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)は一種の特定なmTOR阻害剤で、無細胞試験でIC50値は1.76 μMです。

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JPY 22244.00 あり
JPY 19422.00 あり
JPY 41002.00 あり
JPY 61420.00 あり
JPY 144420.00 あり

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)は一種の特定なmTOR阻害剤で、無細胞試験でIC50値は1.76 μMです。
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 NWftXnlST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXu0UWNQUW6qaXLpeIlwdiCxZjDoeY1idiCKU1OtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTF|IH7N MX;TRW5ITVJ?
human L-363 cell NYXzeYtUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXXJcohq[mm2aX;uJI9nKGi3bXHuJGwuOzZ|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yOFIhdk1? MU\TRW5ITVJ?
human Ramos-2G6-4C10 cell M1;ye2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NW[1NXVSUW6qaXLpeIlwdiCxZjDoeY1idiCUYX3vd{0zTzZvNFOxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzR{IH7N NFXpe3FUSU6JRWK=
human SBC-1 cell M{PG[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVrJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60OFQhdk1? M1Oye3NCVkeHUh?=
human MHH-PREB-1 cell NUH1e|VZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEfacFdKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3QVmVDNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5OUBvVQ>? M{HnOXNCVkeHUh?=
human LNCAP cells Mnu1VJJwdGmoZYLheIlwdiCjc4PhfS=> NH3Ie48{KGSjeYO= NX\0ZYk{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUCuOUBvVQ>? MVGyNVQ{QDV5OR?=
human HH cell Mn;FS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnXWTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNk[0JI5O NITjdoVUSU6JRWK=
human TYK-nu cell Mo\oS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYHM[WJ2UW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd5ODDuUS=> NYOybmVmW0GQR1XS
human H4 cell M1X2bGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFTnfoJKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wO{BvVQ>? M1nIPHNCVkeHUh?=
human K5 cell MmTMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|MzDuUS=> NGrsTmRUSU6JRWK=
human PA-1 cell NUDR[4M5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXrz[I96UW6qaXLpeIlwdiCxZjDoeY1idiCSQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41PyCwTR?= NUL2VHBIW0GQR1XS
human SK-NEP-1 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHNPVRwUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OSXAuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEmgcm0> M3XaWXNCVkeHUh?=
human 697 cell M2rhNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXvJcohq[mm2aX;uJI9nKGi3bXHuJFY6PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNzDuUS=> MlLhV2FPT0WU
human CTB-1 cell NVPab4ZST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWe5cHJ2UW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTNibl2= MkD2V2FPT0WU
human DB cell NFTYe2ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGRDKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5zMjDuUS=> NFvDWFFUSU6JRWK=
human MLMA cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYPNeWhJUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= NWfhWZM6W0GQR1XS
human GAMG cell NHL5[HZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVWwVo5ZUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OiCwTR?= NXKzXVJyW0GQR1XS
human JVM-3 cell NWH1dIFlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYPJcohq[mm2aX;uJI9nKGi3bXHuJGpXVS1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OUBvVQ>? MUPTRW5ITVJ?
human LAMA-84 cell M2\yZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3ub5NwUW6qaXLpeIlwdiCxZjDoeY1idiCOQV3BMVg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yMzDuUS=> MmK0V2FPT0WU
human RPMI-8226 cell MoPLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHHHVmdKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtPFIzPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMUWgcm0> MnKxV2FPT0WU
human MOLT-4 cell NV\2e5QxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3PaXmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{OSCwTR?= NYGzUI1QW0GQR1XS
human CAMA-1 cell NVH6RZRTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHfsZ|hKdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzdibl2= Mln6V2FPT0WU
human NCI-SNU-1 cell Mo\tS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnrvTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjhzIH7N M1q0[nNCVkeHUh?=
human SW780 cell MlfvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGrG[IZKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45OyCwTR?= MWrTRW5ITVJ?
human H9 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXXlbnYyUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFghdk1? NEDrUY1USU6JRWK=
human BE-13 cell MkDMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF7GSXdKdmirYnn0bY9vKG:oIHj1cYFvKEKHLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46OSCwTR?= MX;TRW5ITVJ?
human ES8 cell MkDHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVHJcohq[mm2aX;uJI9nKGi3bXHuJGVUQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwMkegcm0> NWTWNHJKW0GQR1XS
human DEL cell M4fBdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{P6NWlvcGmkaYTpc44hd2ZiaIXtZY4hTEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT60OkBvVQ>? M3HEcXNCVkeHUh?=
human QIMR-WIL cell NX3ZUYlWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXT2OmdSUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Ggcm0> MX;TRW5ITVJ?
human CGTH-W-1 cell NFq2bGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXvJcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44PSCwTR?= MWjTRW5ITVJ?
human CHL-1 cell NUXQN2x1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXHJcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? MYrTRW5ITVJ?
human A2780 cell NYrWUZlIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rXOWlvcGmkaYTpc44hd2ZiaIXtZY4hSTJ5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg5KG6P MmXEV2FPT0WU
human VA-ES-BJ cell NYT3[JplT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUfxdYd5UW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOTDuUS=> NVj1R3c{W0GQR1XS
human BB65-RCC cell NUDRSWlET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NITW[JVKdmirYnn0bY9vKG:oIHj1cYFvKEKENkWtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PyCwTR?= M2LwN3NCVkeHUh?=
human D-566MG cell NXTTWnF3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnfrTY5pcWKrdHnvckBw\iCqdX3hckBFNTV4Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{4yPiCwTR?= MkP6V2FPT0WU
human MDA468 cells NXPZW4VkWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUn6fIJwOyCmYYnz M1XqZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBOFY5KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;ODDuUS=> MnjaNlE1Ozh3N{m=
human HO-1-N-1 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF3hd4xKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> NE\hXlJUSU6JRWK=
human RS4-11 cell NUfDUmk5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4O1OGlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE41PSCwTR?= MXrTRW5ITVJ?
human PC-3 cell MlHTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWLJcohq[mm2aX;uJI9nKGi3bXHuJHBENTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkG0JI5O NVS4W45qW0GQR1XS
human NB69 cell NHrYXGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH23[3hKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ3KG6P MYnTRW5ITVJ?
human HGC-27 cell NUXaN4R{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXTXfmg1UW6qaXLpeIlwdiCxZjDoeY1idiCKR1OtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZibl2= NUS0eFVJW0GQR1XS
human NCI-H720 cell NH72[VJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M121S2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3NlAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZ{IH7N NUfJWppGW0GQR1XS
human NCI-H292 cell NV7VZZdHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVLkXWw1UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTlwOESgcm0> MnzsV2FPT0WU
human A3-KAW cell NXfsbHhnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVvHbnRvUW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC52MzDuUS=> MVTTRW5ITVJ?
human DU-4475 cell Moj2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NELRfmlKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS55MzDuUS=> M{jwSnNCVkeHUh?=
human HuH-7 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NY\JVmRzUW6qaXLpeIlwdiCxZjDoeY1idiCKdVitO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjN{IH7N NUe4ZY5YW0GQR1XS
human J-RT3-T3-5 cell M1nJZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGouWlR|LWSzMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|ODDuUS=> MkPUV2FPT0WU
human VM-CUB-1 cell NYX4fWdYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXrJcohq[mm2aX;uJI9nKGi3bXHuJHZONUOXQj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvPjdibl2= MW\TRW5ITVJ?
human MOLT-16 cell NHroWXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XBbWlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjh2IH7N MYTTRW5ITVJ?
human KG-1 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEn3VFJKdmirYnn0bY9vKG:oIHj1cYFvKEuJLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk46KG6P M1TzUHNCVkeHUh?=
human P12-ICHIKAWA cell MmL6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWqx[JZ1UW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOSCwTR?= M1PxbHNCVkeHUh?=
human ACN cell Mlq5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWf4UZFLUW6qaXLpeIlwdiCxZjDoeY1idiCDQ16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOiCwTR?= MnW2V2FPT0WU
human COLO-684 cell NUeyZmw6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoLRTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjNzIH7N MY\TRW5ITVJ?
human T-24 cell NXvPdZlzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYXJcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz64OkBvVQ>? Mn30V2FPT0WU
human AGS cell M1HrO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX60bXNzUW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE4yOSCwTR?= NWL5WGwyW0GQR1XS
human EW-13 cell Mmm4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV7mbW1VUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV2IH7N M3z4e3NCVkeHUh?=
human SW962 cell MkXVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG\VT3ZKdmirYnn0bY9vKG:oIHj1cYFvKFOZOU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPTlibl2= NUjMRoZtW0GQR1XS
human EW-11 cell NEjoSGxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1jUO2lvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU43KG6P MVvTRW5ITVJ?
human RXF393 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUXCd3dRUW6qaXLpeIlwdiCxZjDoeY1idiCUWF[zPVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS54NjDuUS=> NF;NSWpUSU6JRWK=
human EoL-1-cell cell NWDofWdjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mo\DTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTZwMTDuUS=> MmrWV2FPT0WU

多くの細胞株試験データを見る場合、クリックしてください

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 順序で溶剤を入れること:
2% DMSO+30% PEG 300 +2% Tween 80+ddH2O
7mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01182883 Withdrawn Brain Stem Neoplasms|Glioma|Pinealoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 28, 2010 Phase 1
NCT02908035 Not yet recruiting Chronic Limb Ischemia Mercator MedSystems, Inc. January 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 2016 Phase 3
NCT02693535 Recruiting Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer March 2016 Phase 2
NCT02560012 Recruiting Carcinoma, Renal Cell The University of Texas Health Science Center, Houston December 2015 Phase 2
NCT02420613 Recruiting Diffuse Intrinsic Pontine Glioma M.D. Anderson Cancer Center October 2015 Phase 1

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

mTOR信号経路図

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