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 NI\6WFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4\XSWlvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyOyCwTR?= MlfFV2FPT0WU
human L-363 cell M{fDcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlrOTY5pcWKrdHnvckBw\iCqdX3hckBNNTN4MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQzKG6P MU\TRW5ITVJ?
human Ramos-2G6-4C10 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{nQWGlvcGmkaYTpc44hd2ZiaIXtZY4hWmGvb4OtNmc3NTSFMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM1OiCwTR?= MXHTRW5ITVJ?
human SBC-1 cell Mk\YS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M33HWWlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= NUjz[WRzW0GQR1XS
human MHH-PREB-1 cell NGLh[GFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVLWc29vUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitVHJGSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVUhdk1? NV3zOnE{W0GQR1XS
human LNCAP cells MXfQdo9tcW[ncnH0bY9vKGG|c3H5 MVKzJIRigXN? NISwT4dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;MD61JI5O NUDVdZZrOjF2M{i1O|k>
human HH cell MmfLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{\r[WlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[2OEBvVQ>? NUjHU4tNW0GQR1XS
human TYK-nu cell M2DrUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXq5Z2NCUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd5ODDuUS=> NXPaPZhpW0GQR1XS
human H4 cell NYnzfY9{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2r2T2lvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC3JI5O M3PxVnNCVkeHUh?=
human K5 cell M3\lVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV7FTpB7UW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Mhdk1? MVrTRW5ITVJ?
human PA-1 cell NX\IVWo5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFOyc3ZKdmirYnn0bY9vKG:oIHj1cYFvKFCDLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlQ4KG6P NX73bIRtW0GQR1XS
human SK-NEP-1 cell NUnSelNXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH6ybIZKdmirYnn0bY9vKG:oIHj1cYFvKFONLV7FVE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52OTDuUS=> MVTTRW5ITVJ?
human 697 cell NUW4OlJ{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4TWNGlvcGmkaYTpc44hd2ZiaIXtZY4hPjl5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63JI5O NYrET5o3W0GQR1XS
human CTB-1 cell M{PI[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHP4O21KdmirYnn0bY9vKG:oIHj1cYFvKEOWQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk46OyCwTR?= NED5Wm5USU6JRWK=
human DB cell NFKxbmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoPzTY5pcWKrdHnvckBw\iCqdX3hckBFSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwMUKgcm0> M3fiUXNCVkeHUh?=
human MLMA cell NXXS[41IT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NU\yfHZvUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= NEGyWFFUSU6JRWK=
human GAMG cell MnvLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYnBbJRyUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OiCwTR?= MVPTRW5ITVJ?
human JVM-3 cell Mmi3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1[3dGlvcGmkaYTpc44hd2ZiaIXtZY4hUl[PLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2KG6P M1jjTXNCVkeHUh?=
human LAMA-84 cell NHy4THJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{j1cmlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODNibl2= MWTTRW5ITVJ?
human RPMI-8226 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX\mfWtDUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O MnryV2FPT0WU
human MOLT-4 cell NUXEPHBnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF\lVZBKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOzFibl2= NWG0PYxIW0GQR1XS
human CAMA-1 cell M17oRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWfG[lJGUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd5IH7N MkfGV2FPT0WU
human NCI-SNU-1 cell Mn;DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3;KUGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLWPOWU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56MTDuUS=> NWDubXM{W0GQR1XS
human SW780 cell NVW5To9DT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGnLbW9KdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45OyCwTR?= NVW1fWI{W0GQR1XS
human H9 cell NF\aeHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIHVWIhKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64PEBvVQ>? M4S2U3NCVkeHUh?=
human BE-13 cell M2rZVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\ENGlvcGmkaYTpc44hd2ZiaIXtZY4hSkVvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlkyKG6P MVLTRW5ITVJ?
human ES8 cell NXn1Tm86T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MULJcohq[mm2aX;uJI9nKGi3bXHuJGVUQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwMkegcm0> MmfuV2FPT0WU
human DEL cell M1;4W2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFHoSVRKdmirYnn0bY9vKG:oIHj1cYFvKESHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuOFYhdk1? MlL6V2FPT0WU
human QIMR-WIL cell MnrpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44OSCwTR?= MnTBV2FPT0WU
human CGTH-W-1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfmS4NKdmirYnn0bY9vKG:oIHj1cYFvKEOJVFitW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS55NTDuUS=> NULMPHc2W0GQR1XS
human CHL-1 cell MlywS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmrpTY5pcWKrdHnvckBw\iCqdX3hckBEUExvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFYhdk1? MUHTRW5ITVJ?
human A2780 cell MlHZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHXK[2lKdmirYnn0bY9vKG:oIHj1cYFvKEF{N{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU45QCCwTR?= NWHueVJEW0GQR1XS
human VA-ES-BJ cell NH3IcoFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3r6emlvcGmkaYTpc44hd2ZiaIXtZY4hXkFvRWOtRmoh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njlibl2= M4jXXHNCVkeHUh?=
human BB65-RCC cell NIjme3pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJGJDPjVvUlPDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{BvVQ>? MX3TRW5ITVJ?
human D-566MG cell M{jrOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3H4RWlvcGmkaYTpc44hd2ZiaIXtZY4hTC13Nk\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOTZibl2= M1iz[nNCVkeHUh?=
human MDA468 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 MkX0N{Bl[Xm| NHzQTG5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERVQ3QCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUigcm0> MnvJNlE1Ozh3N{m=
human HO-1-N-1 cell NF\2OZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHvJbXZKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> M3fybHNCVkeHUh?=
human RS4-11 cell NUK5bIVrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmDDTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlQ2KG6P M3rue3NCVkeHUh?=
human PC-3 cell NXHtUnpbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHBENTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkG0JI5O NYXMcohQW0GQR1XS
human NB69 cell Ml:yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIXwWJFKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ3KG6P MlLHV2FPT0WU
human HGC-27 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYDJcohq[mm2aX;uJI9nKGi3bXHuJGhISy1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOkBvVQ>? NHf1NlFUSU6JRWK=
human NCI-H720 cell MmPrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2njSWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3NlAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZ{IH7N MlzpV2FPT0WU
human NCI-H292 cell NFXH[5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH3vXGJKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS56NDDuUS=> NEf0NHBUSU6JRWK=
human A3-KAW cell M3W4WWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYfBZpBFUW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC52MzDuUS=> NH:4dWZUSU6JRWK=
human DU-4475 cell NG\tVJZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWn6eXdrUW6qaXLpeIlwdiCxZjDoeY1idiCGVT20OFc2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwN{Ogcm0> M2HNTXNCVkeHUh?=
human HuH-7 cell NWrETlhST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUL6UWtuUW6qaXLpeIlwdiCxZjDoeY1idiCKdVitO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjN{IH7N NG\BW49USU6JRWK=
human J-RT3-T3-5 cell MlTYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2LMSWlvcGmkaYTpc44hd2ZiaIXtZY4hUi2UVEOtWFMuPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{LkO4JI5O MYjTRW5ITVJ?
human VM-CUB-1 cell MmjFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkjiTY5pcWKrdHnvckBw\iCqdX3hckBXVS2FVVKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjZ5IH7N MVnTRW5ITVJ?
human MOLT-16 cell M{\Hemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEDyUZFKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi56NDDuUS=> MVrTRW5ITVJ?
human KG-1 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYrJcohq[mm2aX;uJI9nKGi3bXHuJGtINTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj65JI5O NVXE[3BtW0GQR1XS
human P12-ICHIKAWA cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYO4fGlrUW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOSCwTR?= MXXTRW5ITVJ?
human ACN cell M{O0emdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJGFEViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCyJI5O NYP6VYFmW0GQR1XS
human COLO-684 cell NITqVWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlPZTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjNzIH7N NULH[pFvW0GQR1XS
human T-24 cell NVrRXVk5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYfJcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz64OkBvVQ>? NWLBNVNJW0GQR1XS
human AGS cell NX3XW5hUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mm\tTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND6xNUBvVQ>? MnPlV2FPT0WU
human EW-13 cell NW[xUXo{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUnYUmlLUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV2IH7N NWi1PGl[W0GQR1XS
human SW962 cell M{XsW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPrcZI2UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjV7IH7N M3[4WnNCVkeHUh?=
human EW-11 cell NHntWolIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWfONYxSUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZibl2= MVPTRW5ITVJ?
human RXF393 cell M3TtTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUXsUFllUW6qaXLpeIlwdiCxZjDoeY1idiCUWF[zPVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS54NjDuUS=> NXTTXGtMW0GQR1XS
human EoL-1-cell cell M3;POWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXTJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi5zIH7N MYHTRW5ITVJ?

... 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03203525 Not yet recruiting Liver Cancer M.D. Anderson Cancer Center|NovoCure Ltd. December 2018 Phase 1
NCT03158389 Recruiting Glioblastoma Adult University Hospital Heidelberg|German Cancer Aid|German Cancer Research Center|National Center for Tumor Diseases Heidelberg May 7 2018 Phase 1|Phase 2
NCT03571438 Recruiting Kidney Cancer University Hospital Grenoble October 16 2017 Not Applicable
NCT03297606 Recruiting Lymphoma Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors Canadian Cancer Trials Group|AstraZeneca|Bristol-Myers Squibb|Hoffmann-La Roche|Pfizer October 6 2017 Phase 2
NCT02908035 Recruiting Chronic Limb Ischemia Mercator MedSystems Inc. March 3 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 23 2016 Phase 3

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID