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.

サイズ 価格(税別)  
In DMSO JPY 24200
JPY 21400
JPY 43000
JPY 63400
JPY 146400
最寄りの販売代理店を探す

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください:[email protected]

バルク問合せ

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 NUjyS3VpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGhUSy12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVMhdk1? NED2UHVUSU6JRWK=
human L-363 cell M{XQcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3X0bGlvcGmkaYTpc44hd2ZiaIXtZY4hVC1|NkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1OiCwTR?= MUTTRW5ITVJ?
human Ramos-2G6-4C10 cell NF\jOJBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlK0TY5pcWKrdHnvckBw\iCqdX3hckBT[W2xcz2yS|YuPENzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|QzKG6P NF7yNHNUSU6JRWK=
human SBC-1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1TsNWlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ1PCCwTR?= MojqV2FPT0WU
human MHH-PREB-1 cell MlPOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGH3ZZhKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3QVmVDNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5OUBvVQ>? MX7TRW5ITVJ?
human LNCAP cells NFexcWxRem:uaX\ldoF1cW:wIHHzd4F6 MVWzJIRigXN? M1fDSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD1yLkWgcm0> NX7QWWVUOjF2M{i1O|k>
human HH cell NUmwZZBXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoGzTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNk[0JI5O NXnQZXVnW0GQR1XS
human TYK-nu cell M4n0PWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml7ETY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlc4QCCwTR?= M2S5eXNCVkeHUh?=
human H4 cell NFzG[29Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yNzDuUS=> MVjTRW5ITVJ?
human K5 cell MnTxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{WyS2lvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOzJI5O MV;TRW5ITVJ?
human PA-1 cell M{LPPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\MTY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? MX\TRW5ITVJ?
human SK-NEP-1 cell M2jWb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGnxZYZKdmirYnn0bY9vKG:oIHj1cYFvKFONLV7FVE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52OTDuUS=> MnW2V2FPT0WU
human 697 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGL1OoZKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO{BvVQ>? NVy5PHd5W0GQR1XS
human CTB-1 cell NYKzcGU6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXzJcohq[mm2aX;uJI9nKGi3bXHuJGNVSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65N{BvVQ>? NX:wT4g6W0GQR1XS
human DB cell MnfHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnHqTY5pcWKrdHnvckBw\iCqdX3hckBFSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwMUKgcm0> MVPTRW5ITVJ?
human MLMA cell M4G0N2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFK4b3lKdmirYnn0bY9vKG:oIHj1cYFvKE2OTVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlMyKG6P NEfzVXRUSU6JRWK=
human GAMG cell M{PDUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGdCVUdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkiyJI5O MUjTRW5ITVJ?
human JVM-3 cell NWPTclZoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX;EXHc4UW6qaXLpeIlwdiCxZjDoeY1idiCMVl2tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTVibl2= MWPTRW5ITVJ?
human LAMA-84 cell NWLtSIRET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3vDNmlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODNibl2= MWjTRW5ITVJ?
human RPMI-8226 cell NITUd3ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXPHbXlHUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O MWjTRW5ITVJ?
human MOLT-4 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnqTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlMyKG6P NELWTG9USU6JRWK=
human CAMA-1 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{LMO2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GPQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44PyCwTR?= M4nLNnNCVkeHUh?=
human NCI-SNU-1 cell M37jXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3T0TGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLWPOWU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56MTDuUS=> NYrYRYZ3W0GQR1XS
human SW780 cell MmL3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkP5TY5pcWKrdHnvckBw\iCqdX3hckBUXzd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFMhdk1? MXjTRW5ITVJ?
human H9 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56ODDuUS=> MXzTRW5ITVJ?
human BE-13 cell M{\XR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUDycZFlUW6qaXLpeIlwdiCxZjDoeY1idiCERT2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTFibl2= NWToPGlGW0GQR1XS
human ES8 cell NVn4d3l6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NULtZo5vUW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlI4KG6P MUPTRW5ITVJ?
human DEL cell NWDQR2JkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWnPNHlMUW6qaXLpeIlwdiCxZjDoeY1idiCGRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ3KG6P Ml[5V2FPT0WU
human QIMR-WIL cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH7vW5VKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS55MTDuUS=> NFj0dIxUSU6JRWK=
human CGTH-W-1 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUjTfHc6UW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Wgcm0> NYXuSGRxW0GQR1XS
human CHL-1 cell M3uyS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYjhVYVWUW6qaXLpeIlwdiCxZjDoeY1idiCFSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDZibl2= NVXzOoFUW0GQR1XS
human A2780 cell NXr1b4s3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGEzPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64PEBvVQ>? M1jGVXNCVkeHUh?=
human VA-ES-BJ cell NXfSOJVHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1[4WmlvcGmkaYTpc44hd2ZiaIXtZY4hXkFvRWOtRmoh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njlibl2= M3LC[nNCVkeHUh?=
human BB65-RCC cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVztWpBuUW6qaXLpeIlwdiCxZjDoeY1idiCEQk[1MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdibl2= NYnKXmtyW0GQR1XS
human D-566MG cell NE\UWlRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEnKeolKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjF4IH7N MY\TRW5ITVJ?
human MDA468 cells M17odHBzd2yrZnXyZZRqd25iYYPzZZk> NIfJbYY{KGSjeYO= M3n1TmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBOFY5KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;ODDuUS=> NVnKO49lOjF2M{i1O|k>
human HO-1-N-1 cell NEHxdFhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUHrR3ZXUW6qaXLpeIlwdiCxZjDoeY1idiCKTz2xMW4uOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;OD6yJI5O Mnf1V2FPT0WU
human RS4-11 cell NGLXVnZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXHJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOFUhdk1? MnjEV2FPT0WU
human PC-3 cell NYT4eFhzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\afGlvcGmkaYTpc44hd2ZiaIXtZY4hWENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuNVQhdk1? MUjTRW5ITVJ?
human NB69 cell NVroeoU4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH:5d3FKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ3KG6P NIHISpZUSU6JRWK=
human HGC-27 cell NWLW[WJ2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnPDTY5pcWKrdHnvckBw\iCqdX3hckBJT0NvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlYhdk1? MWfTRW5ITVJ?
human NCI-H720 cell MkDuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF\tdYRKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|IxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS54MjDuUS=> MnTsV2FPT0WU
human NCI-H292 cell NUHp[JdtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3;xbmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N NGXHbIlUSU6JRWK=
human A3-KAW cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NULoOplWUW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC52MzDuUS=> NVfhdGFnW0GQR1XS
human DU-4475 cell MmHOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnLaTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPzNibl2= NFv2SVlUSU6JRWK=
human HuH-7 cell NIrXPJNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJGh2UC15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|Ihdk1? NELTbG1USU6JRWK=
human J-RT3-T3-5 cell NYDMeoRIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGouWlR|LWSzMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|ODDuUS=> MVzTRW5ITVJ?
human VM-CUB-1 cell M17wUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWLwT3dTUW6qaXLpeIlwdiCxZjDoeY1idiCYTT3DWWIuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lk[3JI5O MWXTRW5ITVJ?
human MOLT-16 cell NWfNcopqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NITVRppKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi56NDDuUS=> MmGyV2FPT0WU
human KG-1 cell NFS0bWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnnkTY5pcWKrdHnvckBw\iCqdX3hckBMTy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuPUBvVQ>? M176TnNCVkeHUh?=
human P12-ICHIKAWA cell NWnhemhET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MW\Jcohq[mm2aX;uJI9nKGi3bXHuJHAyOi2LQ1jJT2FYSSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCxJI5O NEfISXNUSU6JRWK=
human ACN cell NYrqR2lGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIDPR|hKdmirYnn0bY9vKG:oIHj1cYFvKEGFTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlAzKG6P MoLvV2FPT0WU
human COLO-684 cell NITjSWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnuyTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjNzIH7N NUXDTVVGW0GQR1XS
human T-24 cell MlLFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1vDeGlvcGmkaYTpc44hd2ZiaIXtZY4hXC1{NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlg3KG6P MUTTRW5ITVJ?
human AGS cell M{jJXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFfpNJhKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P M3;NbXNCVkeHUh?=
human EW-13 cell NITmbHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWmzVJBtUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV2IH7N NHS4Wo1USU6JRWK=
human SW962 cell NYHyZZdOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXBXVdYUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjV7IH7N MlLwV2FPT0WU
human EW-11 cell NGe5cWZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUPJemtGUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZibl2= NVrqOJZtW0GQR1XS
human RXF393 cell MlSxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkXFTY5pcWKrdHnvckBw\iCqdX3hckBTYEZ|OUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU43PiCwTR?= NEn4SWVUSU6JRWK=
human EoL-1-cell cell M2W1VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHXJOJVKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNj6xJI5O MX;TRW5ITVJ?

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. 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

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

mTOR Inhibitors with Unique Features

相関mTOR製品

Tags: Temsirolimus (CCI-779, NSC 683864)を買う | Temsirolimus (CCI-779, NSC 683864) ic50 | Temsirolimus (CCI-779, NSC 683864)供給者 | Temsirolimus (CCI-779, NSC 683864)を購入する | Temsirolimus (CCI-779, NSC 683864)費用 | Temsirolimus (CCI-779, NSC 683864)生産者 | オーダーTemsirolimus (CCI-779, NSC 683864) | Temsirolimus (CCI-779, NSC 683864)化学構造 | Temsirolimus (CCI-779, NSC 683864)分子量 | Temsirolimus (CCI-779, NSC 683864)代理店
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID