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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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 MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXXTY5pcWKrdHnvckBw\iCqdX3hckBJW0NvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE{KG6P MmrLV2FPT0WU
human L-363 cell NWfHV2ZDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2XmUmlvcGmkaYTpc44hd2ZiaIXtZY4hVC1|NkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI1OiCwTR?= MkPsV2FPT0WU
human Ramos-2G6-4C10 cell NXq3PXFWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJHJidW:|LULHOk01SzFyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zOFIhdk1? NHLve3lUSU6JRWK=
human SBC-1 cell M37oZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkLrTY5pcWKrdHnvckBw\iCqdX3hckBUSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFQ1KG6P NHzyUGFUSU6JRWK=
human MHH-PREB-1 cell NGrrdFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmDGTY5pcWKrdHnvckBw\iCqdX3hckBOUEhvUGLFRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OUWgcm0> NIfMO2JUSU6JRWK=
human LNCAP cells M3ixSHBzd2yrZnXyZZRqd25iYYPzZZk> NYPGe4ZLOyCmYYnz MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGOgZZN{[XluIFnDOVA:OC53IH7N M1;hR|IyPDN6NUe5
human HH cell Ml;jS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLu[mFEUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlY1KG6P Mmj3V2FPT0WU
human TYK-nu cell NX7BeJVXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rRcmlvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44Pzhibl2= MlPqV2FPT0WU
human H4 cell NEfUWopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWTJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yNzDuUS=> NGLKNFBUSU6JRWK=
human K5 cell MmHWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUe0c5hUUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Mhdk1? MmnBV2FPT0WU
human PA-1 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4XGSGlvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOFchdk1? M1nSWnNCVkeHUh?=
human SK-NEP-1 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYrKW4w5UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OSXAuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEmgcm0> NFnrV2pUSU6JRWK=
human 697 cell NWCzU4pqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUP3PYVkUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlchdk1? NULZTGhPW0GQR1XS
human CTB-1 cell MkW3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYfsRpVEUW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTNibl2= M2\zenNCVkeHUh?=
human DB cell MmTNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmixTY5pcWKrdHnvckBw\iCqdX3hckBFSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwMUKgcm0> MYHTRW5ITVJ?
human MLMA cell M2WxWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH7x[WNKdmirYnn0bY9vKG:oIHj1cYFvKE2OTVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlMyKG6P MUTTRW5ITVJ?
human GAMG cell M4Pwfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnoXmNQUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OiCwTR?= M1Hm[XNCVkeHUh?=
human JVM-3 cell Ml23S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{\OUWlvcGmkaYTpc44hd2ZiaIXtZY4hUl[PLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2KG6P M1TLNnNCVkeHUh?=
human LAMA-84 cell Mlr4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnrtTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xOyCwTR?= NEnOPFdUSU6JRWK=
human RPMI-8226 cell MoPqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGi5TnpKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtPFIzPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMUWgcm0> Mn7kV2FPT0WU
human MOLT-4 cell MnPZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;2TY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlMyKG6P NXW5bI5JW0GQR1XS
human CAMA-1 cell NWXibXRlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFvCSI5KdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzdibl2= Mo[wV2FPT0WU
human NCI-SNU-1 cell NX3POGh2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnHGTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjhzIH7N NFexbG1USU6JRWK=
human SW780 cell NXy1Z5NmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGnXbZJKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45OyCwTR?= NXTkeVdwW0GQR1XS
human H9 cell Mn3nS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXvhZZFKUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFghdk1? MUHTRW5ITVJ?
human BE-13 cell NXPGZoU3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND65NUBvVQ>? MXzTRW5ITVJ?
human ES8 cell M2rJOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlG1TY5pcWKrdHnvckBw\iCqdX3hckBGWzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkK3JI5O M4XYW3NCVkeHUh?=
human DEL cell MlXQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn3FTY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O MV3TRW5ITVJ?
human QIMR-WIL cell NXvjS5RzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NULHPXUxUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{Ggcm0> MnT2V2FPT0WU
human CGTH-W-1 cell Mk\KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn\ETY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzVibl2= MULTRW5ITVJ?
human CHL-1 cell NHfUe|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGNJVC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT64OkBvVQ>? MnHCV2FPT0WU
human A2780 cell MkLtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIrMTnJKdmirYnn0bY9vKG:oIHj1cYFvKEF{N{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU45QCCwTR?= M4jQNnNCVkeHUh?=
human VA-ES-BJ cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGPsfJRKdmirYnn0bY9vKG:oIHj1cYFvKF[DLVXTMWJLKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57IH7N NIKzUY9USU6JRWK=
human BB65-RCC cell NEHnW5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEi0eGdKdmirYnn0bY9vKG:oIHj1cYFvKEKENkWtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PyCwTR?= MY\TRW5ITVJ?
human D-566MG cell NVr0c|NxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGQuPTZ4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23MlE3KG6P MX3TRW5ITVJ?
human MDA468 cells NXrYWnNDWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1fYclMh\GG7cx?= Moj2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFG0Olgh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UV{Bie3OjeTygTWM2OD16IH7N MUOyNVQ{QDV5OR?=
human HO-1-N-1 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF\YfXdKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD16LkKgcm0> Moj2V2FPT0WU
human RS4-11 cell NYnu[3U6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTNfopKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvPDVibl2= NVmxSnJEW0GQR1XS
human PC-3 cell M1Lh[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXrKRpY2UW6qaXLpeIlwdiCxZjDoeY1idiCSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU4yPCCwTR?= Mkf0V2FPT0WU
human NB69 cell M3\qV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jEXGlvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOFYhdk1? Mn\SV2FPT0WU
human HGC-27 cell M3ezb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYLJcohq[mm2aX;uJI9nKGi3bXHuJGhISy1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOkBvVQ>? MnzoV2FPT0WU
human NCI-H720 cell M2TOemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlnnTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEeyNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPjJibl2= MofjV2FPT0WU
human NCI-H292 cell NWjPU4JsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NI[xblBKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS56NDDuUS=> NHHEe|BUSU6JRWK=
human A3-KAW cell NWDJVWJKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGE{NUuDVzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlQ{KG6P MnHWV2FPT0WU
human DU-4475 cell MnvMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2TIWmlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjd|IH7N NFm5eYhUSU6JRWK=
human HuH-7 cell MlK5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF22WpNKdmirYnn0bY9vKG:oIHj1cYFvKEi3SD23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvOzJibl2= M3L6bnNCVkeHUh?=
human J-RT3-T3-5 cell M2nEe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI\xXHJKdmirYnn0bY9vKG:oIHj1cYFvKEpvUmSzMXQ{NTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj6zPEBvVQ>? NIOwd4lUSU6JRWK=
human VM-CUB-1 cell NF;u[FBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoLwTY5pcWKrdHnvckBw\iCqdX3hckBXVS2FVVKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjZ5IH7N M4LUZ3NCVkeHUh?=
human MOLT-16 cell NWXMOYtmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2HweWlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjh2IH7N NV3pdIY2W0GQR1XS
human KG-1 cell MkLES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XUSGlvcGmkaYTpc44hd2ZiaIXtZY4hU0dvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlkhdk1? MoXHV2FPT0WU
human P12-ICHIKAWA cell MkfnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV:xTHhQUW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4xOSCwTR?= Ml[4V2FPT0WU
human ACN cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2rUS2lvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuNFIhdk1? MmXhV2FPT0WU
human COLO-684 cell NYnSOGp7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2j1UGlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22PFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy5|MTDuUS=> M{nuUXNCVkeHUh?=
human T-24 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXzyRZZbUW6qaXLpeIlwdiCxZjDoeY1idiCWLUK0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvQDZibl2= MoHkV2FPT0WU
human AGS cell MonTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYrHdG5HUW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE4yOSCwTR?= MUPTRW5ITVJ?
human EW-13 cell M3jUOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3;mV2lvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE42PCCwTR?= NHvWVmFUSU6JRWK=
human SW962 cell Mm[zS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYfCUmI4UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjV7IH7N MV;TRW5ITVJ?
human EW-11 cell MnvRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV\3fnNEUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZibl2= Ml;LV2FPT0WU
human RXF393 cell NIrBfIhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJHJZTjN7MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlY3KG6P MVTTRW5ITVJ?
human EoL-1-cell cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWLrdmVsUW6qaXLpeIlwdiCxZjDoeY1idiCHb1ytNU1k\WyuIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MU[uNUBvVQ>? MnqwV2FPT0WU

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 DMSO 75 mg/mL (72.79 mM)
Ethanol 75 mg/mL (72.79 mM)
Water slightly soluble or insoluble
体内 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol
10 mg/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
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

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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