KU-0063794

For research use only. Not for use in humans.

目录号:S1226

KU-0063794 Chemical Structure

CAS No. 938440-64-3

KU-0063794是一种有效的,高度特异性的,作用于mTORC1mTORC2的双重mTOR抑制剂,在无细胞试验中IC50约为~10 nM;对PI3Ks没有作用。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1464.74 现货
RMB 727.74 现货
RMB 1405.09 现货
RMB 3857.09 现货
RMB 5488.69 现货
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客户使用Selleck生产的KU-0063794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 KU-0063794是一种有效的,高度特异性的,作用于mTORC1mTORC2的双重mTOR抑制剂,在无细胞试验中IC50约为~10 nM;对PI3Ks没有作用。
靶点
mTORC1 [1]
(Cell-free assay)
mTORC2 [1]
(Cell-free assay)
~10 nM ~10 nM
体外研究

与mTOR抑制剂PP242相比, KU-0063794高特异性作用于mTOR,而对PI3Ks或其他76种激酶则无作用活性。30 nM KU-0063794作用于HEK-293细胞,通过抑制疏水基团(Thr389)磷酸化,及随后的T-环残基(Thr229) 磷酸化,而快速切除S6K1活性。300 nM KU-0063794作用于IGF1刺激的血清饥饿处理的 HEK-293细胞,抑制~90%S6K1活性。KU-0063794 为 100-300 nM时,也完全抑制氨基酸诱导的S6K1和 S6蛋白磷酸化。与S6K1类似, KU-0063794抑制mTORC1在 Ser2448位点磷酸化,也抑制mTORC2 在 Ser22481 位点磷酸化,这种作用存在剂量和时间依赖性。在血清存在时,或者IGF1刺激的情况下, KU-0063794抑制Akt 活性,或者Akt在 Ser473和 Thr308(意外的)位点磷酸化,也抑制Akt底物 PRAS40 在 Thr246位点,GSK3α/GSK3β在 Ser21/Ser9位点及Foxo-1/3a 在 Thr24/Thr32位点磷酸化,以上作用存在剂量依赖性。KU-0063794而不是 Rapamycin 抑制SGK1活性和 在Ser422位点磷酸化,也抑制其生理底物NDGR1,与抑制S6K1 和Akt磷酸化程度相似,这种作用存在剂量依赖性,然而KU-0063794 不抑制佛波酯诱导的ERK 或RSK磷酸化和RSK激活。与Rapamycin相比, KU-0063794更有效诱导4E-BP1在 Thr37, Thr46和 Ser65位点完全去磷酸化。KU-0063794抑制野生型和mLST8-缺陷型MEFs细胞生长,也诱导细胞周期停在G1期,比Rapamycin效果更显著。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2  NGHzRm1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmnjNE4y6oDVNUFCpO69VQ>? NIfTUlk4OiCq NUTjT|dx\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ5OEixPUc,OjZ{N{i4NVk9N2F-
HepG2  NUfwWoZFS2:ub375JGZwem2jdHnvckBCe3OjeR?= M1H0[FHjiJN3MNMg{txO MoTqNVAh\A>? NWnKbmJ[\GWlcnXhd4V{KHSqZTDueY1j\XJib3[geoli[mynIFjldGczKGOxbH;ubYV{yqC|aXfubYZq[2GwdHz5 NG\vVIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK3PFgyQSd-Mk[yO|g5OTl:L3G+
HepG2  NYHSbFZUSXCxcITvd4l{KEG|c3H5 MYWwMlHjiJN3MNMg{txO M{TEZVQ5KGh? NIX0ZmVqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NH;KdlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK3PFgyQSd-Mk[yO|g5OTl:L3G+
HepG2  MonYSpVv[3Srb36gRZN{[Xl? NUjNWm94PS9zMDFOwG0> M{DpO|I1KGh? NEfGXXVlemGvYYTpZ4FtdHliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEBifCCVZYKtOFc{ NF\pUWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK3PFgyQSd-Mk[yO|g5OTl:L3G+
HepG2  M33JN2Z2dmO2aX;uJGF{e2G7 NVrpNnVDPS9zMDFOwG0> Mmn3NlQhcA>? Mm\h[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IFjJSlHPuSCjbnSgZ5lkdGmwIFSxxsA> NFvBWnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK3PFgyQSd-Mk[yO|g5OTl:L3G+
HepG2  MYHGeY5kfGmxbjDBd5NigQ>? Mon6NE4y6oDVNUFCpO69VQ>? NXL4fYxmOjRiaB?= NFP0cHVqdmS3Y3XzJJA3OiCmb4fudoVofWyjdHnvckwhSmWlbHnuMVEh\XiycnXzd4lwdiCjbnSgUGM{Si2LIITvJGxEO0JvSVmgZ49vfmW{c3nvckBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M4n0cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mke4PFE6Lz5{NkK3PFgyQTxxYU6=
HepG3  NYDJSlV[TnWwY4Tpc44hSXO|YYm= MYCwMlHjiJN3MNMg{txO NHrVZVY1QCCq MXnpcoR2[2W|IHPlcIwh[XW2b4DoZYd6KGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NIHkdJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK3PFgyQSd-Mk[yO|g5OTl:L3G+
AGS NIrM[mxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PNOGlEPTB;MUWuNEDDuSB{LkmxJO69VQ>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7N{S3PEc,OjR3OUe0O|g9N2F-
HGC27 Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrIN25KSzVyPUG1MlAhyrFiND64NkDPxE1? M17CdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm3OFc5Lz5{NEW5O|Q4QDxxYU6=
MKN45 NV;GfXY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjCTWM2OD1yLkiyJOKyKDBwMEGg{txO M2TkW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm3OFc5Lz5{NEW5O|Q4QDxxYU6=
NUGC4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fwbWlEPTB;Mj65N{DDuSByLkOxJO69VQ>? MojjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3OUe0O|goRjJ2NUm3OFc5RC:jPh?=
PC9 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3oO|IhcA>? NV;pR4pXUUN3ME2xNE4yPcLzMD62NkBvVQ>? NWjTfHBtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4O|Q5QDBpPkKzPFc1QDhyPD;hQi=>
PC9GR NILBT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2q5U|czKGh? NYTDdnhPUUN3ME22MlIyyrFzLkOwJI5O MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh5NEi4NEc,OjN6N{S4PFA9N2F-
H1650 MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;sO|IhcA>? NVO5eWpLUUN3ME23MlYyyrFyLk[yJI5O NHj5UpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i3OFg5OCd-MkO4O|Q5QDB:L3G+
H1975 NYHSbmNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEj4eHo4OiCq NIT5UlZKSzVyPUGxMlE2yrFyLkmzJI5O NYrweYZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4O|Q5QDBpPkKzPFc1QDhyPD;hQi=>
PC9 NI\CPWNHfW6ldHnvckBCe3OjeR?= MUmxNE4yPSCwTR?= NFfLOIY4OiCq NGTwXGxqdmirYnn0d{BuXE:UIIDoc5NxcG:{eXzheIlwdiC|dHH0eZPDqA>? M3zDUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEe0PFgxLz5{M{i3OFg5ODxxYU6=
PC9GR MYLGeY5kfGmxbjDBd5NigQ>? NGTKc|c3NjJzIH7N NH36UXg4OiCq M1PXbYlvcGmkaYTzJI1VV1JicHjvd5Bpd3K7bHH0bY9vKHO2YYT1d:Kh M1T1dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEe0PFgxLz5{M{i3OFg5ODxxYU6=
H1650 MofpSpVv[3Srb36gRZN{[Xl? NXLWeW5oPy54MTDuUS=> MWC3NkBp MX3pcohq[mm2czDtWG9TKHCqb4PwbI9zgWyjdHnvckB{fGG2dYRCpC=> NYDjZXpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4O|Q5QDBpPkKzPFc1QDhyPD;hQi=>
H1975 NXT0eHBSTnWwY4Tpc44hSXO|YYm= M{j5dFEyNjF3IH7N Mn76O|IhcA>? NWG0XVU2cW6qaXLpeJMhdVSRUjDwbI9{eGixconsZZRqd25ic4TheJV{yqB? M1jjNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEe0PFgxLz5{M{i3OFg5ODxxYU6=
PC9 NIP5T4dHfW6ldHnvckBCe3OjeR?= M{jkU|ExNjF3IH7N M1TnVFczKGh? NHjzSY9qdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YheDdyU{\L NG\GcXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i3OFg5OCd-MkO4O|Q5QDB:L3G+
PC9GR Mn3RSpVv[3Srb36gRZN{[Xl? M1mzUFYvOjFibl2= M2f3eFczKGh? M3;0PIlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBxPzCVNlu= NE\ifGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i3OFg5OCd-MkO4O|Q5QDB:L3G+
H1650 NE\XenFHfW6ldHnvckBCe3OjeR?= MnzsO{43OSCwTR?= NXPTUnp5PzJiaB?= M1WwVolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBxPzCVNlu= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh5NEi4NEc,OjN6N{S4PFA9N2F-
H1975 MVjGeY5kfGmxbjDBd5NigQ>? NXvGZ3VwOTFwMUWgcm0> M3mw[lczKGh? MmXubY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJJA4OFN4Sx?= Ml3SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6N{S4PFAoRjJ|OEe0PFgxRC:jPh?=
LNCaP NF3hWYZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3fhOFAuOTBizszN NEjjPGgzPCCqwrC= Mn\2[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M3vvWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OESwOlA2Lz5{M{i0NFYxPTxxYU6=
PC-3 MkHhR4VtdCCYaXHibYxqfHliQYPzZZk> NITKUJQxNTFyIN88US=> M3;5TlI1KGkEoB?= M3Lm[IRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NFftfow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0NFYxPSd-MkO4OFA3ODV:L3G+
MDA-MB-468  Mmi4R4VtdCCYaXHibYxqfHliQYPzZZk> NE\3WGsxNTFyIN88US=> MoDsNlQhcMLi Monr[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NGHOOlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0NFYxPSd-MkO4OFA3ODV:L3G+
LNCaP NYW0cZdvTnWwY4Tpc44hSXO|YYm= MWCyNFDjiJN6MECgcm0> MYeyOEBpyqB? MWLk[YNz\WG|ZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBt\X[nbDDv[kBxPzCVNlugbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NUK4ZodERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFA3ODVpPkKzPFQxPjB3PD;hQi=>
PC-3 NHf2V3ZHfW6ldHnvckBCe3OjeR?= NGXtOlkzODEkgKO4NFAhdk1? MnS2NlQhcMLi M3zKPYRm[3KnYYPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGyndnXsJI9nKHB5MGO2T{BqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NEnT[|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0NFYxPSd-MkO4OFA3ODV:L3G+
MDA-MB-468  MWDGeY5kfGmxbjDBd5NigQ>? M3;mNFIxOOLCk{iwNEBvVQ>? MmLsNlQhcMLi NFjh[ZJl\WO{ZXHz[ZMhfGinIIDoc5NxcG:{eXzheIlwdiCuZY\lcEBw\iCyN{DTOmshcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NXjZeJBJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFA3ODVpPkKzPFQxPjB3PD;hQi=>
Caki-1  NFP1NnVHfW6ldHnvckBCe3OjeR?= MYCxNFAuOjByMDDuUS=> NVLJTFBJOTBvMUiwJI1qdg>? NFXRT2ZFVVOR NXv0UpY{cW6qaXLpeJMh[m:2aDDtWG9TSzFiYX7kJI1VV1KFMjDhd{BqdmSrY3H0[YQh[nlidHjlJIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHnvckBw\iCmb4fud5Rz\WGvIHXm[oVkfG:{cx?= MkHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NEm5PFkoRjJ|M{S5PVg6RC:jPh?=
786-O M{PaSWZ2dmO2aX;uJGF{e2G7 NHvLb2UyODBvMkCwNEBvVQ>? MX[xNE0yQDBibXnu MVrEUXNQ M2DRWolvcGmkaYTzJIJwfGhibWTPVmMyKGGwZDDtWG9TSzJiYYOgbY5lcWOjdHXkJIJ6KHSqZTDk[YNz\WG|ZTDpckBxcG:|cHjvdplt[XSrb36gc4Yh\G:5boP0doVidSCnZn\lZ5RwenN? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2OUm4PUc,OjN|NEm5PFk9N2F-
Caki-1  NFPGTY5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXX4R3VrOzByLUSwNFAhdk1? MVeyOE06PiCq MnX0SG1UVw>? NYnHcJNUe3WycILld5NmeyC2aHWgZ4VtdCC4aXHibYxqfHliaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NEO3TYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0PVk5QSd-MkOzOFk6QDl:L3G+
786-O MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVjIN3BbOzByLUSwNFAhdk1? M4PwPFI1NTl4IHi= M3K0SWROW09? M4TJSZN2eHC{ZYPz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NF22SHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0PVk5QSd-MkOzOFk6QDl:L3G+
Caki-1  MnGzSpVv[3Srb36gRZN{[Xl? MnvRNkDDvU1? NHnw[4Y4OiCq MVfEUXNQ MYTpcoR2[2W|IFexJINmdGxiY4njcIUh[XK{ZYP0JIFv\CCjdYTvdIhi\3l? NYrvSJlyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOFk6QDlpPkKzN|Q6QTh7PD;hQi=>
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SK-N-SH NVPBVINEeUiWUzDhd5NigQ>? M2DlVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vU1igZ4VtdHN? M4rteVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-S6K / S6K / p-4E-BP1 / E7 / E6 / p53 ; 

PubMed: 28115701     


Normoxic HPV-positive cancer cells were treated for 24 h with 0.5, 1.0, or 5 μM KU-0063794 (KU) or 50 nM rapamycin. Shown are immunoblots of P-S6K, S6K, P-4E-BP1, 4E-BP1, HPV16/18 E6/E7, and p53 protein levels. DMSO served as a solvent control; β-actin, as a loading control.

p-mTOR; 

PubMed: 24262658     


Inhibition of mTOR pathway by mTOR kinase inhibitors. MCC-2 cells were treated with WYE354 (3 μM), PP242 (2.5 μM), and Ku-0063794 (5 μM) for 24h, respectively. Lysates were prepared and subjected to immunoblotting analysis with indicated antibodies. 

28115701 24262658
体内研究 Ku0063794在肾脏上皮肾细胞癌的临床前模型中,抑制肿瘤生长和mTOR信号。然而,在动物研究中,Ku0063794没有temsirolimus有效,可能的原因是temsirolimus对肿瘤的微环境有重要的作用,能在异种移植瘤中减少血管生成,而Ku0063794无此效果。经Temsirolimus处理的肿瘤组织比Ku0063794处理的肿瘤组织更少地表达VEGF和PDGF[2]

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

mTOR 复合物激酶检测实验:

HEK-293细胞新鲜溶解在Hepes裂解液中。溶解产物(1-4 mg) 通过与5-20 μL G蛋白的琼脂糖凝胶结合免疫前抗体IgG温育而预先清除。裂解抽提物与5-20 μL G蛋白的琼脂糖凝胶结合的 5-20 μg抗Rictor或抗Raptor抗体的 免疫前抗体IgG温育。所有抗体共价结合到蛋白G蛋白琼脂糖凝胶上。在振动转载台上4oC下进行 免疫沉淀1小时。使用Hepes 裂解液冲洗免疫沉淀物四次,随后使用Hepes激酶buffer冲洗两次。使用 Raptor免疫沉淀物磷酸化 S6K1, 两次冲洗的初始步骤中,buffer 含0.5 M NaCl,确保最佳激酶活性。血清饥饿的 HEK-293细胞中分离的GST-Akt1与PI-103(1 μM 进行 1 小时)温育。从血清饥饿的HEK-293 细胞中纯化的GST-S6K1与Rapamycin (0.1 μM进行1小时)温育。加入0.1 mM ATP和 10 mM MgCl2 ,在不同浓度KU-0063794和GST-Akt1 (0.5 μg)或GST-S6K1 (0.5 μg)存在时,开始mTOR反应。反应在 30oC下在振动转载台上进行30分钟,然后加入SDS样本缓冲液终止反应。反应混合物在0.22-μm-孔径大小 Spin-X过滤器上过滤,样本进行电泳处理,然后使用指定抗体进行免疫印迹分析。
细胞实验:

[1]

- 合并
  • Cell lines: 野生型和mLST8缺陷型MEFs
  • Concentrations: 溶于DMSO,终浓度为~3 μM
  • Incubation Time: 24, 48, 和72 小时
  • Method:

    使用KU-0063794 处理细胞 24, 48, 和72 小时,每24小时更换一次培养基,加入新鲜溶解的KU-0063794。为了测量细胞生长,使用PBS冲洗细胞一次,然后与4% (v/v) 多聚甲醛在 PBS混合15分钟。用水冲洗一次后,使用溶于 10% 乙醇的0.1% 结晶紫对细胞染色20分钟,然后用水冲洗三次。 使用0.5 mL 10% (v/v) 乙酸从细胞中抽提结晶紫20分钟。然后洗脱液在水中按1:10稀释,然后在 590 nm 处测量吸光值。为了测量细胞周期分布,通过胰蛋白酶化作用收集细胞,然后在PBS中冲洗一次,再悬浮于冰冻70% (v/v)乙醇中。细胞在 PBS和 1% (w/v) BSA中冲洗两次,再在 PBS 和含 50 g/mL 碘化丙啶和 50 g/mL RNase A的0.1% (v/v) Triton X-100中染色 20分钟。使用FACSCalibur流式细胞仪和CellQuest软件检测细胞中DNA含量。在线性标度上测量红色荧光(585 nm),进行脉冲宽度分析用于排除双峰值。使用FlowJo软件测定细胞周期分布。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: Nu/Nu裸鼠
  • Dosages: 8 mg/kg
  • Administration: i.p.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 16 mg/mL (34.36 mM)
Water Insoluble
Ethanol 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):
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/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 465.54
化学式

C25H31N5O4

CAS号 938440-64-3
储存条件 粉状
溶于溶剂
别名 N/A

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

技术支持

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

如果有其他问题,请给我们留言。

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mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID