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 22 Publications

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 MlO5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYPwTpFUUW6qaXLpeIlwdiCxZjDoeY1idiCKU1OtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTF|IH7N NIj5WFJUSU6JRWK=
human L-363 cell M1mwOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXXTY5pcWKrdHnvckBw\iCqdX3hckBNNTN4MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQzKG6P Mm\6V2FPT0WU
human Ramos-2G6-4C10 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUTWO3NuUW6qaXLpeIlwdiCxZjDoeY1idiCUYX3vd{0zTzZvNFOxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzR{IH7N NGrKRo9USU6JRWK=
human SBC-1 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3LzbmlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= MWLTRW5ITVJ?
human MHH-PREB-1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWDJcohq[mm2aX;uJI9nKGi3bXHuJG1JUC2SUlXCMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR7NTDuUS=> MknWV2FPT0WU
human LNCAP cells MnzMVJJwdGmoZYLheIlwdiCjc4PhfS=> M3TMWlMh\GG7cx?= MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGOgZZN{[XluIFnDOVA:OC53IH7N MXKyNVQ{QDV5OR?=
human HH cell NE\QOVRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLSRY5PUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlY1KG6P MkPOV2FPT0WU
human TYK-nu cell Mm\uS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1PibWlvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44Pzhibl2= MYrTRW5ITVJ?
human H4 cell NX30Tpd5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXnJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yNzDuUS=> NIjXepdUSU6JRWK=
human K5 cell NUjoOZg{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NETpUGlKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zN{BvVQ>? MmfCV2FPT0WU
human PA-1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlfaTY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? M{XneHNCVkeHUh?=
human SK-NEP-1 cell M3i4c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV7tOWU2UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OSXAuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEmgcm0> NILrVopUSU6JRWK=
human 697 cell NHrTWlhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3:2WmlvcGmkaYTpc44hd2ZiaIXtZY4hPjl5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63JI5O MYfTRW5ITVJ?
human CTB-1 cell M3PzR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65N{BvVQ>? MmDQV2FPT0WU
human DB cell NH[3WWtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXXNYkxUW6qaXLpeIlwdiCxZjDoeY1idiCGQjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVIhdk1? NH;0cJVUSU6JRWK=
human MLMA cell M3n0dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVHMe|JmUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= MmPzV2FPT0WU
human GAMG cell Mn\zS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\2UGlvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPFIhdk1? MWPTRW5ITVJ?
human JVM-3 cell M37ZXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEnTU2FKdmirYnn0bY9vKG:oIHj1cYFvKEqYTT2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTR?= M4KxSHNCVkeHUh?=
human LAMA-84 cell M1ywXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFTlcVdKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB|IH7N MVHTRW5ITVJ?
human RPMI-8226 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2fiO2lvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST24NlI3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5zNTDuUS=> MWPTRW5ITVJ?
human MOLT-4 cell NI\SXYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37QemlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{OSCwTR?= MYHTRW5ITVJ?
human CAMA-1 cell MkDPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXv0fIJoUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd5IH7N MW\TRW5ITVJ?
human NCI-SNU-1 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2VTmWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDFibl2= NV3Qdm5NW0GQR1XS
human SW780 cell M2rpZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVH0RWxWUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDNibl2= MX\TRW5ITVJ?
human H9 cell NHXXfmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYXETVl1UW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFghdk1? NUKxe5FCW0GQR1XS
human BE-13 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND65NUBvVQ>? NVG1bG9QW0GQR1XS
human ES8 cell Ml:xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUPBTFJTUW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlI4KG6P MnXqV2FPT0WU
human DEL cell NHzCXnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVjmNJJXUW6qaXLpeIlwdiCxZjDoeY1idiCGRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ3KG6P NFjCOYpUSU6JRWK=
human QIMR-WIL cell M1rUbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{L0bGlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjdzIH7N M3vVeHNCVkeHUh?=
human CGTH-W-1 cell MoW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2T6SWlvcGmkaYTpc44hd2ZiaIXtZY4hS0eWSD3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njd3IH7N NWfpNnluW0GQR1XS
human CHL-1 cell NIDCTHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkDGTY5pcWKrdHnvckBw\iCqdX3hckBEUExvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFYhdk1? NGXHNoNUSU6JRWK=
human A2780 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlLOTY5pcWKrdHnvckBw\iCqdX3hckBCOjd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFghdk1? M1LKWXNCVkeHUh?=
human VA-ES-BJ cell NFT3SFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIHvTZVKdmirYnn0bY9vKG:oIHj1cYFvKF[DLVXTMWJLKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57IH7N MXrTRW5ITVJ?
human BB65-RCC cell NYHlUpVmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGJDPjVvUlPDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{BvVQ>? M3;FVnNCVkeHUh?=
human D-566MG cell NEHh[2VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2DVfWlvcGmkaYTpc44hd2ZiaIXtZY4hTC13Nk\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOTZibl2= Ml[zV2FPT0WU
human MDA468 cells NUC5PIFtWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlPLN{Bl[Xm| MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQUS2PEBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTTJIF{e2G7LDDJR|UxRThibl2= NFviTYgzOTR|OEW3PS=>
human HO-1-N-1 cell M2D1Smdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWDJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF05NjJibl2= Mlu5V2FPT0WU
human RS4-11 cell Ml7BS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFHmOVFKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvPDVibl2= NXPnTpdzW0GQR1XS
human PC-3 cell MlvvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHu4NnpKdmirYnn0bY9vKG:oIHj1cYFvKFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlE1KG6P NUH3UFlTW0GQR1XS
human NB69 cell MlLuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXSwRm1OUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PiCwTR?= NWfh[nptW0GQR1XS
human HGC-27 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoDXTY5pcWKrdHnvckBw\iCqdX3hckBJT0NvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlYhdk1? M125OnNCVkeHUh?=
human NCI-H720 cell MnHxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M33OdGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3NlAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZ{IH7N MkfZV2FPT0WU
human NCI-H292 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2\Y[GlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N M{H0W3NCVkeHUh?=
human A3-KAW cell NGP0ZWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2nVemlvcGmkaYTpc44hd2ZiaIXtZY4hSTNvS1HXJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvPDNibl2= M2\IfnNCVkeHUh?=
human DU-4475 cell NXuwU3JET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXeyZYtNUW6qaXLpeIlwdiCxZjDoeY1idiCGVT20OFc2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwN{Ogcm0> Mm\0V2FPT0WU
human HuH-7 cell NFPnS3NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3Py[WlvcGmkaYTpc44hd2ZiaIXtZY4hUHWKLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk4{OiCwTR?= Mk\WV2FPT0WU
human J-RT3-T3-5 cell M{nWOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFPR[YJKdmirYnn0bY9vKG:oIHj1cYFvKEpvUmSzMXQ{NTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj6zPEBvVQ>? MorUV2FPT0WU
human VM-CUB-1 cell NF[1TnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NE\i[o5KdmirYnn0bY9vKG:oIHj1cYFvKF[PLVPVRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkegcm0> M4KxNXNCVkeHUh?=
human MOLT-16 cell MonPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVXhOmg3UW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwOESgcm0> Ml\FV2FPT0WU
human KG-1 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1j4cGlvcGmkaYTpc44hd2ZiaIXtZY4hU0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlkhdk1? NWG0Z4JjW0GQR1XS
human P12-ICHIKAWA cell NW\KT45DT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKGi3bXHuJHAyOi2LQ1jJT2FYSSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCxJI5O MkG1V2FPT0WU
human ACN cell MlnLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWDJcohq[mm2aX;uJI9nKGi3bXHuJGFEViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCyJI5O NEjacYdUSU6JRWK=
human COLO-684 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3HWUGlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22PFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy5|MTDuUS=> Mn6xV2FPT0WU
human T-24 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn3yTY5pcWKrdHnvckBw\iCqdX3hckBVNTJ2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuPFYhdk1? MWXTRW5ITVJ?
human AGS cell NHvmU5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mme5TY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND6xNUBvVQ>? NXrSOZZzW0GQR1XS
human EW-13 cell NHfCOYxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoDkTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlU1KG6P MXPTRW5ITVJ?
human SW962 cell NF\JSmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWrxdGFYUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjV7IH7N NEHEXG5USU6JRWK=
human EW-11 cell NWjPO45VT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXWXFFKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPiCwTR?= M1\NRnNCVkeHUh?=
human RXF393 cell NFjz[lZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH;TUmNKdmirYnn0bY9vKG:oIHj1cYFvKFK[RkO5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZ4IH7N M33VSHNCVkeHUh?=
human EoL-1-cell cell NIfrZopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFL6fFlKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNj6xJI5O M1vWbnNCVkeHUh?=

... 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]

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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]

+ 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. February 2019 Phase 1
NCT03203525 Not yet recruiting Liver Cancer M.D. Anderson Cancer Center|NovoCure Ltd. February 2019 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
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

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