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 NVe3VlZnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGDmOHpKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yOTNibl2= M4[4TnNCVkeHUh?=
human L-363 cell NWriVnpOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIT0S2ZKdmirYnn0bY9vKG:oIHj1cYFvKExvM{[zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPDJibl2= NIriVFBUSU6JRWK=
human Ramos-2G6-4C10 cell NYnhZpRwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWnZS5A5UW6qaXLpeIlwdiCxZjDoeY1idiCUYX3vd{0zTzZvNFOxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzR{IH7N Mlu2V2FPT0WU
human SBC-1 cell NF61SoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{O0Z2lvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= M1\hRnNCVkeHUh?=
human MHH-PREB-1 cell M325O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MorxTY5pcWKrdHnvckBw\iCqdX3hckBOUEhvUGLFRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OUWgcm0> MkDCV2FPT0WU
human LNCAP cells M4PqdHBzd2yrZnXyZZRqd25iYYPzZZk> MXOzJIRigXN? MkjVRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOTlPBVEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRTBwNTDuUS=> MX2yNVQ{QDV5OR?=
human HH cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3rrUWlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[2OEBvVQ>? NWnw[XpZW0GQR1XS
human TYK-nu cell NIfkVmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoS5TY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc4QCCwTR?= NIXFOo1USU6JRWK=
human H4 cell NV36dY9KT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmDSTY5pcWKrdHnvckBw\iCqdX3hckBJPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMEegcm0> NIfrflFUSU6JRWK=
human K5 cell M2jTbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2[zOWlvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOzJI5O MYPTRW5ITVJ?
human PA-1 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkD6TY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? M3;PVXNCVkeHUh?=
human SK-NEP-1 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkDwTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QRWCtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDlibl2= M3PuSHNCVkeHUh?=
human 697 cell M1n0PWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUP5TIFQUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlchdk1? NILCfWxUSU6JRWK=
human CTB-1 cell NFrPUYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XhW2lvcGmkaYTpc44hd2ZiaIXtZY4hS1SELUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlk{KG6P M2HnN3NCVkeHUh?=
human DB cell M1fDeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4LjZWlvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O MWrTRW5ITVJ?
human MLMA cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYPqe|l4UW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= NH7qO4pUSU6JRWK=
human GAMG cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{\BfmlvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPFIhdk1? M{fWWXNCVkeHUh?=
human JVM-3 cell M1Xybmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2OyRWlvcGmkaYTpc44hd2ZiaIXtZY4hUl[PLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2KG6P NGmyV|ZUSU6JRWK=
human LAMA-84 cell Mnv5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWfn[nJTUW6qaXLpeIlwdiCxZjDoeY1idiCOQV3BMVg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yMzDuUS=> NVroSlEyW0GQR1XS
human RPMI-8226 cell M3m0OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2faeGlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST24NlI3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5zNTDuUS=> MUjTRW5ITVJ?
human MOLT-4 cell MkjRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIj3eo1KdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOzFibl2= NXzkeXlXW0GQR1XS
human CAMA-1 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJGNCVUFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|chdk1? NVfNXWUzW0GQR1XS
human NCI-SNU-1 cell M2rNW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXWxe4VLUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkixJI5O MVXTRW5ITVJ?
human SW780 cell NIjSTItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGSxXJZKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45OyCwTR?= NYPtbngxW0GQR1XS
human H9 cell NHLVZmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHHRUHFKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64PEBvVQ>? NWXhR3JYW0GQR1XS
human BE-13 cell NHuy[pZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mm\5TY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVEhdk1? MlPGV2FPT0WU
human ES8 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2jkcWlvcGmkaYTpc44hd2ZiaIXtZY4hTVN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6yO{BvVQ>? MV\TRW5ITVJ?
human DEL cell NUj0ZlVYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2LmNmlvcGmkaYTpc44hd2ZiaIXtZY4hTEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT60OkBvVQ>? M{W0RXNCVkeHUh?=
human QIMR-WIL cell M3PKPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHuWotDUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Ggcm0> M2TPWnNCVkeHUh?=
human CGTH-W-1 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFm2VYFKdmirYnn0bY9vKG:oIHj1cYFvKEOJVFitW{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS55NTDuUS=> NGXRVHNUSU6JRWK=
human CHL-1 cell MmC1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? MVfTRW5ITVJ?
human A2780 cell MofpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUfJcohq[mm2aX;uJI9nKGi3bXHuJGEzPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64PEBvVQ>? NFLNfoFUSU6JRWK=
human VA-ES-BJ cell M1nzUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIfDOplKdmirYnn0bY9vKG:oIHj1cYFvKF[DLVXTMWJLKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57IH7N MnGzV2FPT0WU
human BB65-RCC cell NYfUbmtRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIHFTpFKdmirYnn0bY9vKG:oIHj1cYFvKEKENkWtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PyCwTR?= NWTjd5FUW0GQR1XS
human D-566MG cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{D5VWlvcGmkaYTpc44hd2ZiaIXtZY4hTC13Nk\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOTZibl2= NUOwcYVIW0GQR1XS
human MDA468 cells NIHtZXJRem:uaX\ldoF1cW:wIHHzd4F6 MV6zJIRigXN? MmfnRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFG0Olgh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD16IH7N NYTtU2Z4OjF2M{i1O|k>
human HO-1-N-1 cell NFP0dGVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGXpe4JKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> M4jaSHNCVkeHUh?=
human RS4-11 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLvTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlQ2KG6P MUTTRW5ITVJ?
human PC-3 cell NULjU2J4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1jjO2lvcGmkaYTpc44hd2ZiaIXtZY4hWENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuNVQhdk1? NY\NVpAxW0GQR1XS
human NB69 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYHzOGlDUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PiCwTR?= NX3YeFFIW0GQR1XS
human HGC-27 cell M3:zTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUnwV3NtUW6qaXLpeIlwdiCxZjDoeY1idiCKR1OtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZibl2= MYDTRW5ITVJ?
human NCI-H720 cell M3fzb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWDTWnc2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFczOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwNkKgcm0> NFX6ZotUSU6JRWK=
human NCI-H292 cell NVnJVXdvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUPjdlV[UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwOESgcm0> NHv6dWJUSU6JRWK=
human A3-KAW cell Mn\BS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGC0VnpKdmirYnn0bY9vKG:oIHj1cYFvKEF|LVvBW{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjR|IH7N MlSxV2FPT0WU
human DU-4475 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIDsTI1KdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS55MzDuUS=> M37oRnNCVkeHUh?=
human HuH-7 cell M2HuSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUKwN|lzUW6qaXLpeIlwdiCxZjDoeY1idiCKdVitO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjN{IH7N NGTaOppUSU6JRWK=
human J-RT3-T3-5 cell NFLVUWZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NETUSY1KdmirYnn0bY9vKG:oIHj1cYFvKEpvUmSzMXQ{NTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj6zPEBvVQ>? M2nmVXNCVkeHUh?=
human VM-CUB-1 cell M3\ifWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEHNPFJKdmirYnn0bY9vKG:oIHj1cYFvKF[PLVPVRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkegcm0> MoLiV2FPT0WU
human MOLT-16 cell M1LZb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVfJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk45PCCwTR?= M3zlOXNCVkeHUh?=
human KG-1 cell NUDMVmdIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUK2ephLUW6qaXLpeIlwdiCxZjDoeY1idiCNRz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvQSCwTR?= MWPTRW5ITVJ?
human P12-ICHIKAWA cell MoH3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3;aRmlvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFEhdk1? M4\ZbXNCVkeHUh?=
human ACN cell MmPNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYXJcohq[mm2aX;uJI9nKGi3bXHuJGFEViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCyJI5O NUewNXJvW0GQR1XS
human COLO-684 cell M1jsNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoOyTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjNzIH7N NV\R[JFkW0GQR1XS
human T-24 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVP6foJKUW6qaXLpeIlwdiCxZjDoeY1idiCWLUK0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvQDZibl2= M{DNT3NCVkeHUh?=
human AGS cell NF72VGlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLjTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND6xNUBvVQ>? MY\TRW5ITVJ?
human EW-13 cell NGToUlRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYHaPFY3UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV2IH7N MVvTRW5ITVJ?
human SW962 cell NH;oOYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4TjOGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU42QSCwTR?= MUTTRW5ITVJ?
human EW-11 cell M3zsc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1i0bmlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU43KG6P MX3TRW5ITVJ?
human RXF393 cell MonwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NES2dmRKdmirYnn0bY9vKG:oIHj1cYFvKFK[RkO5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZ4IH7N NWnGbWdJW0GQR1XS
human EoL-1-cell cell M1;yT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGP2doZKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNj6xJI5O NF[zV3hUSU6JRWK=

... 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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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID