdiCxZjDoeY1idiCOLUO2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjR{IH7N NFS5TG5USU6JRWK=
human Ramos-2G6-4C10 cell NHXXc|dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlzRTY5pcWKrdHnvckBw\iCqdX3hckBT[W2xcz2yS|YuPENzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|QzKG6P MVXTRW5ITVJ?
human SBC-1 cell NH7rdZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NY[1foQ5UW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDR2IH7N M3;Kb3NCVkeHUh?=
human MHH-PREB-1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NG\icndKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3QVmVDNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5OUBvVQ>? NX;GTYRXW0GQR1XS
human LNCAP cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 MVezJIRigXN? NYjBVFM3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUCuOUBvVQ>? MlTRNlE1Ozh3N{m=
human HH cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn2yTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNk[0JI5O NV[1OnoxW0GQR1XS
human TYK-nu cell NH\SWmhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MojJTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc4QCCwTR?= MnHIV2FPT0WU
human H4 cell NIHtbYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fJWWlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC3JI5O M{W3b3NCVkeHUh?=
human K5 cell NEjBR3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkK3TY5pcWKrdHnvckBw\iCqdX3hckBMPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwM{Ogcm0> MXrTRW5ITVJ?
human PA-1 cell NUTlepBYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJHBCNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkS3JI5O NXnyNGozW0GQR1XS
human SK-NEP-1 cell MkXTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mo\ETY5pcWKrdHnvckBw\iCqdX3hckBUUy2QRWCtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDlibl2= M2DNV3NCVkeHUh?=
human 697 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlnhTY5pcWKrdHnvckBw\iCqdX3hckA3QTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkegcm0> NYKyWVBkW0GQR1XS
human CTB-1 cell NYX6[3l1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFP4c5lKdmirYnn0bY9vKG:oIHj1cYFvKEOWQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk46OyCwTR?= NXH3dFhCW0GQR1XS
human DB cell NU\5[4ZvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4DUeGlvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O M4fTbXNCVkeHUh?=
human MLMA cell NYfROYlHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NY\OVopHUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= M1jiXXNCVkeHUh?=
human GAMG cell NYDNU|ZrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXi1S4luUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OiCwTR?= MlLhV2FPT0WU
human JVM-3 cell NFXNb5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIPqenFKdmirYnn0bY9vKG:oIHj1cYFvKEqYTT2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTR?= MYrTRW5ITVJ?
human LAMA-84 cell NITwSHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;rRWlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODNibl2= Mn\UV2FPT0WU
human RPMI-8226 cell NUTmO2dWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvOEKyOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTVibl2= M3;kcnNCVkeHUh?=
human MOLT-4 cell Mkn1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1HmcGlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{OSCwTR?= NGDTNpRUSU6JRWK=
human CAMA-1 cell MmDlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEnteVlKdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzdibl2= M3SyW3NCVkeHUh?=
human NCI-SNU-1 cell Ml;RS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\0TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjhzIH7N MkPKV2FPT0WU
human SW780 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3va[WlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{KG6P MmDDV2FPT0WU
human H9 cell NFfifW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;VSGlvcGmkaYTpc44hd2ZiaIXtZY4hUDliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lki4JI5O MXPTRW5ITVJ?
human BE-13 cell M4TTU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVfYdIFZUW6qaXLpeIlwdiCxZjDoeY1idiCERT2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTFibl2= MX\TRW5ITVJ?
human ES8 cell M4S2XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{jxS2lvcGmkaYTpc44hd2ZiaIXtZY4hTVN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6yO{BvVQ>? NVrZUnplW0GQR1XS
human DEL cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWXGVZFyUW6qaXLpeIlwdiCxZjDoeY1idiCGRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ3KG6P MVfTRW5ITVJ?
human QIMR-WIL cell MnK5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnPETY5pcWKrdHnvckBw\iCqdX3hckBSUU2ULWfJUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzFibl2= M{SwfHNCVkeHUh?=
human CGTH-W-1 cell NGrYS4ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoOwTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzVibl2= MVTTRW5ITVJ?
human CHL-1 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX3HfVZbUW6qaXLpeIlwdiCxZjDoeY1idiCFSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDZibl2= Mki0V2FPT0WU
human A2780 cell MnjrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEXZWm5KdmirYnn0bY9vKG:oIHj1cYFvKEF{N{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU45QCCwTR?= NXTKO5hMW0GQR1XS
human VA-ES-BJ cell NUDIfWptT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVLJcohq[mm2aX;uJI9nKGi3bXHuJHZCNUWVLVLKJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU46KG6P M2\adnNCVkeHUh?=
human BB65-RCC cell MkXMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\ITY5pcWKrdHnvckBw\iCqdX3hckBDSjZ3LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVchdk1? NUW3cW5yW0GQR1XS
human D-566MG cell NFnzT5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NED2[5NKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjF4IH7N MV7TRW5ITVJ?
human MDA468 cells NEXYcIFRem:uaX\ldoF1cW:wIHHzd4F6 MVSzJIRigXN? MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQUS2PEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRThibl2= NGXIZnczOTR|OEW3PS=>
human HO-1-N-1 cell NUPa[opsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF05NjJibl2= MVTTRW5ITVJ?
human RS4-11 cell MoPNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHvNTXhKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvPDVibl2= MlKwV2FPT0WU
human PC-3 cell NGfpZlVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHfDdotKdmirYnn0bY9vKG:oIHj1cYFvKFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlE1KG6P NXfxSoU6W0GQR1XS
human NB69 cell Mn\NS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkS2JI5O MXfTRW5ITVJ?
human HGC-27 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWTJcohq[mm2aX;uJI9nKGi3bXHuJGhISy1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOkBvVQ>? MmOyV2FPT0WU
human NCI-H720 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MojzTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEeyNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPjJibl2= NWrTUoxWW0GQR1XS
human NCI-H292 cell NWHEco03T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3fobGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N MULTRW5ITVJ?
human A3-KAW cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnLTTY5pcWKrdHnvckBw\iCqdX3hckBCOy2NQWegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE41OyCwTR?= NWfSd5lKW0GQR1XS
human DU-4475 cell MoPQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{OwVGlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjd|IH7N Ml7RV2FPT0WU
human HuH-7 cell M33QdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nRdGlvcGmkaYTpc44hd2ZiaIXtZY4hUHWKLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk4{OiCwTR?= NIH4XVdUSU6JRWK=
human J-RT3-T3-5 cell NH;r[5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkT2TY5pcWKrdHnvckBw\iCqdX3hckBLNVKWMz3UN{02KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwM{igcm0> MoWxV2FPT0WU
human VM-CUB-1 cell NFXPeY9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1H3NmlvcGmkaYTpc44hd2ZiaIXtZY4hXk1vQ2XCMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi54NzDuUS=> NHPlNoNUSU6JRWK=
human MOLT-16 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk45PCCwTR?= NHjU[nZUSU6JRWK=
human KG-1 cell MmrkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIDxSJdKdmirYnn0bY9vKG:oIHj1cYFvKEuJLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk46KG6P M1Xi[XNCVkeHUh?=
human P12-ICHIKAWA cell M4n6SWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVTPS41UUW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOSCwTR?= M1PjeXNCVkeHUh?=
human ACN cell MmPiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1SyPWlvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFIhdk1? MnfPV2FPT0WU
human COLO-684 cell M3HkeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2XNdWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22PFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy5|MTDuUS=> M4PwbHNCVkeHUh?=
human T-24 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWDoVlFoUW6qaXLpeIlwdiCxZjDoeY1idiCWLUK0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvQDZibl2= M1;O[HNCVkeHUh?=
human AGS cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlrFTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND6xNUBvVQ>? MWjTRW5ITVJ?
human EW-13 cell NX;jfoJKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn\QTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlU1KG6P NHzPcZhUSU6JRWK=
human SW962 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXTJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOVkhdk1? MUXTRW5ITVJ?
human EW-11 cell MljBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmnnTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlYhdk1? NYG1[oFpW0GQR1XS
human RXF393 cell NULVWnFiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHziUYRKdmirYnn0bY9vKG:oIHj1cYFvKFK[RkO5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZ4IH7N MnS0V2FPT0WU
human EoL-1-cell cell M{DDfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mkf3TY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwMTDuUS=> NH\TNVNUSU6JRWK=

... 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]

+ Expand

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 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

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

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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