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
JPY 61420.00
JPY 144420.00

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 NELHVmhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{DJTmlvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyOyCwTR?= MWjTRW5ITVJ?
human L-363 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{DodWlvcGmkaYTpc44hd2ZiaIXtZY4hVC1|NkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1OiCwTR?= Mo\wV2FPT0WU
human Ramos-2G6-4C10 cell M1vVUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2rWWGlvcGmkaYTpc44hd2ZiaIXtZY4hWmGvb4OtNmc3NTSFMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM1OiCwTR?= M2SwTHNCVkeHUh?=
human SBC-1 cell NEXGPXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX:3[|cxUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDR2IH7N NVfrWlE1W0GQR1XS
human MHH-PREB-1 cell NEHtUVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYH3fW45UW6qaXLpeIlwdiCxZjDoeY1idiCPSFitVHJGSi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVUhdk1? MoXNV2FPT0WU
human LNCAP cells Ml7pVJJwdGmoZYLheIlwdiCjc4PhfS=> M4Dt[FMh\GG7cx?= NVfkdoFRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUCuOUBvVQ>? M4LBVlIyPDN6NUe5
human HH cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4LCeGlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[2OEBvVQ>? MoH2V2FPT0WU
human TYK-nu cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|c5KG6P Mmm4V2FPT0WU
human H4 cell NH3MPZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yNzDuUS=> MoXQV2FPT0WU
human K5 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF3FbZBKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zN{BvVQ>? MYXTRW5ITVJ?
human PA-1 cell NGnESoRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXezeo81UW6qaXLpeIlwdiCxZjDoeY1idiCSQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41PyCwTR?= MWXTRW5ITVJ?
human SK-NEP-1 cell Ml\jS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXTzW3hYUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OSXAuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEmgcm0> NHrvO4lUSU6JRWK=
human 697 cell MmjvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJFY6PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNzDuUS=> MUjTRW5ITVJ?
human CTB-1 cell NYrPRoFVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlnVTY5pcWKrdHnvckBw\iCqdX3hckBEXEJvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVMhdk1? MkfjV2FPT0WU
human DB cell M13tOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYm1bI5EUW6qaXLpeIlwdiCxZjDoeY1idiCGQjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVIhdk1? MYPTRW5ITVJ?
human MLMA cell M3vsdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzBSZZPUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OSCwTR?= MYDTRW5ITVJ?
human GAMG cell M3zqeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\S[2lvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPFIhdk1? MYLTRW5ITVJ?
human JVM-3 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnOyTY5pcWKrdHnvckBw\iCqdX3hckBLXk1vMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVUhdk1? NF[yPZZUSU6JRWK=
human LAMA-84 cell NEH6cYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{X4eWlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODNibl2= NVS0Vo1tW0GQR1XS
human RPMI-8226 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXH2SphwUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVgzOjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG1JI5O M{PCb3NCVkeHUh?=
human MOLT-4 cell MlXGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYrt[oJYUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjNzIH7N MVXTRW5ITVJ?
human CAMA-1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV:5do5RUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd5IH7N MmW3V2FPT0WU
human NCI-SNU-1 cell NFPpO4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGG0Z4VKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwOEGgcm0> M1Ph[3NCVkeHUh?=
human SW780 cell MkTMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{LlcGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{KG6P NEHmZldUSU6JRWK=
human H9 cell NW\GSGZST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC56ODDuUS=> NWHtT3pJW0GQR1XS
human BE-13 cell NXPKVpZ4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkjPTY5pcWKrdHnvckBw\iCqdX3hckBDTS1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVEhdk1? NX7qOIZjW0GQR1XS
human ES8 cell NULuXI1wT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGftUWFKdmirYnn0bY9vKG:oIHj1cYFvKEWVODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNlchdk1? NGL5[VRUSU6JRWK=
human DEL cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3f1OGlvcGmkaYTpc44hd2ZiaIXtZY4hTEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT60OkBvVQ>? MXrTRW5ITVJ?
human QIMR-WIL cell NX7TTlFLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFL3dZFKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS55MTDuUS=> M1\0cnNCVkeHUh?=
human CGTH-W-1 cell MkfQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4j6TGlvcGmkaYTpc44hd2ZiaIXtZY4hS0eWSD3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njd3IH7N M1jwdHNCVkeHUh?=
human CHL-1 cell NE[ySIRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? MonQV2FPT0WU
human A2780 cell NES1XIlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2fQNWlvcGmkaYTpc44hd2ZiaIXtZY4hSTJ5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg5KG6P M3ribXNCVkeHUh?=
human VA-ES-BJ cell Mk\YS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGTQTGlKdmirYnn0bY9vKG:oIHj1cYFvKF[DLVXTMWJLKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57IH7N MnHPV2FPT0WU
human BB65-RCC cell NV;UcZB{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoHiTY5pcWKrdHnvckBw\iCqdX3hckBDSjZ3LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVchdk1? NY\xSFFDW0GQR1XS
human D-566MG cell MnHsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEPNcpdKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjF4IH7N NGns[2ZUSU6JRWK=
human MDA468 cells NI[4S5pRem:uaX\ldoF1cW:wIHHzd4F6 MnjoN{Bl[Xm| MonPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFG0Olgh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD16IH7N NFfNSHMzOTR|OEW3PS=>
human HO-1-N-1 cell NXLrPHUyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUjCTotwUW6qaXLpeIlwdiCxZjDoeY1idiCKTz2xMW4uOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;OD6yJI5O MVnTRW5ITVJ?
human RS4-11 cell NVjaNGE1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXHJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuOFUhdk1? M1fidnNCVkeHUh?=
human PC-3 cell M3rY[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHBENTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17LkG0JI5O MmrSV2FPT0WU
human NB69 cell MkP3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWTSTWh4UW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PiCwTR?= NVjBUpJYW0GQR1XS
human HGC-27 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX3jVYNGUW6qaXLpeIlwdiCxZjDoeY1idiCKR1OtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZibl2= NI\1WWpUSU6JRWK=
human NCI-H720 cell NXnDOmRuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2DXVWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3NlAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjZ{IH7N NIXRWXJUSU6JRWK=
human NCI-H292 cell NHnOfGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4TTW2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N NWjhXndKW0GQR1XS
human A3-KAW cell MnjFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3[0cmlvcGmkaYTpc44hd2ZiaIXtZY4hSTNvS1HXJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvPDNibl2= MXnTRW5ITVJ?
human DU-4475 cell Mn7hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1zoOWlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjd|IH7N M3;CVXNCVkeHUh?=
human HuH-7 cell M4ixPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYXJcohq[mm2aX;uJI9nKGi3bXHuJGh2UC15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|Ihdk1? MWHTRW5ITVJ?
human J-RT3-T3-5 cell M1XzW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVjJcohq[mm2aX;uJI9nKGi3bXHuJGouWlR|LWSzMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi5|ODDuUS=> NFHRSZBUSU6JRWK=
human VM-CUB-1 cell NXzFVo5kT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIfTcZFKdmirYnn0bY9vKG:oIHj1cYFvKF[PLVPVRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkegcm0> MnryV2FPT0WU
human MOLT-16 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk45PCCwTR?= M3T5ZnNCVkeHUh?=
human KG-1 cell NHzrZ2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoTpTY5pcWKrdHnvckBw\iCqdX3hckBMTy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuPUBvVQ>? NWPUd24{W0GQR1XS
human P12-ICHIKAWA cell M2TqR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3nEeWlvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFEhdk1? MYHTRW5ITVJ?
human ACN cell M{[3R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWD1SHhTUW6qaXLpeIlwdiCxZjDoeY1idiCDQ16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOiCwTR?= NVLJ[HN3W0GQR1XS
human COLO-684 cell NV7hWodVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWO3UmJOUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY5PCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkOxJI5O NF3M[YZUSU6JRWK=
human T-24 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVnJcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz64OkBvVQ>? Ml3zV2FPT0WU
human AGS cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NInucphKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P MXfTRW5ITVJ?
human EW-13 cell NU\yNnFvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYq4R3I1UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjV2IH7N MVrTRW5ITVJ?
human SW962 cell M4CzS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\mTGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU42QSCwTR?= MlXtV2FPT0WU
human EW-11 cell NIq0dYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIXJSnVKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPiCwTR?= NWC1NlM3W0GQR1XS
human RXF393 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NULiNJFOUW6qaXLpeIlwdiCxZjDoeY1idiCUWF[zPVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS54NjDuUS=> MkPaV2FPT0WU
human EoL-1-cell cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXTJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi5zIH7N NEDafHRUSU6JRWK=

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
NCT01010126 Completed Adult Hepatocellular Carcinoma|Advanced Adult Hepatocellular Carcinoma|Endometrial Serous Adenocarcinoma|Localized Non-Resectable Adult Liver Carcinoma|Lung Carcinoid Tumor|Malignant Pancreatic Gastrinoma|Malignant Pancreatic Glucagonoma|Malignant Pancreatic Insulinoma|Malignant Pancreatic Somatostatinoma|Metastatic Digestive System Neuroendocrine Tumor G1|Ovarian Carcinosarcoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Surface Papillary Adenocarcinoma|Pancreatic Alpha Cell Adenoma|Pancreatic Beta Cell Adenoma|Pancreatic Delta Cell Adenoma|Pancreatic G-Cell Adenoma|Pancreatic Polypeptide Tumor|Recurrent Adult Liver Carcinoma|Recurrent Digestive System Neuroendocrine Tumor G1|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Pancreatic Neuroendocrine Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma|Regional Digestive System Neuroendocrine Tumor G1|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Primary Peritoneal Cancer|Stage IIIA Uterine Corpus Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Primary Peritoneal Cancer|Stage IIIB Uterine Corpus Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Cancer|Stage IIIC Primary Peritoneal Cancer|Stage IIIC Uterine Corpus Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer|Stage IVA Uterine Corpus Cancer|Stage IVB Uterine Corpus Cancer|Uterine Carcinosarcoma National Cancer Institute (NCI) September 8 2009 Phase 2
NCT00703625 Completed Resistant Solid Malignancies Washington University School of Medicine March 8 2008 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
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
NCT02389309 Recruiting Solid Tumors M.D. Anderson Cancer Center October 5 2015 Phase 1
NCT01687673 Active not recruiting Hepatocellular Carcinoma University of California San Francisco|Robert H. Lurie Cancer Center|Pfizer October 5 2012 Phase 2

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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。

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