Rapamycin (Sirolimus)

Licensed by Pfizer Catalog No.S1039 Synonyms: AY 22989,NSC-2260804

Rapamycin (Sirolimus) Chemical Structure

Molecular Weight(MW): 914.18

Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

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Cited by 64 Publications

13 Customer Reviews

  • Protein blots showing MYC expression in naive and persister cells after 3 d of treatment with 2 uM AKT inhibitor MK-2206 (AKTi) or 10 nM mTOR inhibitor rapamycin (Rapa).

    Nat Genet 2014 46(4), 364-70. Rapamycin (Sirolimus) purchased from Selleck.

    Cooperative Effects of AR and mTOR Inhibition In Vitro and In Vivo (A) In vitro response of Pten null;Ar+ murine (CaP8) and human (LNCaP) prostate cancer cells to AR knockdown (sh-AR) or pharmacological inhibition of AR (MDV3100, 10 nM) with and without rapamycin (R: 1 nM) treatment (Sc, control sh oligo). (B and D) In vivo response to treatments with castration, MDV3100, rapamycin, or their combinations as measured by cell proliferation (Ki67+cells) and (C and D) tumor burden in Pb-Cre+;-PtenL/L and Pb-Cre+;PtenL/L:ArL/Y mutants. Scale bars represent 2 mm (C), 200 mm (D), and 75 mm (D, inset). Error bars represent mean ±SD.

    Cancer Cell 2011 19(6), 792-804. Rapamycin (Sirolimus) purchased from Selleck.

  • 48 hours after addition of rapamycin(150 nM), the cells were imaged as described in Figure A to detect formation of punctuated GFP-LC3 structure. Quantification represented the ratio of GFP-LC3 punctuated positive cell to the total cell counted(Figure B).

    Cell Res 2012 22(6), 1003-21. Rapamycin (Sirolimus) purchased from Selleck.

    H4-LC3-GFP cells were treated with 1 nM IFNA2 for the indicated periods in the presence of 200 nM rapamycin. Images of the cells were collected using an ArrayScan HCS 4.0 Reader. Representative cells are shown. The average spot intensity in 500 cells from each indicated sample was determined. Data are displayed as means ?SD of the spot intensity per cell (below). RLU, relative leight unit.

    Autophagy 2015 11(4), 617-28. Rapamycin (Sirolimus) purchased from Selleck.

  • Rheb Induces Phospho-eIF2a Independent of mTORC1 and Promotes Phospho-eIF2a Predominantly through PERK (A) Western blotting of indicated proteins of HEK293 expressing cDNAs of myc (control) or myc-Rheb WT were grown in DMEM with serum (+) or without serum (-) or pretreated with the inhibitors rapamycin (250 nM) or DMSO (0.5%, control). (B) Western blotting of indicated proteins in HEK293 cells expressing myc or myc-Rheb and pretreated with rapamycin or DMSO as in (A). (C) Western blotting of indicated proteins in HEK293 cells expressing myc or myc-Rheb and pretreated with inhibitors of MAPK (PD98059, 50 mM) or PI3K (wortmannin, 100 nM), rapamycin, or DMSO.

    Cell Rep 2015 10.1016/j.celrep.2015.01.014. Rapamycin (Sirolimus) purchased from Selleck.

    Cells were cultured with the indicated concentrations of PLS-123, rapamycin (Granta519 0.002 μM, Mino 0.001 μM, Z138 0.005 μM), and their combination for 48 h. The results are expressed as the mean of relative activity and S.D. from triplicate cultures. The results are representative of at least three similar experiments.

    Int J Cancer, 2018, 142(1):202-213. Rapamycin (Sirolimus) purchased from Selleck.

  • Autophagy induced by PL-0N and PL may restrict LPS-induced inflammatory responses in RAW264.7 cells. LPS induced autophagy in RAW264.7 cells. Cells were incubated with 1 mM 3-MA or 10 uM Rapamycin in the absence or presence of LPS (1 ug/mL) for 16 h. Then immunofluorescence for LC3 was visualized using a Zeiss LSM 710 confocal microscope.

    Biochem Pharmacol 2015 95(3), 156-69. Rapamycin (Sirolimus) purchased from Selleck.

    Inhibition of mTOR activity may be responsible for sorafenib-induced down-regulation of survivin. H1299 cells were treated with the indicated concentration of RAD001 or Rapamycin for 48 h. Then H1299 cells were incubated with or without 5 μM sorafenib, with or without 5 μM RAD001, and with or without 2 μM rapamycin for 48 h.  The indicated protein levels were determined by Western blot analysis. β-Actin protein levels were measured as loading controls.

     

     

    Biochem Pharmacol 2011 82, 216-226. Rapamycin (Sirolimus) purchased from Selleck.

  • Rapamycin (RPM) inhibits OA-induced lipogenesis. Male SD rats were divided into three groups, and then treated as follows for seven days: group I (control; Ctrl), normal diet + vehicle; group II (OA), 1% OA diet + vehicle; group III (OA + RPM), 1% OA diet + RPM. (A) Hepatic TG concentrations were determined using the serum triglyceride determination kit. (B) Fixed liver sections were subjected to HE and Oil Red O staining as well as immunohistochemistry assays with SREBP-1 antibody. Representative microphotographs of liver specimens from all groups of rats are shown. (C) The levels of mRNA of the indicated genes involved in lipogenesis were determined by real-time PCR. Each bar represents the mean ±SE of the results obtained from six rats. * P < 0.05, ** P < 0.01, *** P < 0.001.

    J Lipid Res 2011 52, 1617-1625. Rapamycin (Sirolimus) purchased from Selleck.

    Immunophilins participate in SOCE activation by CN-dependent but also CN-independent signaling pathways. Fura-2 loaded platelets were suspended in HBS and subsequently incubated at 37oC for 30 min with rapamycin (500 nM). Once incubation time was over, platelets were stimulated with TG (200 nM) in a calcium free-HBS (EGTA 100 μM was added as indicated the by arrowhead) and 4 min later CaCl2 (300 µM) was added to visualized calcium entry. Changes in fura-2 fluorescence were monitored using the 340/380nm ratio and calibrated in terms of [Ca2+]c . Traces are representative of four to six independent experiments. *,**, *** represents p < 0.05, p < 0.01 and p <0.001, respect control platelets.

    Biochim Biophys Acta 2013 1833(3), 652-62. Rapamycin (Sirolimus) purchased from Selleck.

  • Tuberc Respir Dis 2013 75(1), 9-17. Rapamycin (Sirolimus) purchased from Selleck.

    2013 Dr. Zhang of Tianjin Medical University. Rapamycin (Sirolimus) purchased from Selleck.

  • Rapamycin inhibits growth-dependent TCTP induction. Cells were serum-starved for 24h and restimulated with 20% FBS for the indicated times in the presence or absence of rapamycin. The graph shows the relative TCTP signal, corrected for the loading control.

    2011 Dr.Ulrich Bommer of University of Wollongong. Rapamycin (Sirolimus) purchased from Selleck.

Purity & Quality Control

Choose Selective mTOR Inhibitors

Biological Activity

Description Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.
Targets
mTOR [1]
(HEK293 cells)
~0.1 nM
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 NWTLS|c3S3m2b4TvfIlkKEG|c3H5 M4G3Z|ExKG6P MYq3NkBp MVzEUXNQ Ml\lVI91\W62aXH0[ZMh[2GvcITveIhm[2mwLXnu[JVk\WRiY4n0c5RwgGmlaYT5 NUTjbmdQOjR7MEC4O|M>
HT-29 M1jmVGN6fG:2b4jpZ{BCe3OjeR?= M1XubVExKG6P NFWwRpY4OiCq NI\lV|JFVVOR NHjFSYNRd3SnboTpZZRmeyCmaXfpeI95cW5vaX7keYNm\CCleYTveI95cWOrdIm= M4\XRVI1QTByOEez
HT-29 NEDE[2dEgXSxdH;4bYMhSXO|YYm= NGPvbnYyOCCwTR?= M1TvWVczKGh? MW\EUXNQ NVzHW45FWG:2ZX70bYF1\XNiNT3mcJVwem:3cnHjbYwucW6mdXPl[EBkgXSxdH;4bYNqfHl? NHnsfHMzPDlyMEi3Ny=>
PC3 NETCe5lMcW6jc3WgRZN{[Xl? MUCxNFAhdk1? M{\NW|EhcA>? NGjVT|BFVVOR Mn\UVI91\W62bImgbY5pcWKrdIOgcXRQWi2vZXTpZZRm\CCVNjDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFwyOCCwTT6= NHv0RoozOTl5OE[4Ny=>
PC3 M3LoR2tqdmG|ZTDBd5NigQ>? M3rhfVExOCCwTR?= MmjsNUBp M4DPbWROW09? NUjjbXhTTG:nczDuc5QhcW6qaXLpeEBuXE:ULX3l[IlifGWmIFHreEBxcG:|cHjvdplt[XSrb36= MWWyNVk4QDZ6Mx?=
PC3 NWTMfmJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;afoEyNjVizszN MY[xJIg> NUPtVnpDTE2VTx?= MXXJcoR2[2W|IHHueIlxem:uaX\ldoF1cX[nIHHjeIl3cXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KHerdHigTWM2OCCxZjC8NVAhdk1? Ml3TNlE6Pzh4OEO=
HEK293 MofYSpVv[3Srb36gRZN{[Xl? NWK5ellYOTByIH7N M1XiOVghcA>? NHLrcldFVVOR NULpdY5mUW6qaXLpeJMhXFCDLXnu[JVk\WRiZHXndoFl[XSrb36gc4YhWGSlZESge4l1cCCHQ{WwJI9nKDVyIH7N NWHoWno4OjF3M{mzNFE>
BT-20 NIDOfJRMcW6jc3WgRZN{[Xl? NFLrSYYzOCEQvF2= M3[1NmROW09? NUWwPYc1TG:nczDuc5QhcW6qaXLpeEBuXE:UQ{Kg[IVx\W6mZX70JJBCc1RiU{S3N{BxcG:|cHjvdplt[XSrb36= MYSyNVM2OzV3MR?=
U937 MVXBcpRq[mGldHXybYFtKEG|c3H5 MnTUOVAh|ryP NFfOWlc1QCCq MW\EUXNQ M4S3c2lv\HWlZYOgZY51cWKjY4TldolidCCjY4Tpeol1gSCjZ3HpcpN1KHerbHSgeJlx\SCOZXfpc45mdGyjIIDu[ZVud3CqaXzhJHBpcWyjZHXsdIhq[S1zIFrSN|IhcW5iVUmzO{Bk\Wyucx?= NGDlNlIzOTF2MkGwOi=>
U937 MUPBcpRq[mGldHXybYFtKEG|c3H5 MoTKOVAh|ryP NIm1e3U1QCCq NVXsPYtQTE2VTx?= MYjEc4V{KG6xdDDpcoR2[2ViYX70bYJi[3SncnnhcEBi[3Srdnn0fUBi\2GrboP0JG1KWCCycn;0[YlvNWSnZnnjbYVvfCCOZXfpc45mdGyjIIDu[ZVud3CqaXzhJGpTOzJvMjDpckBWQTN5IHPlcIx{ MXmyNVE1OjFyNh?=
U937 MWrBcpRq[mGldHXybYFtKEG|c3H5 MVy1NEDPxE1? MX60PEBp M{\QT2ROW09? M2rOZ2Rw\XNibn;0JIlv\HWlZTDhcpRq[mGldHXybYFtKGGldHn2bZR6KGGpYXnud5QhTXOlaHXybYNpcWFiY3;sbUBJSjFyMTDpckBWQTN5IHPlcIx{ MmfnNlEyPDJzME[=
MCF-7 MojIRZV1d3CqYXf5JGF{e2G7 MmrJN|Ahdk1? NIPlOGg1KGh? MYXEUXNQ MVfJcoR2[2W|IHH1eI9xcGGpeR?= NH7JbmMzODB{OEGzOC=>
U87MG NEP3d4lMcW6jc3WgRZN{[Xl? MUKxJO69VQ>? NFLNO283KGh? NXTLTVY6TE2VTx?= M3H0bnBwfGWwdHz5JIlvcGmkaYTzJI1VV1JvbXXkbYF1\WRiU{[gdIhwe3Cqb4L5cIF1cW:w MVuxPVg1QDRyNB?=
U87MG NX3ZeGdNU2mwYYPlJGF{e2G7 NITZdmwyKM7:TR?= NWfhOZhqPiCq MWjEUXNQ Mn;zVI91\W62bImgbY5pcWKrdIOgOGVDWDFqVEewLUBxcG:|cHjvdplt[XSrb36= NIm5UmcyQTh2OESwOC=>
U87MG MoDKT4lv[XOnIFHzd4F6 M2PybFEh|ryP MUG2JIg> MW\EUXNQ MUTEc4V{KG6xdDDpcohq[mm2IH3UU3IudWWmaXH0[YQhSWu2IIDoc5NxcG:{eXzheIlwdg>? MVOxPVg1QDRyNB?=
U87MG MVzLbY5ie2ViQYPzZZk> M1m3TFEh|ryP NHjIU3o3KGh? MX3EUXNQ NIq0S45Fd2W|IH7veEBqdmirYnn0JHAuPEWEUEGoWFM4NzR4KTDwbI9{eGixconsZZRqd25? M1HsNVE6QDR6NEC0
COS7 cells expressing EGFP-HDQ74/rheb M1vsT2F2fG:yaHHnfUBCe3OjeR?= NXzXUYdxOC5{IN88US=> M1vVS|I1KGh? MlSySG1UVw>? MUfJcoR2[2W|IHH1eI9xcGGpeR?= NX\5Rm01OTh|OUG5OFk>
COS7 cells expressing EGFP-LC3 NVW3Z4x[SXW2b4DoZYd6KEG|c3H5 NI\XNVAxNjJizszN NYjnTmNKOjRiaB?= NFXPZXpFVVOR MoXQTY5lfWOnczDheZRweGijZ4m= NVX6Vo9xOTh|OUG5OFk>
H4 M{XsPWZ2dmO2aX;uJGF{e2G7 Ml61NE4zKM7:TR?= NEXXV2IzPCCq M1fV[mROW09? NF[1fVBKdmO{ZXHz[ZMhfGinIILheIlwKG:oIHzp[4h1KGOqYXnuJFMhe3WkdX7peEAzKHSxIHzp[4h1KGOqYXnuJFMhe3WkdX7peEAyKGmwIHj1cYFvKEh2IHPlcIx{ NGnvSokyQDB{NEW4OC=>
HeLa NFjKZnhHfW6ldHnvckBCe3OjeR?= MnTENVAxKG6P M3XrdFM3KGh? NFTBXGNFVVOR M1uybmlv\HWlZYOgSnJDKEt{MEm1VEwhXDJyOUjMMEBYOjFyMV[gcZV1[W62LYXibZF2cXSrblOgbY51\XKjY4Tpc44> NHPyPZkyPzV4M{O4OS=>
HeLa NWi3OnQ1TnWwY4Tpc44hSXO|YYm= NInyW3AyODBibl2= MV6zOkBp NUHxW41HTE2VTx?= MkDtTY5lfWOnczDGVmIhXzJzMEHGJI12fGGwdD31ZolyfWm2aX7DJIlvfGW{YXP0bY9v NWq0UoF1OTd3NkOzPFU>
HeLa NXjncFJ6TnWwY4Tpc44hSXO|YYm= M3jO[FExOCCwTR?= MXmzOkBp NIrMdVlFVVOR MojkTY5lfWOnczDGVmIuTkuEUDDjc41xdGW6IHnueIVz[WO2aX;u MXWxO|U3OzN6NR?=
SYF MUfGeY5kfGmxbjDBd5NigQ>? NYXJOoN3OTByIH7N MXqyOEBp NV[2XHFJTE2VTx?= NILveWRKdmS3Y3XzJGZTSi2IS1LQJINwdXCuZYigbY51\XKjY4Tpc44> M4ezTFE4PTZ|M{i1
SYF MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXlOGdMOTByIH7N NVGwU3d[OjRiaB?= M3LsdmROW09? MXrJcoR2[2W|IHHueIlxem:uaX\ldoF1cX[nIHHjeIl3cXS7IHHnZYlve3RiU2nGJINmdGy| MX2xO|U3OzN6NR?=
HEK293T MY\BcpRqfmm{YXygRZN{[Xl? NVTPVY9lOSCwTR?= Ml7rOEBl NV\3SFNFTE2VTx?= NUTnboxOUW6mdXPld{BidnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIGK1JJdqfGhiRVO1NEBw\iByLkGgcm0> NFv6UlYyPzR6NUWwNS=>
HEK293T NHG2ZolCdnSrdnnyZYwhSXO|YYm= MmC4NUBvVQ>? M4DrWlQh\A>? MoXxSG1UVw>? NHrKSoZKdmS3Y3XzJIFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiWESge4l1cCCHQ{WwJI9nKDBwMzDuUS=> NIS4doUyPzR6NUWwNS=>
PBMC MnTKSpVv[3Srb36gRZN{[Xl? MmjONUBvVQ>? NWrjT4ZyOTRiZB?= MkPlSG1UVw>? MnjxVoVlfWOnczDDR3I2KGSnboPpeJk> M4TDVVE4PDh3NUCx
PBMC NWXSdodbTnWwY4Tpc44hSXO|YYm= Ml\KNUBvVQ>? MXKxOEBl M4\1eWROW09? NVfBR3p6TG:nczDuc5Qh[W[oZXP0JGNZS1J2IHTlcpNqfHl? NVHvOm1OOTd2OEW1NFE>
HEK293 cells Mnz1T4lv[XOnIFHzd4F6 M4Czd|UxKG6P NYTNUGRMPDVibXnu M4\5dWROW09? NEPjd2VKdmirYnn0d{BuXE:UIHvpcoF{\SCjY4Tpeol1gSC5aYToJGlEPTBib3[gNE4yKG6P M331e|E4OzVyOUWz
Drosophila melanogaster S2 cells transfected with N-luc and C-luc M{fnfGZ2dmO2aX;uJGF{e2G7 MmrFNVAxKG6P MUe0JIg> M3;j[2ROW09? NGP5XWRKdmS3Y3XzJIx2[2moZYLhd4UheHKxdHXpckB1emGwcz3zdIxq[2mwZzDpckBFem:|b4DobYxiKG2nbHHuc4die3SncjDTNkBk\WyuczD0doFve2[nY4Tl[EB4cXSqIF6tcJVkKGGwZDDDMYx2[w>? MlX4NVcyOjh{NkK=
Human mixed lymphocyte NEjBRpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvWOUBvVQ>? NWLSfVE6TE2VTx?= NEDsRXlKSzVyPUGuOkBvVS5? M3zCNVE3OTh3OE[1
Lewis rat lymph node cells MkO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS1JO69VQ>? MmHSSG1UVw>? M3TpbmlEPTB;Mj62JO69VQ>? NGnKRZIyPjF6NUi2OS=>
cells from the thymus of normal BALB/c mice NIDpdnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWxNEBvVQ>? NIrEfFM4OiCq M2TlXWROW09? M1rOeGlvcGmkaYTzJIx6dXCqb4Dyc4xq\mW{YYTpc44hMEyDRjmge4l1cCCLQ{WwJI9nKDNibl2= M4S5T|ExODJzOUS4
MRK-nu-1 M1G0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwOES1JJBO MmXhV2FPT0WU
OCUB-M NInkTmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTVwMkSgdG0> M{j5bnNCVkeHUh?=
SF539 M2DCd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDl[4FKSzVyPUGxMlYheE1? NUnTUWF5W0GQR1XS
ES4 NIe0NJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTJzLkWgdG0> MX3TRW5ITVJ?
RL95-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zhU2lEPTB;MUC3JJBO MnLwV2FPT0WU
LC-2-ad MkHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37PdWlEPTB;NEKzJJBO MknFV2FPT0WU
Daudi M2\nVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrnTWM2OD12M{SgdG0> NInCWmtUSU6JRWK=
NTERA-S-cl-D1 NVq4cmV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTR2MzDwUS=> NE\2NoNUSU6JRWK=
OS-RC-2 NUXJcXBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln5TWM2OD14NUKgdG0> Mlf3V2FPT0WU
VA-ES-BJ MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;PTWM2OD15MkOgdG0> NXOwXG9wW0GQR1XS
GR-ST M4nnSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTh2NjDwUS=> M{n1V3NCVkeHUh?=
SW872 MlW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTh2NjDwUS=> MXPTRW5ITVJ?
NOS-1 NFzQdYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTh5MTDwUS=> NYfzbHA1W0GQR1XS
MC116 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7qTWM2OD17OEWgdG0> NGTuXm9USU6JRWK=
NCI-H1355 NWPudpA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTFwMEGgcm0> M{i2cnNCVkeHUh?=
RPMI-8226 M1\2Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorGTWM2OD1zLkG5JI5O MVnTRW5ITVJ?
TE-15 NGXxPIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEmybXFKSzVyPUGuN|Yhdk1? M1LKNHNCVkeHUh?=
Ramos-2G6-4C10 NUHlTnZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrURW1KSzVyPUGuOFYhdk1? MlrVV2FPT0WU
KU812 NWfa[2hHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXu0co5iUUN3ME2yMlAyKG6P MVjTRW5ITVJ?
EW-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH32RXJKSzVyPUKuNVchdk1? NUjaUYJDW0GQR1XS
KS-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv1[W1KSzVyPUKuOFUhdk1? NGDEbGJUSU6JRWK=
SK-LMS-1 M2XqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLROJVKSzVyPUKuOFkhdk1? NH73SGtUSU6JRWK=
TGBC1TKB NUKzfG57T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;PXGlEPTB;Mj62PUBvVQ>? NHLVRmVUSU6JRWK=
TE-6 M2PodGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJwN{egcm0> NVPuVYVuW0GQR1XS
ETK-1 NV7zNIk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrwbINKSzVyPUKuPFIhdk1? NIrGVo5USU6JRWK=
BE-13 M2D6Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TnfWlEPTB;Mj65PUBvVQ>? NFTGNotUSU6JRWK=
A3-KAW M2Hsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTzTWM2OD1{Lkm5JI5O NFz6cpZUSU6JRWK=
TE-10 NHjVW2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvYfIxKSzVyPUOuN{BvVQ>? MnH3V2FPT0WU
DOHH-2 M{XoOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfDU4xTUUN3ME2zMlM2KG6P MnHEV2FPT0WU
ES6 NVyybpVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLxTWM2OD1|LkSzJI5O NH;ifXNUSU6JRWK=
OPM-2 NGPwNWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHyZ|lbUUN3ME20MlE2KG6P NYfQUZBMW0GQR1XS
SH-4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvPcYhIUUN3ME20MlM1KG6P MoH0V2FPT0WU
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MEG-01 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrZe2dKSzVyPUKwNU46PiCwTR?= NH\PSFZUSU6JRWK=
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OVCAR-4 MkXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJ|Nz6yOEBvVQ>? MUDTRW5ITVJ?
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NCI-H1648 NX3wUWdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTRzNz61N{BvVQ>? MYfTRW5ITVJ?
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KLE MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;iTWM2OD13OEWuNkBvVQ>? MmH4V2FPT0WU
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LB2518-MEL NG\sd|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHW1VJpKSzVyPUGyMlY5OTVizszN NGnpSGFUSU6JRWK=
NCI-H23 NID4ZlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP6[mpKSzVyPUGzMlI1OjVizszN NX24[lJlW0GQR1XS
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NCI-H1650 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXSTWM2OD1zNT60PVc6KM7:TR?= NF7x[3hUSU6JRWK=
NCI-H226 M4HXbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PBO2lEPTB;MUWuPFc3QCEQvF2= MX\TRW5ITVJ?
COR-L88 NULRTZVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTF4LkOxOEDPxE1? MWrTRW5ITVJ?
SCC-15 NHPhPYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fFcGlEPTB;MU[uN|g3QSEQvF2= MlvjV2FPT0WU
GOTO NF35dWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3izXmlEPTB;MU[uOFc6OyEQvF2= NWfpcGZCW0GQR1XS
SIMA MmnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3DW4VKSzVyPUG2MlQ5ODJizszN MlPlV2FPT0WU
NCI-H1299 NV;DNpdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\HcHhKSzVyPUG3MlE2QTFizszN NHfxTXdUSU6JRWK=
NCI-H1581 NVLwOWo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfWUotpUUN3ME2xO{41OjF7IN88US=> MYrTRW5ITVJ?
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ES7 NYDLd3FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\U[WlEPTB;MUiuOVQ{OSEQvF2= NVXZXpBFW0GQR1XS
JVM-3 NHz1SVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\JeYRKSzVyPUG4MlcyPyEQvF2= MmD4V2FPT0WU
RL MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJyLkO4PEDPxE1? NV;MOJN{W0GQR1XS
EC-GI-10 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjlTWM2OD1{MT6yNFQyKM7:TR?= MmLjV2FPT0WU
LNCaP-Clone-FGC M3XlNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJzLk[3Olgh|ryP NFLqTmhUSU6JRWK=
IMR-5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUToeIVqUUN3ME2yNU45PDl2IN88US=> MnT0V2FPT0WU
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NCI-H128 NXvp[IdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXuTWM2OD1{Mz61PFU{KM7:TR?= M1rmXnNCVkeHUh?=
RH-1 NXyy[VlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHhTWM2OD1{Mz63PFY3KM7:TR?= Mn3VV2FPT0WU
NCI-H2171 Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJ2LkK0PFUh|ryP M{Ph[HNCVkeHUh?=
RPMI-8866 NXviW4t[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH63PIJKSzVyPUK2Mlc1OiEQvF2= M3uzT3NCVkeHUh?=
SK-N-FI NFHJc4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTJ5LkO4NVEh|ryP NH[5U2RUSU6JRWK=
LOXIMVI M1GwZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXmWWtYUUN3ME2yO{45ODVzIN88US=> MmCyV2FPT0WU
P31-FUJ M{ixV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTNzLkWzO|Qh|ryP MVfTRW5ITVJ?
KMS-12-PE MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTR7LkWzNFIh|ryP MlnyV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:

[1]

+ Expand

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
Cell Research:

[3]

+ Expand
  • Cell lines: U87-MG, T98G, and U373-MG
  • Concentrations: Dissolved in DMSO, final concentrations ~25 μM
  • Incubation Time: 72 hours
  • Method:

    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.


    (Only for Reference)
Animal Research:

[7]

+ Expand
  • Animal Models: Athymic Nu/Nu mice inoculated subcutaneously with VEGF-A-expressing C6 rat glioma cells
  • Formulation: Dissolved in solvent solution (0.2% carboxymethylcellulose and 0.25% Tween-80 in sterile H2O)
  • Dosages: ~4 mg/kg/day
  • Administration: Injection i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (21.87 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* 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.

Chemical Information

Molecular Weight 914.18
Formula

C51H79NO13

CAS No. 53123-88-9
Storage powder
Synonyms AY 22989,NSC-2260804

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00062712 Completed Kidney Transplantation National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) June 9, 2003 Phase 2
NCT01814059 Terminated Eosinophilic Gastroenteritis|Eosinophilic Esophagitis National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) March 7, 2013 Phase 1
NCT01303965 Active, not recruiting Multiple Myeloma Sherif S. Farag|Celgene Corporation|Indiana University February 7, 2011 Phase 1|Phase 2
NCT02891603 Not yet recruiting Graft Vs Host Disease|GVHD H. Lee Moffitt Cancer Center and Research Institute April 30, 2017 Phase 1|Phase 2
NCT02423915 Recruiting Leukemia|Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Targazyme, Inc.|Cancer Prevention Research Institute of Texas July 30, 2015 Phase 1|Phase 2
NCT01182883 Withdrawn Brain Stem Neoplasms|Glioma|Pinealoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 28, 2010 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID