Temsirolimus (CCI-779)

For research use only. Not for use in humans.

Pfizer辉瑞授权 目录号:S1044 别名: NSC 683864 中文名称:替西罗莫司

Temsirolimus (CCI-779) Chemical Structure

CAS No. 162635-04-3

Temsirolimus (CCI-779, NSC 683864)是一种特定的mTOR抑制剂,在无细胞试验中IC50为1.76 μM。Temsirolimus 可诱导自噬和凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1087.98 现货
RMB 953.84 现货
RMB 2025.24 现货
RMB 3016.49 现货
RMB 7122.99 现货
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客户使用Selleck生产的Temsirolimus (CCI-779)发表文献65篇:

产品安全说明书

mTOR抑制剂选择性比较

生物活性

产品描述 Temsirolimus (CCI-779, NSC 683864)是一种特定的mTOR抑制剂,在无细胞试验中IC50为1.76 μM。Temsirolimus 可诱导自噬和凋亡。
靶点
mTOR [1]
(Cell-free assay)
1.76 μM
体外研究

Temsirolimus抑制核糖体蛋白S6磷酸化,作用于PTEN阳性DU145细胞比作用于PTEN阴性PC-3细胞更有效,且抑制细胞生长,和细胞的克隆生存,这种作用存在浓度依赖性。[5] Temsirolimus按100 ng/mL剂量处理原代人淋巴细胞性白血病(ALL) 细胞,显著抑制增殖,且诱导凋亡。[6]在 FKBP12存在时, Temsirolimus 有效抑制mTOR 激酶活性,IC50为1.76 μM, 与Rapamycin(IC50为1.74 μM)类似。Temsirolimus按纳摩尔浓度(10 nM 到<5 μM) 处理,通过FKBP12依赖机制,具有适度的选择性抗增殖活性,在低微摩尔浓度 (5-15 μM)时,可以完全抑制多种肿瘤细胞增殖,涉及FKBP12非依赖性的 mTOR信号阻断。Temsirolimus 按微摩尔而不是纳摩尔浓度 (20 μM)处理,显著降低全部蛋白质合成,也显著降低多聚核糖体的分解, 伴随着翻译延伸因子 eEF2和翻译起始因子eIF2A的磷酸化快速提高。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HSC-4 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYjFUGNkUW6qaXLpeIlwdiCxZjDoeY1idiCKU1OtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTF|IH7N M4PMUnNCVkeHUh?=
human L-363 cell NFj0b4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlPaTY5pcWKrdHnvckBw\iCqdX3hckBNNTN4MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlQzKG6P NY\wTG82W0GQR1XS
human Ramos-2G6-4C10 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MknxTY5pcWKrdHnvckBw\iCqdX3hckBT[W2xcz2yS|YuPENzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|QzKG6P MVzTRW5ITVJ?
human SBC-1 cell NIjGNXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVy1Vo9CUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDR2IH7N NHj1UZFUSU6JRWK=
human MHH-PREB-1 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnX4TY5pcWKrdHnvckBw\iCqdX3hckBOUEhvUGLFRk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OUWgcm0> NH;VU21USU6JRWK=
human LNCAP cells NGTJW|JRem:uaX\ldoF1cW:wIHHzd4F6 MUOzJIRigXN? NV3I[HFPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUCuOUBvVQ>? M1jwXFIyPDN6NUe5
human HH cell NF3iSnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkTFTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNk[0JI5O M3juTHNCVkeHUh?=
human TYK-nu cell M3vIdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|c5KG6P NIfGc5FUSU6JRWK=
human H4 cell NFjjSHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUTn[ZA5UW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFchdk1? MVTTRW5ITVJ?
human K5 cell NXXGdVBvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoC5TY5pcWKrdHnvckBw\iCqdX3hckBMPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwM{Ogcm0> MYjTRW5ITVJ?
human PA-1 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkT6TY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT60O{BvVQ>? MYDTRW5ITVJ?
human SK-NEP-1 cell NUXITldiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3PrVWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTlXQMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR7IH7N Mn;nV2FPT0WU
human 697 cell M4H1bmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIfLbXVKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO{BvVQ>? M3q5SnNCVkeHUh?=
human CTB-1 cell NGTvVndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXHIW45YUW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTNibl2= MoPWV2FPT0WU
human DB cell M33VN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJGRDKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5zMjDuUS=> NXPOXFJQW0GQR1XS
human MLMA cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TPbGlvcGmkaYTpc44hd2ZiaIXtZY4hVUyPQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|Ehdk1? M1nQc3NCVkeHUh?=
human GAMG cell MkLnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWHtO4lHUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OiCwTR?= NIHTTGFUSU6JRWK=
human JVM-3 cell M{HB[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWLDV2pWUW6qaXLpeIlwdiCxZjDoeY1idiCMVl2tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTVibl2= NUPJWG11W0GQR1XS
human LAMA-84 cell NV;odYN5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF6wblFKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB|IH7N NVrobIZIW0GQR1XS
human RPMI-8226 cell MlzMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVPJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvOEKyOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTVibl2= MUHTRW5ITVJ?
human MOLT-4 cell MoLIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXnHXItLUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjNzIH7N M2TGfnNCVkeHUh?=
human CAMA-1 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVH4Vm06UW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd5IH7N MXHTRW5ITVJ?
human NCI-SNU-1 cell Ml3mS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2VTmWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQDFibl2= MUXTRW5ITVJ?
human SW780 cell MnTGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILDc3NKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45OyCwTR?= NXjqOlRCW0GQR1XS
human H9 cell NXHNcHVzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEPlVIlKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND64PEBvVQ>? MnLGV2FPT0WU
human BE-13 cell M3PNXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYXJcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND65NUBvVQ>? NFfSboFUSU6JRWK=
human ES8 cell M2XqZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHfZSoJKdmirYnn0bY9vKG:oIHj1cYFvKEWVODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNlchdk1? MkDVV2FPT0WU
human DEL cell NXHpSHdrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mnm4TY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS2JI5O M3\nUXNCVkeHUh?=
human QIMR-WIL cell M{TkbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVjJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44OSCwTR?= NW\ZZ4RUW0GQR1XS
human CGTH-W-1 cell NX3CU4RMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2fxdWlvcGmkaYTpc44hd2ZiaIXtZY4hS0eWSD3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njd3IH7N NHn6dm1USU6JRWK=
human CHL-1 cell MlW0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEDmO|JKdmirYnn0bY9vKG:oIHj1cYFvKEOKTD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU45PiCwTR?= NEe4e|BUSU6JRWK=
human A2780 cell MkfMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWi3OW17UW6qaXLpeIlwdiCxZjDoeY1idiCDMke4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDhibl2= NXnocoh3W0GQR1XS
human VA-ES-BJ cell MkjCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnLFTY5pcWKrdHnvckBw\iCqdX3hckBXSS2HUz3CTkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQSCwTR?= M2rKWnNCVkeHUh?=
human BB65-RCC cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mkj2TY5pcWKrdHnvckBw\iCqdX3hckBDSjZ3LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVchdk1? NVToTY43W0GQR1XS
human D-566MG cell NHKzdYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XmZ2lvcGmkaYTpc44hd2ZiaIXtZY4hTC13Nk\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOTZibl2= NF33NHVUSU6JRWK=
human MDA468 cells NYXY[YVQWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlXLN{Bl[Xm| M2qzfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBOFY5KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;ODDuUS=> M1eydVIyPDN6NUe5
human HO-1-N-1 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{m1S2lvcGmkaYTpc44hd2ZiaIXtZY4hUE9vMT3OMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRThwMjDuUS=> M2O5THNCVkeHUh?=
human RS4-11 cell M2LDSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVj2PXpsUW6qaXLpeIlwdiCxZjDoeY1idiCUU{StNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR3IH7N M1e4TXNCVkeHUh?=
human PC-3 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MonhTY5pcWKrdHnvckBw\iCqdX3hckBRSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OT6xOEBvVQ>? MVPTRW5ITVJ?
human NB69 cell NYfNS4ttT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX[5PXFCUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PiCwTR?= MVzTRW5ITVJ?
human HGC-27 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJGhISy1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOkBvVQ>? MYnTRW5ITVJ?
human NCI-H720 cell M{P5Zmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoXsTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEeyNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPjJibl2= MkXHV2FPT0WU
human NCI-H292 cell M{HDbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2fXS2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Njh2IH7N MlO4V2FPT0WU
human A3-KAW cell NXq4NZFIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUX2ZVBTUW6qaXLpeIlwdiCxZjDoeY1idiCDMz3LRXch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC52MzDuUS=> NHK5elFUSU6JRWK=
human DU-4475 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlfOTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPzNibl2= M3:5SnNCVkeHUh?=
human HuH-7 cell M3Lic2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml3zTY5pcWKrdHnvckBw\iCqdX3hckBJfUhvNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyMlMzKG6P MnWxV2FPT0WU
human J-RT3-T3-5 cell M{TwZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYDCbHNWUW6qaXLpeIlwdiCxZjDoeY1idiCMLWLUN{1VOy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKuN|ghdk1? M4DWUHNCVkeHUh?=
human VM-CUB-1 cell NXfDTG5sT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYC2SWpvUW6qaXLpeIlwdiCxZjDoeY1idiCYTT3DWWIuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lk[3JI5O NHjrN2lUSU6JRWK=
human MOLT-16 cell M3TK[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3vq[mlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjh2IH7N MnHWV2FPT0WU
human KG-1 cell M33mOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVjJcohq[mm2aX;uJI9nKGi3bXHuJGtINTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMj65JI5O M1vCcHNCVkeHUh?=
human P12-ICHIKAWA cell M13j[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlfrTY5pcWKrdHnvckBw\iCqdX3hckBROTJvSVPITWtCX0FiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6wNUBvVQ>? M4\wPHNCVkeHUh?=
human ACN cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWDJcohq[mm2aX;uJI9nKGi3bXHuJGFEViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkCyJI5O M1;ldnNCVkeHUh?=
human COLO-684 cell M2HscGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4rkTmlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22PFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy5|MTDuUS=> NIr0ZmFUSU6JRWK=
human T-24 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NE\yR3hKdmirYnn0bY9vKG:oIHj1cYFvKFRvMkSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{45PiCwTR?= MlrIV2FPT0WU
human AGS cell M4PpZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGSxemVKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlEyKG6P NXrtd5pjW0GQR1XS
human EW-13 cell NF;IRZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHy5R2JKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTRibl2= MnzpV2FPT0WU
human SW962 cell NXLEZ4tRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYjJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuOVkhdk1? M2XadXNCVkeHUh?=
human EW-11 cell M2TMS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXrTV5k3UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjZibl2= MXPTRW5ITVJ?
human RXF393 cell M1fLbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJHJZTjN7MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlY3KG6P MUnTRW5ITVJ?
human EoL-1-cell cell MljpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEG1TXVKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNj6xJI5O NWHiTHAxW0GQR1XS

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-mTOR / mTOR / p-S6 / S6 / p-4E-BP1 / 4E-BP1 ; 

PubMed: 23291985     


The mTOR inhibitor temsirolimus inhibits the activation of mTOR and its downstream molecules in esophageal cancer cells. Three esophageal cancer cell lines (TE-1, TE-8, and TE-10) were treated with different concentrations of temsirolimus (0–1000nM) and western blot was performed with appropriate antibodies to detect the expression of mTOR and its downstream effectors. β-actin was served as an internal control.

p-rS6 / rS6 / p-AKT /AKT ; 

PubMed: 22039466     


C, D, Phosphorylation of rS6 (P-rS6) and Akt (P-Akt T308 and P-Akt S473) after treatment with indicated doses of temsirolimus for 72 hrs in temsirolimus-sensitive (C) or temsirolimus-resistant (D) cells was determined by Western blotting. Expression of total rS6 and Akt protein serves as loading controls.

23291985 22039466
Immunofluorescence
NRF2; 

PubMed: 22848625     


Ectopic expression of Nrf2 (red) and nuclear staining with Dapi (blue) after a 6 hour drug incubation. Yellow numbers represent the percent of cells with nuclear Nrf2 +/− the standard deviation. Scale bar = 10 µM.

22848625
Growth inhibition assay
Cell growth (HGC-3 cells) ; 

PubMed: 30866995     


Effect of temsirolimus on the growth of HGC-3 and -20 cells in primary culture. 

Cell viability ; 

PubMed: 22039466     


A, B, Endometrial cancer cells were treated with increasing doses of temsirolimus for 72 hrs. Results are separated by (A) sensitivity or (B) resistance as determined by cell viability. 

30866995 22039466
体内研究 Temsirolimus 按20 mg/kg 剂量腹腔注射,每周5天,显著延迟DAOY 移植瘤生长,与对照组相比,处理一周,延迟160%,处理两周,延迟240%。Temsirolimus按 100 mg/kg高剂量单独给药腹腔注射,一周内,诱导肿瘤体积衰退37%。 Temsirolimus 处理2两周,也延迟抗Rapamycin的U251移植瘤生长,延迟148%。[2]Temsirolimus 作用于患Huntington疾病的小鼠模型,抑制mTOR,提高四种不同行为任务的表现,且降低聚合形成。[3] Temsirolimus处理8226, OPM-2,和 U266移植瘤的皮下生长,诱导显著的抗癌反应,这种作用存在剂量依赖性,作用于8226和 OPM-2移植瘤,ED50分别为20 mg/kg 和2 mg/kg,与抑制增殖和血管生长,诱导凋亡,和肿瘤细胞尺寸降低相关。 [4] 每天按10 mg/kg剂量处理携带人ALL的NOD/SCID移植瘤模型,降低外周血膨胀和脾肿大。[6]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

体外mTOR 催化活性检测:

Flag标记的野生型人 mTOR (Flag-mTOR) DNA 结构短暂转染进HEK293 细胞。48小时后,进行蛋白提取和Flag-mTOR纯化。在体外,在不同浓度Temsirolimus存在而没 FKBP12 时,在96孔板上进行纯化的Flag-mTOR激酶实验,通过解离增强镧系荧光免疫分析(DELFIA),使用His6-S6K1 作为底物来测量。在激酶实验 buffer (10 mM Hepes pH 7.4, 50 mM NaCl, 50 mM β-甘油磷酸,10 mM MnCl2, 0.5 mM DTT, 0.25 μM微囊藻素 LR, 和 100 μg/mL BSA)上第一次对酶进行稀释。每孔中,12 μL 稀释的酶与0.5 μL Temsirolimus混合。加入含ATP 和His6-S6K 的12.5 μL 激酶buffer开始激酶反应,终体积为25 μL,含800 ng/mL FLAG-mTOR, 100 μM ATP, 和 1.25 μM His6-S6K。反应板在室温下温和震荡温育2小时,加入 25 μL 终止液(20 mM Hepes pH 7.4, 20 mM EDTA, 和 20 mM EGTA)终止反应。磷酸化的(Thr-389) His6-S6K 的DELFIA 检测在室温下使用单克隆抗P(T389)-p70S6K抗体进行,抗体使用铕-N1-ITC (Eu) (每种抗体10.4 Eu)标记。45 μL终止的激酶反应混合物转移到含55 μL PBS的MaxiSorp板上。His6-S6K 粘附2小时后,吸除每孔,使用PBS冲洗。加入含40 ng/mL Eu-P(T389)-S6K 抗体的 100 μL DELFIA buffer。轻轻搅拌,再使抗体结合持续进行1小时。吸除每孔,然后使用含0.05% Tween-20(PBST)的PBS冲洗4次。每孔加入100 μL of DELFIA增强溶液,然后在 PerkinElmer Victor 模板酶标仪上读数。
细胞实验:[1]
- 合并
  • Cell lines: A549, H157, H460, H446, HCT116, HT29, SW480, DLD1, Caco2, LNCap, DU145, MDA468, MDA231, HEK293, 和PC3-MM2
  • Concentrations: 溶于DMSO,终浓度为~20 μM
  • Incubation Time: 72小时
  • Method: 使用不同浓度Temsirolimus处理细胞72小时。处理后,通过MTS染料转换,使用CellTiter AQ 检测试剂盒测定存活细胞密度。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 皮下注射DAOY, 或U251细胞的雌性无胸腺裸鼠
  • Dosages: 20 mg/kg
  • Administration: 每天注射,每周5次
    (Only for Reference)

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 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300 +2% Tween 80+ddH2O
7mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 1030.29
化学式

C56H87NO16

CAS号 162635-04-3
储存条件 粉状
溶于溶剂
别名 NSC 683864

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01653067 Unknown status Drug: Rituximab Temsirolimus DHAP intravenous Diffuse Large B-Cell Lymphoma Mathias Witzens-Harig|Johannes Gutenberg University Mainz|Technische Universität München|Ludwig-Maximilians - University of Munich|University Hospital Ulm|University Hospital Erlangen|Charite University Berlin Germany|University Hospital Freiburg|Johann Wolfgang Goethe University Hospital|University Hospital Heidelberg September 2012 Phase 2
NCT02093598 Completed Drug: Temsirolimus Carcinoma Endometrioid|mTOR Protein MedSIR May 2012 Phase 2

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在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID