Rapamycin (Sirolimus) 化学構造
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製品説明

  • Compare mTOR Inhibitors
    mTOR製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Rapamycin (Sirolimus) は、特定のmTOR阻害剤で、IC50 が ~0.1 nMです。
ターゲット

mTOR

IC50

~0.1 nM [1]

In vitro試験 Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. [1] In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. [2] Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity Description
HT-29 MUfDfZRwfG:6aXOgRZN{[Xl? Ml;yNVAhdk1? NIPIVJo4OiCq NFnWVGhFVVOR NETlPZRRd3SnboTpZZRmeyClYX3weI91cGWlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJk>
HT-29 NXrsepdmS3m2b4TvfIlkKEG|c3H5 NEL4XHIyOCCwTR?= Mle0O|IhcA>? NH\lR|lFVVOR MmjUVI91\W62aXH0[ZMh\GmpaYTvfIlvNWmwZIXj[YQh[3m2b4TvfIlkcXS7
HT-29 MYXDfZRwfG:6aXOgRZN{[Xl? NITk[Y0yOCCwTR?= NIXqSHM4OiCq NUjJVWJoTE2VTx?= Mlv6VI91\W62aXH0[ZMhPS2obIXvdo92emGlaXytbY5lfWOnZDDjfZRwfG:6aXPpeJk>
PC3 MmLUT4lv[XOnIFHzd4F6 NGfYdpQyODBibl2= MWWxJIg> NUnYWZg{TE2VTx?= M3HHS3BwfGWwdHz5JIlvcGmkaYTzJI1VV1JvbXXkbYF1\WRiU{[gdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kA9OTBibl2u
PC3 NXWy[mF1U2mwYYPlJGF{e2G7 MkH1NVAxKG6P NYDPcnpjOSCq MX\EUXNQ M2iyZ2Rw\XNibn;0JIlvcGmkaYSgcXRQWi2vZXTpZZRm\CCDa4SgdIhwe3Cqb4L5cIF1cW:w
PC3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXuwboE2OS53IN88US=> NIO3WpAyKGh? M{TpTGROW09? NFS2OXdKdmS3Y3XzJIFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IIfpeIghUUN3MDDv[kA9OTBibl2=
HEK293 NG\Q[WpHfW6ldHnvckBCe3OjeR?= MWexNFAhdk1? NYPHN2dYQCCq MWTEUXNQ MofBTY5pcWKrdIOgWHBCNWmwZIXj[YQh\GWpcnHkZZRqd25ib3[gVIRk\DRid3n0bEBGSzVyIH;mJFUxKG6P
BT-20 NIqyZYpMcW6jc3WgRZN{[Xl? MnPTNlAh|ryP MWDEUXNQ NUmyT4VDTG:nczDuc5QhcW6qaXLpeEBuXE:UQ{Kg[IVx\W6mZX70JJBCc1RiU{S3N{BxcG:|cHjvdplt[XSrb36=
U937 MmjKRY51cWKjY4TldolidCCDc4PhfS=> NFuwRok2OCEQvF2= MVK0PEBp NUPoSHM4TE2VTx?= MoHQTY5lfWOnczDhcpRq[mGldHXybYFtKGGldHn2bZR6KGGpYXnud5Qhf2muZDD0fZBmKEynZ3nvcoVtdGFicH7leY1weGirbHGgVIhqdGGmZXzwbIliNTFiSmKzNkBqdiCXOUO3JINmdGy|
U937 M2HQeGFvfGmkYXP0[ZJq[WxiQYPzZZk> M4HxblUxKM7:TR?= Mm\sOFghcA>? MlnNSG1UVw>? MU\Ec4V{KG6xdDDpcoR2[2ViYX70bYJi[3SncnnhcEBi[3Srdnn0fUBi\2GrboP0JG1KWCCycn;0[YlvNWSnZnnjbYVvfCCOZXfpc45mdGyjIIDu[ZVud3CqaXzhJGpTOzJvMjDpckBWQTN5IHPlcIx{
U937 NHLvUGJCdnSrYnHjeIVzcWGuIFHzd4F6 M4nDUlUxKM7:TR?= NFywcpo1QCCq NXK2eXdtTE2VTx?= MYPEc4V{KG6xdDDpcoR2[2ViYX70bYJi[3SncnnhcEBi[3Srdnn0fUBi\2GrboP0JGV{[2incnnjbIliKGOxbHmgTGIyODFiaX6gWVk{PyClZXzsdy=>
MCF-7 NVzDfYxKSXW2b4DoZYd6KEG|c3H5 NWnhfmVoOzBibl2= NXH6c3NPPCCq NGnl[mhFVVOR Ml\KTY5lfWOnczDheZRweGijZ4m=
U87MG MWLLbY5ie2ViQYPzZZk> NWe3TmR5OSEQvF2= NI\mWYo3KGh? NHO3VIhFVVOR MkLMVI91\W62bImgbY5pcWKrdIOgcXRQWi2vZXTpZZRm\CCVNjDwbI9{eGixconsZZRqd25?
U87MG Mlz2T4lv[XOnIFHzd4F6 Mm\HNUDPxE1? M331blYhcA>? NV:zVXptTE2VTx?= MYjQc5RmdnSueTDpcohq[mm2czC0SWJROSiWN{CpJJBpd3OyaH;yfYxifGmxbh?=
U87MG MXrLbY5ie2ViQYPzZZk> M1j2TlEh|ryP NXL1OZhSPiCq MlPTSG1UVw>? NI[wNXlFd2W|IH7veEBqdmirYnn0JI1VV1JvbXXkbYF1\WRiQXv0JJBpd3OyaH;yfYxifGmxbh?=
U87MG M2jUUmtqdmG|ZTDBd5NigQ>? NWLWVIVbOSEQvF2= NUDNN4k6PiCq Mm\lSG1UVw>? NW\vOGJKTG:nczDuc5QhcW6qaXLpeEBRNTSHQmCxLHQ{Py92NjmgdIhwe3Cqb4L5cIF1cW:w
COS7 cells expressing EGFP-HDQ74/rheb Mk\iRZV1d3CqYXf5JGF{e2G7 NWO4TWpOOC5{IN88US=> NWjp[|hMOjRiaB?= NXrYfYdUTE2VTx?= MVXJcoR2[2W|IHH1eI9xcGGpeR?=
COS7 cells expressing EGFP-LC3 MmXyRZV1d3CqYXf5JGF{e2G7 NGO5VncxNjJizszN NGDETYozPCCq M4\GUmROW09? M371UWlv\HWlZYOgZZV1d3CqYXf5
H4 M3;CfWZ2dmO2aX;uJGF{e2G7 MnnGNE4zKM7:TR?= MUOyOEBp NF3xeHhFVVOR M1\uXGlv[3KnYYPld{B1cGVicnH0bY8hd2ZibHnnbJQh[2ijaX6gN{B{fWK3bnn0JFIhfG9ibHnnbJQh[2ijaX6gN{B{fWK3bnn0JFEhcW5iaIXtZY4hUDRiY3XscJM>
HeLa M1zUZWZ2dmO2aX;uJGF{e2G7 MUSxNFAhdk1? M1r6OVM3KGh? Mn3WSG1UVw>? MlH2TY5lfWOnczDGVmIhUzJyOUXQMEBVOjB7OFysJHczOTBzRjDteZRidnRvdXLpdZVqfGmwQzDpcpRmemGldHnvci=>
HeLa NHn3b3BHfW6ldHnvckBCe3OjeR?= M2P2Z|ExOCCwTR?= NUnxfJl3OzZiaB?= MkXISG1UVw>? NG\USolKdmS3Y3XzJGZTSiCZMkGwNWYhdXW2YX70MZVjcXG3aYTpcmMhcW62ZYLhZ5Rqd25?
HeLa MoLRSpVv[3Srb36gRZN{[Xl? NYTy[VhUOTByIH7N Ml3nN|YhcA>? NW\zd29bTE2VTx?= MXnJcoR2[2W|IF\SRk1HU0KSIHPvcZBt\XhiaX70[ZJi[3Srb36=
SYF M1O2ZWZ2dmO2aX;uJGF{e2G7 M3PlVFExOCCwTR?= MUOyOEBp Mm\mSG1UVw>? MkiwTY5lfWOnczDGVmIuTkuEUDDjc41xdGW6IHnueIVz[WO2aX;u
SYF MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq4TZMxOTByIH7N NXPjXJRCOjRiaB?= MVTEUXNQ M1rje2lv\HWlZYOgZY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDTXWYh[2WubIO=
HEK293T M4r1V2FvfGm4aYLhcEBCe3OjeR?= MWKxJI5O Mo\yOEBl Mn;lSG1UVw>? NUjUWXdHUW6mdXPld{BidnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIGK1JJdqfGhiRVO1NEBw\iByLkGgcm0>
HEK293T NE\iem5CdnSrdnnyZYwhSXO|YYm= NIG4T2oyKG6P NELpbIE1KGR? M2LaPGROW09? MVHJcoR2[2W|IHHueIl3cXKjbDDhZ5Rqfmm2eTDh[4FqdnO2IFjJWlEhYDRid3n0bEBGSzVyIH;mJFAvOyCwTR?=
PBMC MXXGeY5kfGmxbjDBd5NigQ>? MnyzNUBvVQ>? M1fue|E1KGR? M1r5NmROW09? NEWzT2pT\WS3Y3XzJGNEWjViZHXud4l1gQ>?
PBMC NILET|FHfW6ldHnvckBCe3OjeR?= M3P4bVEhdk1? MWqxOEBl NF\2WGdFVVOR MkLhSI9meyCwb4SgZYZn\WO2IFPYR3I1KGSnboPpeJk>
HEK293 cells Mn7YT4lv[XOnIFHzd4F6 NF\XeXg2OCCwTR?= NGC1c4o1PSCvaX6= NVf4[FQ1TE2VTx?= NGXvSnVKdmirYnn0d{BuXE:UIHvpcoF{\SCjY4Tpeol1gSC5aYToJGlEPTBib3[gNE4yKG6P
Drosophila melanogaster S2 cells transfected with N-luc and C-luc NGW5R|lHfW6ldHnvckBCe3OjeR?= NFTzdVkyODBibl2= NXKzO2tVPCCq M{i1OmROW09? NXjtcmxHUW6mdXPld{BtfWOrZnXyZZNmKHC{b4TlbY4hfHKjboOtd5BtcWOrbnegbY4hTHKxc3;wbIlt[SCvZXzhco9o[XO2ZYKgV|Ih[2WubIOgeJJidnOoZXP0[YQhf2m2aDDOMYx2[yCjbnSgR{1tfWN?
Human mixed lymphocyte Ml7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\xbGlKPSCwTR?= MUjEUXNQ NFm3cW1KSzVyPUGuOkBvVS5?
Lewis rat lymph node cells MnnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnxWZZIPSEQvF2= MVzEUXNQ Mln2TWM2OD1{Lk[g{txO
cells from the thymus of normal BALB/c mice M2HKPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\IXFEyOCCwTR?= NGPOfI04OiCq M3Psc2ROW09? M4r5c2lvcGmkaYTzJIx6dXCqb4Dyc4xq\mW{YYTpc44hMEyDRjmge4l1cCCLQ{WwJI9nKDNibl2=
MRK-nu-1 NYrIZld2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7ITWM2OD1yLki0OUBxVQ>?
OCUB-M M2mwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXoWI5UUUN3ME21MlI1KHCP
SF539 NUHNS4tKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFzLk[gdG0>
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RL95-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TmZ2lEPTB;MUC3JJBO
LC-2-ad NFWyUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXFTWM2OD12MkOgdG0>
Daudi MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTR|NDDwUS=>
NTERA-S-cl-D1 NXv3blJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvlfpdpUUN3ME20OFMheE1?
OS-RC-2 NYPCRmtvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTZ3MjDwUS=>
VA-ES-BJ MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHafoJKSzVyPUeyN{BxVQ>?
GR-ST M2LYRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3wXng5UUN3ME24OFYheE1?
SW872 NGe1dmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P4UGlEPTB;OES2JJBO
NOS-1 NV3kWJdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;mWmJQUUN3ME24O|EheE1?
MC116 M4HHO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP3WVJKSzVyPUm4OUBxVQ>?
NCI-H1355 NVT5WFl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIji[41KSzVyPUGuNFEhdk1?
RPMI-8226 MlnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfrZmw2UUN3ME2xMlE6KG6P
TE-15 NGXTdGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoizTWM2OD1zLkO2JI5O
Ramos-2G6-4C10 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTFwNE[gcm0>
KU812 NGfmPGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL6Zm1KSzVyPUKuNFEhdk1?
EW-1 M120[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTJwMUegcm0>
KS-1 NXjvSHRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\nTWM2OD1{LkS1JI5O
SK-LMS-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\0TWM2OD1{LkS5JI5O
TGBC1TKB MknlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHoNZU1UUN3ME2yMlY6KG6P
TE-6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmm4TWM2OD1{Lke3JI5O
ETK-1 M2Lv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fMOGlEPTB;Mj64NkBvVQ>?
BE-13 NGTzbllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DFfmlEPTB;Mj65PUBvVQ>?
A3-KAW MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Xjd2lEPTB;Mj65PUBvVQ>?
TE-10 MmjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPwfmFKSzVyPUOuN{BvVQ>?
DOHH-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vxOWlEPTB;Mz6zOUBvVQ>?
ES6 NF\NPG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zocGlEPTB;Mz60N{BvVQ>?
OPM-2 M4jIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYe3fHlTUUN3ME20MlE2KG6P
SH-4 M4K4Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTRwM{Sgcm0>
NB13 NXrlVpQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjCUmdmUUN3ME20MlM3KG6P
HUTU-80 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTRwNEKgcm0>
CCRF-CEM NVXPd5BTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{W1TmlEPTB;ND65OEBvVQ>?
TGBC24TKB M37FfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3xN3plUUN3ME21MlUyKG6P
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J-RT3-T3-5 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnaVpFKSzVyPU[uOFYhdk1?
KALS-1 Mm\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHWfmFCUUN3ME22MlU3KG6P
no-10 NETJWHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTdwMkmgcm0>
SK-NEP-1 MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRThwN{mgcm0>
L-540 NYXHblRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPUfGxlUUN3ME2xNE41OiCwTR?=
JiyoyeP-2003 NFTaRlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHhTWM2OD1zMD65OEBvVQ>?
HH MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFzLkO5JI5O
SR M33jZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILBV2tKSzVyPUGxMlQ2KG6P
QIMR-WIL MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG5PGp1UUN3ME2xNU45PSCwTR?=
A4-Fuk MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXBbGRYUUN3ME2xN{4yOiCwTR?=
CESS MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XKW2lEPTB;MUOuNVMhdk1?
KE-37 NIqzbZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{X2RmlEPTB;MU[uNFchdk1?
SK-UT-1 NY\MS|JVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjsTpFpUUN3ME2xOk45OSCwTR?=
SIG-M5 MljIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\ueJFZUUN3ME2xO{4zPSCwTR?=
HT NGHiNZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTmZ4pKSzVyPUG3MlYhdk1?
DEL NH21V|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlK3TWM2OD1zNz65PUBvVQ>?
SK-PN-DW NET6[o9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTJyLkKzJI5O
RPMI-8402 MmLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z0SGlEPTB;MkGuO|chdk1?
RPMI-6666 M2i3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDzTWM2OD1{ND60NkBvVQ>?
NCI-H720 NUD3OoFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTJ3LkSxJI5O
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SF126 M2DC[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTNyLkO4JI5O
BC-1 NEDH[oFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTNzLkK2JI5O
MHH-PREB-1 MmnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LJVWlEPTB;M{KuOFQhdk1?
A101D NHLjUGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTN{Lk[yJI5O
NMC-G1 M3XTXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\LUlA1UUN3ME2zN{43PyCwTR?=
LB1047-RCC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO5RnAxUUN3ME2zOE43QSCwTR?=
EM-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfmTWM2OD1|OD61N{BvVQ>?
COLO-684 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDRTWM2OD1|OT64JI5O
Becker MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIH5[oVKSzVyPUSxMlA2KG6P
BL-41 NIDZT4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPFTWM2OD12Mz62OkBvVQ>?
MDA-MB-134-VI NYHmflZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGqyZ|FKSzVyPUS0MlAzKG6P
L-363 M1:1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljRTWM2OD12ND63N{BvVQ>?
ECC4 NVfBcmdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTR2Lke4JI5O
A388 NVHPblJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTR2LkiyJI5O
HEL NWfX[2dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH4eG5JUUN3ME20PU44QSCwTR?=
RKO M4DHO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTVyLkK5JI5O
KINGS-1 M2fBWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULscYtKUUN3ME21NU42PSCwTR?=
EB-3 M2qzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrvTWM2OD13Mj62O{BvVQ>?
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LB771-HNC M3nsRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\UOY8xUUN3ME2yMlkxQTR4IN88US=>
GI-ME-N MnfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIG2VWdKSzVyPUOuNFA6ODRizszN
NALM-6 NXLSdWVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NID1[o1KSzVyPUOuNFA6OzNizszN
LU-134-A M{TkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTNwMEW0NlUh|ryP
DMS-153 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm2bmRTUUN3ME2zMlA2QDJ2IN88US=>
MZ1-PC NH\HeXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TEdmlEPTB;Mz6wPVA4QCEQvF2=
NCI-H1155 NWryO3o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHRfHVsUUN3ME2zMlEyPjFizszN
CAS-1 MnHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTNwMUO3NFch|ryP
D-502MG NELSSYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTNwMUSzPUDPxE1?
NCI-H2141 NXjtT|VsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknZTWM2OD1|LkG3OFUzKM7:TR?=
NB6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTNwMUiyOVkh|ryP
NCCIT MmLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HEXmlEPTB;Mz6yNVgxQSEQvF2=
NB69 NE\jOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTNwM{G4PVEh|ryP
JVM-2 NXrMNJhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTNwM{[0N|Mh|ryP
K052 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XqOmlEPTB;Mz6zO|k3QCEQvF2=
HCC2157 Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fDb2lEPTB;Mz61N|IzQCEQvF2=
KMOE-2 NXG0cWJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M173fWlEPTB;Mz61OFI1OiEQvF2=
SF268 M1rPdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;iUWF3UUN3ME2zMlcyPTV2IN88US=>
CHP-126 NU\CNI0{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\PO2xjUUN3ME2zMlc3PDV6IN88US=>
CP66-MEL M1LDVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\NVo1iUUN3ME2zMlc6ODl2IN88US=>
NCI-H69 MkPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1y1NWlEPTB;ND6wNVk{PiEQvF2=
A253 M1OzXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHvVnV3UUN3ME20MlAzOTBzIN88US=>
NB14 NWf5dHpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHK3fVFKSzVyPUSuNVA1PzlizszN
NCI-H1694 MnjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rRe2lEPTB;ND6xN|EyOiEQvF2=
NCI-H2196 Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfoOHZKSzVyPUSuNVcyPjlizszN
TE-9 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXrTWM2OD12LkG3OVgzKM7:TR?=
D-283MED Mn\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTYTWM2OD12LkG4PFQh|ryP
OCI-AML2 MmLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDjTWM2OD12LkG5OFg6KM7:TR?=
D-263MG M1TjSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYiwbpNVUUN3ME20MlIzQTZzIN88US=>
MPP-89 NIDqfpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q5VGlEPTB;ND6yO|MxPCEQvF2=
LAMA-84 MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTRwM{C0NlEh|ryP
LB373-MEL-D NYmzb|RRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3IRnBjUUN3ME20MlM3Pzh7IN88US=>
UACC-257 M4jLXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v3UWlEPTB;ND6zPVU{PCEQvF2=
MC-CAR MmPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmf2TWM2OD12LkSzPVkh|ryP
COLO-320-HSR NUnYc2JJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jTOGlEPTB;ND60OFQzPyEQvF2=
P30-OHK M1\4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnLWWZKSzVyPUSuOlY2QDFizszN
UACC-812 NUHrbI13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;SUGlEPTB;ND62PVE3OSEQvF2=
CTB-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTRwN{G1OVUh|ryP
ALL-PO NXLYcWp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf0RVhKSzVyPUSuPFQxPzdizszN
SK-MEL-2 M3zLbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PGc2lEPTB;ND64Olk2PSEQvF2=
TC-YIK NX34O5FMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTRwOUe5OFIh|ryP
NCI-H1882 NYDsNIxwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTPTWM2OD13LkCyNFAyKM7:TR?=
MHH-CALL-2 NGPIenRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom5TWM2OD13LkC1NFQzKM7:TR?=
U-87-MG M2PtfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1v5RmlEPTB;NT6wPVQ3PiEQvF2=
NCI-H1092 Ml:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnRUo04UUN3ME21MlI3PTV3IN88US=>
TE-441-T NVrTVWRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j3VWlEPTB;NT6yO|gzKM7:TR?=
SK-MEL-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTVwMkmwOFQh|ryP
EW-22 NIXXWldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTkTWM2OD13LkK5OFY3KM7:TR?=
MZ7-mel NFfhTJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2L0WWlEPTB;NT60NFY6OSEQvF2=
LP-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTVwNEGyPVEh|ryP
NCI-SNU-16 NF\SN4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfkTWM2OD13Lk[0NFc1KM7:TR?=
LU-65 NUOySGJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2D0W2lEPTB;NT63OlM4OyEQvF2=
CW-2 M3XoTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe5e|M5UUN3ME21Mlg2QTV7IN88US=>
WSU-NHL NYHncnZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;3VmlEPTB;NT65OVE4PCEQvF2=
IST-MES1 M2\nTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTZfnRLUUN3ME21Mlk2PDR|IN88US=>
U-266 M1XJbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTVwOUiyNFIh|ryP
TALL-1 MkW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPhcmZKSzVyPU[uNVQ3QDhizszN
Calu-6 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnT2TWM2OD14LkG1N|E3KM7:TR?=
MMAC-SF M1\iW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPERlE3UUN3ME22MlE5PTV4IN88US=>
NCI-H82 MnO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTZwMkC0PFkh|ryP
RS4-11 NUniPVJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ri[GlEPTB;Nj6yOVg6PyEQvF2=
SNU-C2B NEnWS45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1i2VGlEPTB;Nj60NFk3QSEQvF2=
BOKU MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfJTWM2OD14LkS3OVk4KM7:TR?=
C8166 Mo\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT4flhvUUN3ME22MlU2QTF{IN88US=>
D-247MG MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTdwMESzOFch|ryP
EW-18 NIDXT4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv3R4hFUUN3ME23MlA4Ojl{IN88US=>
KG-1 NHfje29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTdwNkK3N|gh|ryP
REH M4nYWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTdwNkixNFkh|ryP
U-698-M MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf6bmxKSzVyPUeuPFQ{OTVizszN
KP-N-RT-BM-1 M{HmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTdwOUOwNlkh|ryP
MS-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTdwOU[wOFEh|ryP
SNU-C1 MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnud3pCUUN3ME23Mlk5OTl{IN88US=>
SK-MM-2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzY[5JKSzVyPUiuNlYxPjVizszN
LAN-6 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jDNmlEPTB;OD6zNFAxOSEQvF2=
NEC8 NIm4SFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLiXIIxUUN3ME24MlMxPjlzIN88US=>
NCI-H1770 MnvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLqXXFKSzVyPUiuN|gxODJizszN
D-336MG Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjrcZd[UUN3ME24MlQxOTF4IN88US=>
COLO-829 NX\BbY5HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\ZU5lKSzVyPUiuOFg5PzlizszN
LS-513 NXzrbHc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofnTWM2OD16LkW5OVk6KM7:TR?=
YT MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmX2TWM2OD16Lk[yOFI4KM7:TR?=
EW-24 NXG2WmhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXNTWM2OD16Lke2OVQh|ryP
IST-SL1 Mmn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRThwOE[1OFMh|ryP
CA46 NFLnPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnpcIhRUUN3ME24Mlk2ODl6IN88US=>
NCI-H1838 NXTOeWVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRThwOUi2NFIh|ryP
NCI-H719 NYj4e5RET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTidWpKSzVyPUmuNlUzPzlizszN
HCE-T NGCwd5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTlwM{C4OVEh|ryP
A498 M1\E[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PvbGlEPTB;OT6zOlEzPCEQvF2=
LB831-BLC M4\ST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTTcJNFUUN3ME25Mlc3PTJzIN88US=>
SKM-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D1NGlEPTB;OT64OVk3OyEQvF2=
THP-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2H5fGlEPTB;OT65OlkyQCEQvF2=
SHP-77 Mn74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTFyLkSwO{DPxE1?
EW-3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFyLk[yPFkh|ryP
KY821 M4nUb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFyLke2N{DPxE1?
NCI-SNU-1 NYDmb5A4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofmTWM2OD1zMT6wNlE4KM7:TR?=
HCC2218 M3L3Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7WW4FKSzVyPUGxMlM6QDZizszN
IM-9 NYLVTFlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTFzLkWxNFYh|ryP
NCI-H889 MmDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFzLkWzNVMh|ryP
HDLM-2 MoLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TTeWlEPTB;MUKuOFE2QSEQvF2=
LB2518-MEL MnTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTF{Lk[4NVUh|ryP
NCI-H23 MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF|LkK0NlUh|ryP
NB17 M2HaRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPpR|ZKSzVyPUGzMlQ2PzlizszN
NCI-H322M M3rNdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTF2LkSwOlgh|ryP
SUP-T1 NF\Md3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;1fZlGUUN3ME2xOE41OTNizszN
ES3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnMbYxOUUN3ME2xOU4xPzB|IN88US=>
ES5 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITUe45KSzVyPUG1MlA4QDdizszN
NCI-H1650 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLFWXhKSzVyPUG1MlQ6PzlizszN
NCI-H226 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjYTWM2OD1zNT64O|Y5KM7:TR?=
COR-L88 Ml;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TXc2lEPTB;MU[uN|E1KM7:TR?=
SCC-15 MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHZTWM2OD1zNj6zPFY6KM7:TR?=
GOTO MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nvWWlEPTB;MU[uOFc6OyEQvF2=
SIMA NXfjRpo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nCT2lEPTB;MU[uOFgxOiEQvF2=
NCI-H1299 MnHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTlfItKSzVyPUG3MlE2QTFizszN
NCI-H1581 M2G0[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTF5LkSyNVkh|ryP
MHH-NB-11 M4TaNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTF5Lkm2PFMh|ryP
MFM-223 MkHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf2NmpKSzVyPUG4MlA2OzhizszN
ES7 MoX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{eybWlEPTB;MUiuOVQ{OSEQvF2=
JVM-3 NGeyOo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHSOWlsUUN3ME2xPE44OTdizszN
RL M2j2[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYT0SZZJUUN3ME2yNE4{QDhizszN
EC-GI-10 NGLO[WpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzVTWM2OD1{MT6yNFQyKM7:TR?=
LNCaP-Clone-FGC NFPCdpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJzLk[3Olgh|ryP
IMR-5 M3z2PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\veYRKSzVyPUKxMlg1QTRizszN
KP-N-YS MoGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTJzLki3OUDPxE1?
Mo-T NWrwRVg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;aOFlKSzVyPUKyMlIyQDVizszN
NCI-H128 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPwXHNDUUN3ME2yN{42QDV|IN88US=>
RH-1 MlPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXm3WJlJUUN3ME2yN{44QDZ4IN88US=>
NCI-H2171 NGG2XoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\ye2lEPTB;MkSuNlQ5PSEQvF2=
RPMI-8866 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHLTmJLUUN3ME2yOk44PDJizszN
SK-N-FI MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTJ5LkO4NVEh|ryP
LOXIMVI M4XvUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTJ5LkiwOVEh|ryP
P31-FUJ MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPicZpKSzVyPUOxMlU{PzRizszN
KMS-12-PE NHrlNHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DD[GlEPTB;NEmuOVMxOiEQvF2=

... Click to View More Cell Line Experimental Data

In vivo試験 Treatment with Rapamycin in vivo specifically blocks targets known to be downstream of mTOR such as the phosphorylation and activation of p70S6K and the release of inhibition of eIF4E by PHAS-1/4E-BP1, leading to complete blockage of the hypertrophic increases in plantaris muscle weight and fibre size. [4] Short-term Rapamycin treatment, even at the lowest dose of 0.16 mg/kg, produces profound inhibition of p70S6K activity, which correlates with increased tumor cell death and necrosis of the Eker renal tumors. [5] Rapamycin inhibits metastatic tumor growth and angiogenesis in CT-26 xenograft models by reducing the production of VEGF and blockage of VEGF-induced endothelial cell signaling. [6] Rapamycin treatment at 4 mg/kg/day significantly reduces tumor growth of C6 xenografts, and tumor vascular permeability. [7]
臨床試験 A Phase II study of Rapamycin to erase angiofibromas in patients with Tuberous Sclerosis Complex (TSC) is currently ongoing.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

Immunoblotting for the mTOR kinase assay HEK293 cells are plated at 2-2.5×105 cells/well of a 12-well plate and serum-starved for 24 hours in DMEM. Cells are treated with increasing concentrations of Rapamycin (0.05-50 nM) for 15 minutes at 37 °C. Serum is added to a final concentration of 20% for 30 minutes at 37 °C. Cells are lysed, and cell lysates are separated by SDS-PAGE. Resolved proteins are transferred to a polyvinylidene difluoride membrane and immunoblotted with a phosphospecific primary antibody against Thr-389 of p70 S6 kinase. Data are analyzed using ImageQuant and KaleidaGr

細胞アッセイ:

[3]

細胞株 U87-MG, T98G, and U373-MG
濃度 Dissolved in DMSO, final concentrations ~25 μM
反応時間 72 hours
実験の流れ

Cells are exposed to various concentrations of Rapamycin for 72 hours. For the assessment of cell viability, cells are collected by trypsinization, stained with trypan blue, and the viable cells in each well are counted. For the determination of cell cycle, cells are trypsinized, fixed with 70% ethanol, and stained with propidium iodide using a flow cytometry reagent set. Samples are analyzed for DNA content using a FACScan flow cytometer and CellQuest software. For apoptosis detection, cells are stained with the terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) technique using an ApopTag apoptosis detection kit. To detect the development of acidic vesicular organelles (AVO), cells are stained with acridine orange (1 μg/mL) for 15 minutes, and examined under a fluorescence microscope. To quantify the development of AVOs, cells are stained with acridine orange (1 μg/mL) for 15 minutes, removed from the plate with trypsin-EDTA, and analyzed using the FACScan flow cytometer and CellQuest software. To analyze the autophagic process, cells are incubated for 10 minutes with 0.05 mM monodansylcadaverine at 37 °C and are then observed under a fluorescence microscope.

動物実験:

[7]

動物モデル Athymic Nu/Nu mice inoculated subcutaneously with VEGF-A-expressing C6 rat glioma cells
製剤 Dissolved in solvent solution (0.2% carboxymethylcellulose and 0.25% Tween-80 in sterile H2O)
投薬量 ~4 mg/kg/day
投与方法 Injection i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Rapamycin (Sirolimus) SDF
分子量 914.18
化学式

C51H79NO13

CAS No. 53123-88-9
保管 2年-20℃
6月-80℃in solvent
別名 AY 22989,NSC-2260804
溶解度 (25°C) * In vitro DMSO 20 mg/mL (21.87 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 0.5% CMC/0.25% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone

カスタマーフィードバック (12)


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Source Nat Genet, 2014, 46(4), 364-70. Rapamycin (Sirolimus) purchased from Selleck
Method Western blot
Cell Lines Persister cells
Concentrations 10 nM
Incubation Time 3 days
Results While added with a specific mTOR inhibitor, rapamycin(Rapa), it inhibitied endogenous mTOR activity, showed that markedly reduced MYC protein levels in persister cells but not in naive T-ALL cells.

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Source Cancer Cell, 2011, 19(6), 792-804. Rapamycin (Sirolimus) purchased from Selleck
Method Cell viability Analysis
Cell Lines Ar+murine (CaP8) and human (LNCaP) prostate cancer cells, Pb-Cre+;PtenL/L mice, Pb-Cre+;PtenL/L;ArL/Y mice
Concentrations 1 nM, 4 mg/kg
Incubation Time 0-4 weeks
Results These data suggest that CaPs with AR loss have greater reliance upon the PI3K/AKT/mTOR-signaling pathways and that combined AR/androgen blockage in conjunction with PI3K/AKT/mTOR inhibition (by Rapamycin) is more effective for CaPs initiated by PTEN loss or PI3K/AKT activation.

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Source Cell Res, 2012, 22(6), 1003-21. Rapamycin (Sirolimus) purchased from Selleck
Method EdU labeling
Cell Lines MCF-7 cells
Concentrations 150 nM
Incubation Time 48 h
Results The punctate structures from SRC-3 or MIF knockdown cells are very similar to that found in cells treated with rapamycin, a known inducer of autophagy.

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Source Autophagy, 2015, 11(4), 617-28. Rapamycin (Sirolimus) purchased from Selleck
Method Cell imaging
Cell Lines H4-LC3-GFP cells
Concentrations 200 nM
Incubation Time 24 h
Results Consistent with inhibition of autophagy, the levels of LC3-II were lower and the levels of SQSTM1/p62 were higher in this USP18 knockdown cell line compared to that of control under basal conditions as well as the induced condition after the treatment with rapamycin.

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Source Cell Rep, 2015, 10.1016/j.celrep.2015.01.014. Rapamycin (Sirolimus) purchased from Selleck
Method Western blotting
Cell Lines HEK293 cells
Concentrations 250 nM
Incubation Time 24 h
Results Rapamycin virtually abolishes stimulation by Rheb of phospho-S6 kinase and phospho-4EBP1 but has negligible effects on phospho-eIF2a (A). In contrast to phosphorylation of eIF2a, which is not mediated by mTORC1, phosphorylation of other elongation factors does involve mTORC1. Thus, rapamycin prevents phosphorylation of eIF4G and eIF4B, targets of S6K, but not eIF2a (B). By contrast, rapamycin, as expected, abolishes phospho-S6 kinase but fails to influence phospho-eIF2a, phospho-Erk or phospho-Akt (C).

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Source Biochem Pharmacol, 2015, 95(3), 156-69. Rapamycin (Sirolimus) purchased from Selleck
Method Immunofluorescence
Cell Lines RAW264.7 cells
Concentrations 10 uM
Incubation Time 16 h
Results It has been reported that autophagy can directly regulate inflammatory responses. To confirm this phenomenon, we pre-treated RAW264.7 cells with 3-MA (an autophagy inhibitor by blocking the class III PI3Ks) or rapamycin (an autophagy inducer by targeting the negative regulators against autophagy as mammalian target of rapamycin (mTOR)), followed by addition of LPS. LPS-induced punctate LC3 was markedly reduced and enhanced in the presence of 3-MA and rapamycin, respectively.

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Source Biochem Pharmacol , 2011, 82, 216-226. Rapamycin (Sirolimus) purchased from Selleck
Method Western blot
Cell Lines H1299 cells
Concentrations 2 μM
Incubation Time 48 h
Results RAD001 and other mTOR inhibitors decreased the levels of survivin protein, as assessed by Western blot analysis, without affecting the levels of other IAP members. In addition, combined treatment with sorafenib and mTOR inhibitor Rapamycin and RAD001 decreased survivin expression to a greater extent than treatment with either alone.

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Source J Lipid Res, 2011, 52, 1617-1625. Rapamycin (Sirolimus) purchased from Selleck
Method Histological analysis, immunohistochemistry, Liver triglyceride content analysis, real-time PCR
Cell Lines Male SD rats
Concentrations
Incubation Time 7 d
Results To determine the effect of rapamycin, an mTOR inhibitor, in the OA-induced fatty liver, rats were fed 1% OA and administered rapamycin for seven days. OA-induced lipid accumulation was completely inhibited by the treatment with rapamycin (Fig. A). HE and Oil Red O staining of liver sections clearly confi rmed the results (Fig. B). Immunohistochemistry analyses showed signifi cantly repressed SREBP-1 in the rapamycin-cotreatment liver ( Fig. B ). All the downstream effectors of SREBP-1, such as Lxr-α, Acc, Scd-1 and Fas, were consistently suppressed by rapamycin ( Fig. C ).

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Source Biochim Biophys Acta, 2013, 1833(3), 652-62. Rapamycin (Sirolimus) purchased from Selleck
Method Measurement of cytosolic free Ca2+concentration ([Ca2+]c )
Cell Lines Human platelets
Concentrations 500 nM
Incubation Time 30 min
Results Rapamycin administration significantly reduced TG-evoked Ca2+ -entry by 19. 5 ?9.4 %.

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Source Tuberc Respir Dis, 2013, 75(1), 9-17. Rapamycin (Sirolimus) purchased from Selleck
Method Microscope imaging
Cell Lines NCI-H1299 cells
Concentrations 10 uM
Incubation Time 48 h
Results Growth inhibition induced by rapamycin or erlotinib is enhanced by combination treatment with monensin in NCI-H1299 cells.

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Source 2011, Dr.Ulrich Bommer of University of Wollongong. Rapamycin (Sirolimus) purchased from Selleck
Method Western blot
Cell Lines
Concentrations
Incubation Time 0-6 h
Results Rapamycin inhibits growth-dependent TCTP induction.

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Source 2013, Dr. Zhang of Tianjin Medical University. Rapamycin (Sirolimus) purchased from Selleck
Method Western Blot
Cell Lines HeLa cells
Concentrations 0/2/20/200 nM
Incubation Time 24 h
Results

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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