Temsirolimus (CCI-779)

For research use only.

Licensed by Pfizer Catalog No.S1044 Synonyms: NSC 683864

48 publications

Temsirolimus (CCI-779) 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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Selleck's Temsirolimus (CCI-779) has been cited by 48 publications

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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 MnzvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4nnVmlvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyOyCwTR?= NFXiTVZUSU6JRWK=
human L-363 cell NWLMZmp4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUfJcohq[mm2aX;uJI9nKGi3bXHuJGwuOzZ|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFIhdk1? NWrZTFBLW0GQR1XS
human Ramos-2G6-4C10 cell MnPOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVTJcohq[mm2aX;uJI9nKGi3bXHuJHJidW:|LULHOk01SzFyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOFIhdk1? NYXoTYt5W0GQR1XS
human SBC-1 cell M2jXRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUX3TpNJUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDR2IH7N MmHoV2FPT0WU
human MHH-PREB-1 cell M4DFOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGfhSmtKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3QVmVDNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5OUBvVQ>? MnHFV2FPT0WU
human LNCAP cells NX\1c4Q{WHKxbHnm[ZJifGmxbjDhd5NigQ>? M{HlZlMh\GG7cx?= M1PQXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD1yLkWgcm0> MkXwNlE1Ozh3N{m=
human HH cell M3zDeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2ri[WlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[2OEBvVQ>? NHXmN5lUSU6JRWK=
human TYK-nu cell MofUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEHxe5BKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzd6IH7N M4fPNXNCVkeHUh?=
human H4 cell NEW1SndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2nCemlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC3JI5O MXzTRW5ITVJ?
human K5 cell M4nLUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEjWOZNKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zN{BvVQ>? NWj3SWJMW0GQR1XS
human PA-1 cell M17J[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4fwPGlvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOFchdk1? M4nDe3NCVkeHUh?=
human SK-NEP-1 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHrJSllKdmirYnn0bY9vKG:oIHj1cYFvKFONLV7FVE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52OTDuUS=> M1zGN3NCVkeHUh?=
human 697 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUPoZ3FiUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlchdk1? NFvjfFRUSU6JRWK=
human CTB-1 cell MmD1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHSzSolKdmirYnn0bY9vKG:oIHj1cYFvKEOWQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk46OyCwTR?= M1KwbnNCVkeHUh?=
human DB cell M172dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4fHW2lvcGmkaYTpc44hd2ZiaIXtZY4hTEJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkGyJI5O M1vXVXNCVkeHUh?=
human MLMA cell MmH3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF\jXodKdmirYnn0bY9vKG:oIHj1cYFvKE2OTVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlMyKG6P MXjTRW5ITVJ?
human GAMG cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFOzTYNKdmirYnn0bY9vKG:oIHj1cYFvKEeDTVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlgzKG6P NUDnV5pxW0GQR1XS
human JVM-3 cell NHnHRpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHTyR4hKdmirYnn0bY9vKG:oIHj1cYFvKEqYTT2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTR?= NXfiUIFtW0GQR1XS
human LAMA-84 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPTTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xOyCwTR?= MY\TRW5ITVJ?
human RPMI-8226 cell NGLJO5VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlfSTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUiyNlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjF3IH7N NGLMSlhUSU6JRWK=
human MOLT-4 cell NF;FZmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1PWN2lvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{OSCwTR?= NF3UW5hUSU6JRWK=
human CAMA-1 cell NGD5c|BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1PZN2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44PyCwTR?= MnH4V2FPT0WU
human NCI-SNU-1 cell MlXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{nLc2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLWPOWU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56MTDuUS=> M4H2THNCVkeHUh?=
human SW780 cell M4O2[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX;MfnQ1UW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDNibl2= NHrId3lUSU6JRWK=
human H9 cell MmmyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE\t[XVKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64PEBvVQ>? NVjJWppQW0GQR1XS
human BE-13 cell M1WwbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXW2WXZiUW6qaXLpeIlwdiCxZjDoeY1idiCERT2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTFibl2= NUjJempnW0GQR1XS
human ES8 cell NHvOPHVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnfJTY5pcWKrdHnvckBw\iCqdX3hckBGWzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkK3JI5O Ml\BV2FPT0WU
human DEL cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUfJcohq[mm2aX;uJI9nKGi3bXHuJGRGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNE[gcm0> NXjocJBnW0GQR1XS
human QIMR-WIL cell M4nP[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUHJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44OSCwTR?= MoSzV2FPT0WU
human CGTH-W-1 cell M37zNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlLVTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzVibl2= NFjzRmdUSU6JRWK=
human CHL-1 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? NV:xVYtPW0GQR1XS
human A2780 cell M1TjNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{fvOGlvcGmkaYTpc44hd2ZiaIXtZY4hSTJ5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg5KG6P MWDTRW5ITVJ?
human VA-ES-BJ cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NU\LOZUxUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> NH;mUplUSU6JRWK=
human BB65-RCC cell NGDBR3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJGJDPjVvUlPDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{BvVQ>? MUfTRW5ITVJ?
human D-566MG cell NE[4TVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGQuPTZ4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23MlE3KG6P NV\OeVlMW0GQR1XS
human MDA468 cells Ml3zVJJwdGmoZYLheIlwdiCjc4PhfS=> NWnKSWRLOyCmYYnz MlHFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFG0Olgh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD16IH7N M3XFWVIyPDN6NUe5
human HO-1-N-1 cell M{DSTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHHHSpBKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> M3uxR3NCVkeHUh?=
human RS4-11 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkjWTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlQ2KG6P M{m3U3NCVkeHUh?=
human PC-3 cell NYDm[JBpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoC3TY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OT6xOEBvVQ>? NYrNNHd[W0GQR1XS
human NB69 cell M{\Zdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3PrSmlvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOFYhdk1? NUfL[o8{W0GQR1XS
human HGC-27 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofaTY5pcWKrdHnvckBw\iCqdX3hckBJT0NvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlYhdk1? MWTTRW5ITVJ?
human NCI-H720 cell MoDWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIHHXVhKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|IxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS54MjDuUS=> MYLTRW5ITVJ?
human NCI-H292 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHzRTWVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS56NDDuUS=> NU\v[olkW0GQR1XS
human A3-KAW cell MoP0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn7LTY5pcWKrdHnvckBw\iCqdX3hckBCOy2NQWegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE41OyCwTR?= NHix[JhUSU6JRWK=
human DU-4475 cell M320bGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2f5[GlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjd|IH7N MWnTRW5ITVJ?
human HuH-7 cell NVP5[GlVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGj5fo9KdmirYnn0bY9vKG:oIHj1cYFvKEi3SD23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvOzJibl2= M37zVnNCVkeHUh?=
human J-RT3-T3-5 cell NXXwTWZ7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGouWlR|LWSzMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|ODDuUS=> NGfLZW5USU6JRWK=
human VM-CUB-1 cell MkDzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M13tfmlvcGmkaYTpc44hd2ZiaIXtZY4hXk1vQ2XCMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi54NzDuUS=> NEfGcI9USU6JRWK=
human MOLT-16 cell NIjYfWlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHn1eZlKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi56NDDuUS=> NFzISItUSU6JRWK=
human KG-1 cell NWC5PVdbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF;YZ5VKdmirYnn0bY9vKG:oIHj1cYFvKEuJLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk46KG6P M2n6cHNCVkeHUh?=
human P12-ICHIKAWA cell NELD[4xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1XOTGlvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFEhdk1? MXHTRW5ITVJ?
human ACN cell M4j1eWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{H3R2lvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFIhdk1? NHq1WXlUSU6JRWK=
human COLO-684 cell M1XGT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFzVcoFKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwM{Ggcm0> MWrTRW5ITVJ?
human T-24 cell NGDpPXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnm1TY5pcWKrdHnvckBw\iCqdX3hckBVNTJ2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuPFYhdk1? M3vofHNCVkeHUh?=
human AGS cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NI\1R4pKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P M4jzRnNCVkeHUh?=
human EW-13 cell Mon0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE\WUYdKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTRibl2= MmTpV2FPT0WU
human SW962 cell NGnSZphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4\VWmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU42QSCwTR?= MoO0V2FPT0WU
human EW-11 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWHJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOkBvVQ>? NIXYZVVUSU6JRWK=
human RXF393 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2LpeGlvcGmkaYTpc44hd2ZiaIXtZY4hWliIM{mzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPjZibl2= NH65enFUSU6JRWK=
human EoL-1-cell cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWHKZYRXUW6qaXLpeIlwdiCxZjDoeY1idiCHb1ytNU1k\WyuIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MU[uNUBvVQ>? NHzteZJUSU6JRWK=

... 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
  • 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 NSC 683864
Smiles COC1CC(CCC1OC(=O)C(C)(CO)CO)CC(C)C2CC(=O)C(C)\C=C(C)\C(O)C(OC)C(=O)C(C)CC(C)/C=C/C=C/C=C(C)/C(CC3CCC(C)C(O)(O3)C(=O)C(=O)N4CCCCC4C(=O)O2)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tech Support

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Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID