Temsirolimus (CCI-779, NSC 683864)

Licensed by Pfizer 製品コードS1044

Temsirolimus (CCI-779, NSC 683864)化学構造

分子量(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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JPY 22244.00
JPY 19422.00
JPY 41002.00
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カスタマーフィードバック(4)

  • 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.

製品安全説明書

mTOR阻害剤の選択性比較

生物活性

製品説明 Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay.
ターゲット
mTOR [1]
(Cell-free assay)
1.76 μM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HSC-4 cell MkLqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGhUSy12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVMhdk1? NYrmV|ZsW0GQR1XS
human L-363 cell NF;tU4xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3LKUWlvcGmkaYTpc44hd2ZiaIXtZY4hVC1|NkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1OiCwTR?= NV7abFE4W0GQR1XS
human Ramos-2G6-4C10 cell M1nU[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1O5[GlvcGmkaYTpc44hd2ZiaIXtZY4hWmGvb4OtNmc3NTSFMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM1OiCwTR?= MkHUV2FPT0WU
human SBC-1 cell M1z1dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFjDOWJKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41PDRibl2= MmW1V2FPT0WU
human MHH-PREB-1 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXTWc|VlUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitVHJGSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVUhdk1? M3HLenNCVkeHUh?=
human LNCAP cells MmfYVJJwdGmoZYLheIlwdiCjc4PhfS=> M1PYfVMh\GG7cx?= NIC3S4hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;MD61JI5O MVuyNVQ{QDV5OR?=
human HH cell NEjTRoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGhJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54NkSgcm0> NETydHpUSU6JRWK=
human TYK-nu cell M2HEWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYPMU|BlUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd5ODDuUS=> MVnTRW5ITVJ?
human H4 cell M3nBcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlXkTY5pcWKrdHnvckBw\iCqdX3hckBJPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMEegcm0> M4PBU3NCVkeHUh?=
human K5 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|MzDuUS=> Ml;IV2FPT0WU
human PA-1 cell MkjzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVnQWnk6UW6qaXLpeIlwdiCxZjDoeY1idiCSQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41PyCwTR?= MoD0V2FPT0WU
human SK-NEP-1 cell NGT4ZmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXvJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU6HUD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41QSCwTR?= NIXFfY5USU6JRWK=
human 697 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXTXPZpGUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlchdk1? MkPMV2FPT0WU
human CTB-1 cell NVrtZlZnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX3ONYpIUW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTNibl2= NGD2dWFUSU6JRWK=
human DB cell M4qwdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH3sVGpKdmirYnn0bY9vKG:oIHj1cYFvKESEIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6xNkBvVQ>? MmPaV2FPT0WU
human MLMA cell NEHUTGVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX[yXJZPUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= NI\RdFZUSU6JRWK=
human GAMG cell NEfublZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkfkTY5pcWKrdHnvckBw\iCqdX3hckBISU2JIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz64NkBvVQ>? M13EfXNCVkeHUh?=
human JVM-3 cell NVvaXIk{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXvJcohq[mm2aX;uJI9nKGi3bXHuJGpXVS1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OUBvVQ>? MlrtV2FPT0WU
human LAMA-84 cell NHzPW21Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2DkbmlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODNibl2= M1zQ[nNCVkeHUh?=
human RPMI-8226 cell NWD3eIdmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUizWpB[UW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O NEDIUYhUSU6JRWK=
human MOLT-4 cell NIm2OXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVfpO2JxUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjNzIH7N NIC2ZmZUSU6JRWK=
human CAMA-1 cell NFjYUHFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3HzTWlvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44PyCwTR?= MYnTRW5ITVJ?
human NCI-SNU-1 cell M1G4Vmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnrFTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjhzIH7N NHvVfJRUSU6JRWK=
human SW780 cell Mm[4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVG4Rll4UW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDNibl2= NX\IdnRwW0GQR1XS
human H9 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYDwe5ZXUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFghdk1? NHyxfJBUSU6JRWK=
human BE-13 cell NF7kbYxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUjaR4x5UW6qaXLpeIlwdiCxZjDoeY1idiCERT2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTFibl2= NE[1NHlUSU6JRWK=
human ES8 cell M3TJbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXS0fItbUW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlI4KG6P MUfTRW5ITVJ?
human DEL cell NXfWN49PT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJGRGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNE[gcm0> MkT2V2FPT0WU
human QIMR-WIL cell MkC0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnnNTY5pcWKrdHnvckBw\iCqdX3hckBSUU2ULWfJUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzFibl2= NVrDflI{W0GQR1XS
human CGTH-W-1 cell Mln2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXWwTFVQUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Wgcm0> Mor6V2FPT0WU
human CHL-1 cell Ml[5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? MULTRW5ITVJ?
human A2780 cell MnfzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVzEXpRXUW6qaXLpeIlwdiCxZjDoeY1idiCDMke4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDhibl2= MWnTRW5ITVJ?
human VA-ES-BJ cell NIC5cZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;1VWlvcGmkaYTpc44hd2ZiaIXtZY4hXkFvRWOtRmoh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njlibl2= M37mOnNCVkeHUh?=
human BB65-RCC cell MkDuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWnPSW44UW6qaXLpeIlwdiCxZjDoeY1idiCEQk[1MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdibl2= M1ntfHNCVkeHUh?=
human D-566MG cell M3\WUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1HEW2lvcGmkaYTpc44hd2ZiaIXtZY4hTC13Nk\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOTZibl2= M{nwVXNCVkeHUh?=
human MDA468 cells MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 Ml;zN{Bl[Xm| NIDHW4xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERVQ3QCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUigcm0> M1PVblIyPDN6NUe5
human HO-1-N-1 cell NIjY[5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkHwTY5pcWKrdHnvckBw\iCqdX3hckBJVy1zLV6tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:QC5{IH7N MmjaV2FPT0WU
human RS4-11 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEKwfndKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvPDVibl2= NHvuVo9USU6JRWK=
human PC-3 cell NYPtfVU3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHBENTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkG0JI5O M{CyRXNCVkeHUh?=
human NB69 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXrJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkS2JI5O MnHnV2FPT0WU
human HGC-27 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnfWTY5pcWKrdHnvckBw\iCqdX3hckBJT0NvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlYhdk1? NYrESI9SW0GQR1XS
human NCI-H720 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYjyeVIyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFczOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwNkKgcm0> NEHpT5hUSU6JRWK=
human NCI-H292 cell NH2xd|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MonRTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvQDRibl2= NHW4dXBUSU6JRWK=
human A3-KAW cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKGi3bXHuJGE{NUuDVzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlQ{KG6P MVTTRW5ITVJ?
human DU-4475 cell NYPxb4Y4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUf0PIpKUW6qaXLpeIlwdiCxZjDoeY1idiCGVT20OFc2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwN{Ogcm0> MlXTV2FPT0WU
human HuH-7 cell NHOxRWpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXlepFKdmirYnn0bY9vKG:oIHj1cYFvKEi3SD23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvOzJibl2= M1jEd3NCVkeHUh?=
human J-RT3-T3-5 cell NX;JfJpIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTCbolqUW6qaXLpeIlwdiCxZjDoeY1idiCMLWLUN{1VOy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|ghdk1? M{O4bXNCVkeHUh?=
human VM-CUB-1 cell MmjkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJHZONUOXQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvPjdibl2= NIfD[3pUSU6JRWK=
human MOLT-16 cell NInkW5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXjpRpByUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwOESgcm0> MmDTV2FPT0WU
human KG-1 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYjWU5FkUW6qaXLpeIlwdiCxZjDoeY1idiCNRz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvQSCwTR?= M1\nSXNCVkeHUh?=
human P12-ICHIKAWA cell NEPN[lVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHHmTpdKdmirYnn0bY9vKG:oIHj1cYFvKFBzMj3JR2hKU0GZQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlAyKG6P NI\vc5RUSU6JRWK=
human ACN cell MkjpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NInNRpFKdmirYnn0bY9vKG:oIHj1cYFvKEGFTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlAzKG6P MU\TRW5ITVJ?
human COLO-684 cell M4\lbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNki0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvOzFibl2= MUnTRW5ITVJ?
human T-24 cell M1jSXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4Lv[2lvcGmkaYTpc44hd2ZiaIXtZY4hXC1{NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlg3KG6P NEPUdnlUSU6JRWK=
human AGS cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHLhdJpKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P MXnTRW5ITVJ?
human EW-13 cell NYj1bJM6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuOVQhdk1? M3\xSnNCVkeHUh?=
human SW962 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnjzTY5pcWKrdHnvckBw\iCqdX3hckBUXzl4MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlU6KG6P NEnpV|dUSU6JRWK=
human EW-11 cell MmfmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlTqTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlYhdk1? MlWzV2FPT0WU
human RXF393 cell NF6yWWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVTJcohq[mm2aX;uJI9nKGi3bXHuJHJZTjN7MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlY3KG6P MUDTRW5ITVJ?
human EoL-1-cell cell NFjRR|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi5zIH7N NHSyV|hUSU6JRWK=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[1]

+ 展開
  • 細胞株: A549, H157, H460, H446, HCT116, HT29, SW480, DLD1, Caco2, LNCap, DU145, MDA468, MDA231, HEK293, and PC3-MM2
  • 濃度: Dissolved in DMSO, final concentrations ~20 μM
  • 反応時間: 72 hours
  • 実験の流れ:

    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.


    (参考用のみ)
動物試験:

[4]

+ 展開
  • 動物モデル: Female athymic nude mice injected s.c. with DAOY, or U251 cells
  • 製剤: Prepared in 100% EtOH as a 50 mg/mL stock solution, and diluted in 5% Tween 80 and 5% polyethylene glycol 400
  • 投薬量: 20 mg/kg
  • 投与方法: Injection daily 5 times per week
    (参考用のみ)

溶解度 (25°C)

体外 Ethanol 75 mg/mL (72.79 mM)
DMSO 67 mg/mL (65.03 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300 +2% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
7mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 1030.29
化学式

C56H87NO16

CAS No. 162635-04-3
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

mTORシグナル伝達経路

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