Torkinib (PP242)

Catalog No.S2218

Torkinib (PP242) Chemical Structure

Molecular Weight(MW): 308.34

Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.

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8 Customer Reviews

  • MTORC1 regulates the subcellular distribution of TFEB. Immunofluorescence confocal microscopy showing nuclear localization of recombinant TFEB-Flag in ARPE-19 cells incubated with MTORC1 inhibitors (PP242, LY294002, Wortmannin).

    Autophagy 2012 8(6), 903-14. Torkinib (PP242) purchased from Selleck.

    Pharmacological PP242 induces transport of TFEB to the nucleus. HeLa cells stably expressing TFEB (CF7) were incubated with the indicated kinase inhibitors and the electrophoretic mobility of TFEB was monitored by immunoblotting.

    Autophagy 2012 8(6), 903-14. Torkinib (PP242) purchased from Selleck.

  • AKT protein kinase activity controls protein synthesis by regulating the multistep process of mRNA translation at multiple stages from ribosome biogenesis to translation initiation and elongation. PC3-LN4 cells were treated with GSK690693 (5 uM) alone, or in combination with PP242 (2 uM) or AZD8055 (1 uM) for 24 h, and immunoblotting performed.

    Cancer Res 2013 73(11), 3402-11. Torkinib (PP242) purchased from Selleck.

    Synergistic effect of BMS-777607 with mTOR inhibitors in reduction of CSCs+24/44/ESA viability. CSCs+24/44/ESA at 5,000 cells per well with stem cell culture media in triplicate in an ultra-low adhesion plate were treated with 5 umol/L BMS-777607, 1 umol/L AZD8055, 1 umol/L RAD001, and 1 umol/L PP242 alone, or in their different combinations. Cells were cultured for 72 hours. Percentages of polyploid cells were determined by counting 300 cells from two different regions. Results shown here were from one of two experiments with similar results.

    Mol Cancer Ther 2014 13(1), 37-48. Torkinib (PP242) purchased from Selleck.

  • (A) MEF and PC3-LN4 cells were treated with GNE-652 or LGB321 in a dose dependent manner and PP242 (1 µmol/L) for 16 hr

    Oncotarget, 2016, 7(15):20152-65. Torkinib (PP242) purchased from Selleck.

    HeLa cells were treated with MK2206 (1 uM), rapamycin (Rapa; 100 nM), PP242 (1 uM), BEZ235 (0.5 uM), U0126 (U0; 15 uM), BI-D1870 (BI; 10 uM), GNE-652 (1 uM), AZD1208 (3 uM), and the indicated inhibitor combinations for 3 h. Cell lysates were analyzed by immunoblot assays using indicated antibodies.

    Mol Cell Biol 2014 34(13), 2517-32. Torkinib (PP242) purchased from Selleck.

  • Torkinib (PP242) purchased from Selleck.

    A549 cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of  PP242 for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. Torkinib (PP242) purchased from Selleck.

Purity & Quality Control

Choose Selective mTOR Inhibitors

Biological Activity

Description Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.
Features One of the first selective inhibitors that targets ATP domain of mTOR.
Targets
mTOR [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
DNA-PK [1]
(Cell-free assay)
PDGFR [1]
(Cell-free assay)
8 nM 0.10 μM 0.41 μM 0.41 μM
In vitro

PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively. PP242 displays some inhibitory activity against Ret, PKCα, PKCβ, and JAK2, while exhibits remarkable selectivity against 215 other protein kinases. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2. In BT549 cells, PP242 treatment (0.04-10 μM) inhibits the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner. [1] PP242 potently inhibits PKCα with IC50 of 49 nM. Low concentrations of PP242 inhibit the phosphorylation of Akt S473 and higher concentrations partially inhibit Akt T308-P in addition to S473-P. As PP242 is a more effective mTORC1 inhibitor than rapamycin, PP242 inhibits the proliferation of primary MEFs, and the phosphorylation of 4EBP1 at T36/45 and S65, more potently than rapamycin. PP242 but not rapamycin potently inhibits cap-dependent translation, by causing a higher level of binding between 4EBP1 and eIF4E than rapamycin. [2] PP242 potently inhibits the proliferation of p190-transformed murine BM, SUP-B15, and K562 cells with GI50 of 12 nM, 90 nM, and 85 nM, respectively. PP242 also inhibits the growth of solid tumor cell lines such as SKOV3, PC3, 786-O, and U87 with GI50 of 0.49 μM, 0.19 μM, 2.13 μM, and 1.57 μM, respectively. [3] PP242 is also more effective than rapamycin in achieving cytoreduction and apoptosis in multiple myeloma (MM) cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-p21 NGiyO2VHfW6ldHnvckBCe3OjeR?= NE\vclY2OC1zMkWwJI5O M3vlbVI1KGh? NFnPdXBFVVOR M4nQTolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPiCtaX7hd4UhMHSjcnfleEBw\iCvVF;SR|EqKGGwZDDpeJMh\G:5boP0doVidSC2YYLn[ZQheGixc4Doc{1UPsLi M320elI3OTd5MEWx
U87vIII  MVLGeY5kfGmxbjDBd5NigQ>? NUnRd|hZOC5yND2yMlUh|ryP MmP5NlQhcA>? NVrMcWlOcW6qaXLpeJMhdVSRUlOxJIFv\CCvVF;SR|Ih[WO2aY\peIlme8Li NFSyZo0zPjF|NE[xOy=>
U87vIII  Mn3hSpVv[3Srb36gRZN{[Xl? Mk\wNk42NzVizszN M1joelEzKGh? Mni5bY5pcWKrdIOg[4FxKGOub4PpcochcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlfaNlYyOzR4MUe=
PC12  MkPISpVv[3Srb36gRZN{[Xl? M{D6PVQxyqCwTR?= M{nhVolv\HWlZYOgcJl{d3OxbXHsJIJqd2enbnXzbZMh[W6mIHHscIV3cWG2ZXSg{tEuW1mQIHHjZ5VufWyjdHnvcuKh MmnvNlYxODF4MUS=
3T3-L1 M4rud2Z2dmO2aX;uJGF{e2G7 M3jYVlE2KM7:TR?= MV60JIg> M2jP[pN2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhTWe{MTDwdo91\WmwwrC= NFr1NlUzPThzNE[2Ni=>
Rh30 M1z6dWZ2dmO2aX;uJGF{e2G7 M13hb|Eh|ryP MkOzNkBp NU\GS4NKcW6qaXLpeJMh[m:2aDDtWG9TSzFvbXXkbYF1\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGO2T|Eh[W6mIH3UU3JEOi2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NYT3[2pqOjV5NkK2NVk>
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Rh30 MkPZSpVv[3Srb36gRZN{[Xl? Mk\NNUDPxE1? NGLSV48zKGh? M3XxS5N2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> NG\DToIzPTd4Mk[xPS=>
HT29 NGLiVHRHfW6ldHnvckBCe3OjeR?= MYWxJO69VQ>? NF6y[GszKGh? NVixTYFCe3WycILld5NmeyC2aHWgZoF{[Wxib4KgTWdHNTFvc4TpcZVt[XSnZDDj[YxtKGGmaHXzbY9v MVmyOVc3OjZzOR?=
U87 M1[2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOyOUBvVQ>? NIHqZXYzPCCq NUTiPHRLcW6lcnXhd4V{KESXU2CxNEBsdm:la3XkMYRwf25iaX7keYNm\CClZXzsJIlvcGmkaYTpc44> NXTOXIRJOjV3Nki2OlU>
AGS NHz3WYJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFv3b4wxNTFyMECgcm0> NHTpZ24zPC92ODDo M17sOGROW09? NGfER3ll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MWOyOVA{PTl4MR?=
MKN45 MVTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkDGNE0yODByIH7N NIG2RZAzPC92ODDo NGDKfHNFVVOR NHzIW3ll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NX7OdVJwOjVyM{W5OlE>
MKN28 NIPFcIdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NX;2e4hCOC1zMECwJI5O NULDRmZPOjRxNEigbC=> M1zl[WROW09? M2fLZoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1K3OFI2ODN3OU[x
KATO3 NV\vSlg4S2WubDDWbYFjcWyrdImgRZN{[Xl? NUL5VJc4OC1zMECwJI5O NFPOUHkzPC92ODDo NVrSbYZsTE2VTx?= M2S3WoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Mk\nNlUxOzV7NkG=
SGC7901 MVrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUGwMVExODBibl2= NHn6UWszPC92ODDo MnTSSG1UVw>? M362XIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NF;IUZEzPTB|NUm2NS=>
N87 NVKyV3MxS2WubDDWbYFjcWyrdImgRZN{[Xl? NWL6V4ZOOC1zMECwJI5O NWPP[XJxOjRxNEigbC=> Mn3JSG1UVw>? NG\MeIRl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M2nwbVI2ODN3OU[x
HMEC M33LVWNmdGxiVnnhZoltcXS7IFHzd4F6 M4rWflAuOTByMDDuUS=> M4Ow[VI1NzR6IHi= Mo\6SG1UVw>? NUfUflhw\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= Mo\HNlUxOzV7NkG=
HUVEC MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHzWO5kxNTFyMECgcm0> NEjWbpczPC92ODDo M3K5VGROW09? NITVO5Vl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MWqyOVA{PTl4MR?=
MG63 NV63bVllTnWwY4Tpc44hSXO|YYm= M17Td|UxNTFyMECgcm0> MWOwMlUhcA>? M4TrZoRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MkjLNlQ5PDBzM{S=
U2OS  MXvGeY5kfGmxbjDBd5NigQ>? NFnLSmw2OC1zMECwJI5O NEK3cHgxNjViaB?= M1;NS4Rwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M3TkbFI1QDRyMUO0
Saos-2  MmLrSpVv[3Srb36gRZN{[Xl? M1HpelUxNTFyMECgcm0> MVuwMlUhcA>? MnW1[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NHzFbHMzPDh2MEGzOC=>
Saos-2 NEHwZotHfW6ldHnvckBCe3OjeR?= NEXUXowyODBibl2= M2Pa[FAvPSCq MoX6dJJmfmWwdIOgc5N1\W:|YYLjc41iKGOnbHygcYloemG2aX;u MnzvNlQ5PDBzM{S=
MG63 M17WVmFxd3C2b4Ppd{BCe3OjeR?= NEC1UGgyODBibl2= NV3UZVM3OzZiaB?= MoC5dJJwdW:2ZYOgZZBweHSxc3nz Mmi5NlQ5PDBzM{S=
U2OS  MWDBdI9xfG:|aYOgRZN{[Xl? NEGyN2syODBibl2= MVuzOkBp MlrqdJJwdW:2ZYOgZZBweHSxc3nz NUPUZ4FGOjR6NECxN|Q>
Saos-2  MY\BdI9xfG:|aYOgRZN{[Xl? NXHIS4gxOTByIH7N MXuzOkBp M3;ZOpBzd22xdHXzJIFxd3C2b4Ppdy=> Ml3sNlQ5PDBzM{S=
HT1376 NXzZXHFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPIZ3p3UUN3ME2xMlg5KMLzIEGuNUDPxE1? M3K2NVI1ODV2OEex
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UM-UC-3 M{fifmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi1ZmNoUUN3ME2wMlY{KMLzMD6xJO69VQ>? NYrHVHJYOjRyNUS4O|E>
DLD-1 NIrlVZBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NULHPWJpOC1zMECwJI5O Mnu1NlQhcA>? MlPzbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mli3NlM6QTFzN{m=
Caco2 NI[zeHlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mli5NE0yODByIH7N M4nzUFI1KGh? MoTUbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{fqUFI{QTlzMUe5
HT29 NYrSTGJvS2WubDDWbYFjcWyrdImgRZN{[Xl? M365OVAuOTByMDDuUS=> MlTrNlQhcA>? MWHpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MWWyN|k6OTF5OR?=
H116 M4XrbGNmdGxiVnnhZoltcXS7IFHzd4F6 NXK3ZnNZOC1zMECwJI5O NXize3RlOjRiaB?= M1vRdYlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mn;iNlM6QTFzN{m=
Hct-8 MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVTzSGx2OC1zMECwJI5O NYPKUoJ1OjRiaB?= Mm[zbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFLDUYQzOzl7MUG3PS=>
Colo320 M2TZVGNmdGxiVnnhZoltcXS7IFHzd4F6 M1LqdVAuOTByMDDuUS=> NEW5fGgzPCCq M1i1W4lvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWXYWGJoOjN7OUGxO|k>
Sw948 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M33KZ|AuOTByMDDuUS=> MkHDNlQhcA>? Mm\vbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NH3FV5IzOzl7MUG3PS=>
Colo205 Mo\zR4VtdCCYaXHibYxqfHliQYPzZZk> MWqwMVExODBibl2= MXOyOEBp NVfVbYxWcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIey[5IzOzl7MUG3PS=>
Colo320 NXzn[3BGTnWwY4Tpc44hSXO|YYm= MlfpNUDPxE1? NFroRWcxNTJ2IHi= MV\hZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 NXT1[GQ3OjN7OUGxO|k>
HT29 MlPZSpVv[3Srb36gRZN{[Xl? M4LYcFEh|ryP NHi5clkxNTJ2IHi= NWTTV49P[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? M2XzRlI{QTlzMUe5
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DLD-1 M{jLWmZ2dmO2aX;uJGF{e2G7 M2HOVlEh|ryP NGrWTpoxNTJ2IHi= NFS1S45i[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 NI\1fm0zOzl7MUG3PS=>
SW620 NFjmZ4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjVNJlnUUN3ME23Mlgh|ryP NYP0ZopsOjN3NEKxO|g>
SW480 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHodWNKSzVyPUSuOkDPxE1? MoW5NlM2PDJzN{i=
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LS-513 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzVT3FpUUN3ME2zMlkh|ryP NEL2d48zOzV2MkG3PC=>
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LS-174T MmHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PtfGlEPTB;MD64OEDPxE1? MXyyN|U1OjF5OB?=
HCT 116 NFjFZ2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H4SWlEPTB;MD60NUDPxE1? M32yXFI{PTR{MUe4
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COLO 201 M4nxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HaPWlEPTB;MD6yN{DPxE1? NXvHUWVMOjN3NEKxO|g>
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SW48 MnP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjCTWM2OD1yLkC5JO69VQ>? MX:yN|U1OjF5OB?=
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TMD8 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvoU25DOC5{NT:wMlUwOSEQvF2= Mmi0SG1UVw>? NX3uTHZWcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M3LicFI{PDh{N{S4
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KOPT-K1 NHTwXHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVewMlI2NzBwNT:xJO69VQ>? MmjISG1UVw>? NH3RfY5qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NG\OVVQzOzR6Mke0PC=>
TMD7 NGXQT5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7jNE4zPS9yLkWvNUDPxE1? NHLobVdFVVOR NVSyS2ducW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mm\FNlM1QDJ5NEi=
THP-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmwMlI2NzBwNT:xJO69VQ>? MYXEUXNQ MXvpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MV6yN|Q5Ojd2OB?=
786-O NWftVHVETnWwY4Tpc44hSXO|YYm= Mnr0NE4yNzBwNTFOwG0> NHrPdYQzPCCq MYrEUXNQ M2HLXIlv[3KnYYPld{BGNWOjZHjldolvKG2UTlGgcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHl? NIfOd2ozOzF2N{K1NS=>
786-O MkH4SpVv[3Srb36gRZN{[Xl? NWLtfJpjOC1yLkWg{txO NGCzTWMzPCCq NEewSW5FVVOR MUHy[ZN2dHS|IHnuJIEh\G:|ZTDk[ZBmdmSnboSgbY5kemWjc3WgbY4hTS2lYXTo[ZJqdiCycn;0[YlvKGW6cILld5Nqd28EoB?= MViyN|E1PzJ3MR?=
OCI-AML3 NYPhTpMzSXCxcITvd4l{KEG|c3H5 NGD6RVczNjVizszN M1XUV|czKGh? NX\B[FVMcW6mdXPld{BieG:ydH;zbZM> M3rI[FIzQDJ4NU[1
Jurkat MVfGeY5kfGmxbjDBd5NigQ>? NGnsN4UyODBxMkCwM|QxOCCwTR?= NGHuUpAyQCCq NFjPeZdqdmirYnn0d{BuXE:UQ{Gt[IVx\W6mZX70JHM3KFN{M{WvNlM3KHCqb4PwbI9zgWyjdHnvci=> MlLJNlI2PjZ4MES=
p210 BCR-Abl NXPDTYxpTnWwY4Tpc44hSXO|YYm= NYnjWnBHOTByL{KwNE81ODBibl2= M3\2OlE5KGh? NH\Md3FqdmirYnn0d{BuXE:UQ{Gt[IVx\W6mZX70JHM3KFN{M{WvNlM3KHCqb4PwbI9zgWyjdHnvci=> M3G3OlIzPTZ4NkC0
Jurkat NWixPYo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\nO|QxOG6P M3Xl[FI1NzR6IHi= M2ryOpN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= MoH2NlI2PjZ4MES=
p210 BCR-Abl NUnoe|ZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nF[|QxOG6P M1\sOFI1NzR6IHi= NVrDPXB7e3mwZYLnbZpmKHerdHigNVcuSUGJIITvJJN2eHC{ZYPzJINmdGxicILvcIln\XKjdHnvci=> NH3ZOY4zOjV4Nk[wOC=>
8226 NH3NO|dHfW6ldHnvckBCe3OjeR?= MUGxNFAuOTByMDDuUS=> NVT5[Yx2OzBibXnu NI[w[GNFVVOR MlvCZYN1cX[jdHXzJGVTU8Li NI\KNJAzOjV3NkSwPS=>
MM1.S  M3;IemZ2dmO2aX;uJGF{e2G7 MYixNFAuOTByMDDuUS=> M1HI[lMxKG2rbh?= Mmn3SG1UVw>? M121VYFkfGm4YYTld{BGWkwEoB?= NFLwPJczOjV3NkSwPS=>
8226 M2m1Z2Z2dmO2aX;uJGF{e2G7 NW\2Xo9lOC53IN88US=> NX\PWnlLOzBibXnu M2PS[mROW09? NVntcJJOcW6mdXPld{Bi[3SrdnH0bY9vKG:oIGLBSkBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIF3FTy=> MmLQNlI2PTZ2MEm=
MM1.S  MX\GeY5kfGmxbjDBd5NigQ>? MkD3NE42KM7:TR?= MVmzNEBucW5? NIPQWYtFVVOR NGTVNXBqdmS3Y3XzJIFkfGm4YYTpc44hd2ZiUlHGJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiTVXL MnfqNlI2PTZ2MEm=
MCF-7 NGDxOndHfW6ldHnvckBCe3OjeR?= MkTHOVAwOjByL{WwNEBvVQ>? M{K4Z|MxKG2rbh?= M2PjSYRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MYKyNlQ4Pjh3Mh?=
T47D M3\wOGZ2dmO2aX;uJGF{e2G7 NInTeI02OC9{MECvOVAxKG6P MkLrN|AhdWmw MWnkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M2DnVlIzPDd4OEWy
MDA-MB-231 MnPaSpVv[3Srb36gRZN{[Xl? NVXtUWZPPTBxMkCwM|UxOCCwTR?= M2SzdlMxKG2rbh?= NXPqOYtD\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? NWK5VJdMOjJ2N{[4OVI>
Bcap-37 NWnieXkzTnWwY4Tpc44hSXO|YYm= M2jMbFUxNzJyMD:1NFAhdk1? NIPjV4I{OCCvaX6= NXXINldz\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MnrPNlI1PzZ6NUK=
MCF-7 M{PzS2Fxd3C2b4Ppd{BCe3OjeR?= M2rNPFIxOMLibl2= NWXmPVRXOzZiaB?= M3KyU2ROW09? M4rv[4lv\HWlZYOgZZBweHSxc3nz NV;FSmtGOjJ2N{[4OVI>
MDA-MB-231 NUTkd49USXCxcITvd4l{KEG|c3H5 NUfyNYdnOjBywrDuUS=> NHmwb4Q{PiCq MVfEUXNQ NXPMeotqcW6mdXPld{BieG:ydH;zbZM> MXyyNlQ4Pjh3Mh?=
Bcap-37 MXHBdI9xfG:|aYOgRZN{[Xl? M4P4S|IxOMLibl2= M3m3TVM3KGh? M{L0OWROW09? MVTpcoR2[2W|IHHwc5B1d3Orcx?= NGfxRZgzOjR5Nki1Ni=>
LS174T NVHMdZJCTnWwY4Tpc44hSXO|YYm= NFjZZ4syOC9zMECvNVAxOCCwTR?= MlKyOkBp MnvUSG1UVw>? NYTFO4Z3cW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? Mo\zNlI1ODF{OUS=
DLD-1  MWHGeY5kfGmxbjDBd5NigQ>? Mnf5NVAwOTByL{GwNFAhdk1? Mlj2OkBp MXfEUXNQ MXjpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu MorXNlI1ODF{OUS=
SW480 NXnmd3A5TnWwY4Tpc44hSXO|YYm= M1raelExNzFyMD:xNFAxKG6P MUm2JIg> MmPBSG1UVw>? MomwbY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> MXmyNlQxOTJ7NB?=
SW-48 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X5cWlEPTB;MD6xJO69VQ>? M2\JUVIzOjdyMkW3
HCT-15 NH;HV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2m3UWlEPTB;MD6zJO69VQ>? MUCyNlI4ODJ3Nx?=
HCT 116 NWrLeGJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fiU2lEPTB;MD62JO69VQ>? NFHIS2gzOjJ5MEK1Oy=>
SW620-R NV;pcYlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFwMzFOwG0> MX6yNlI4ODJ3Nx?=
SK-CO-1 M4TFWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPsTWM2OD1{LkGg{txO Mn7sNlIzPzB{NUe=
SW620 NYewR4NNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXXNoRKSzVyPUGxJO69VQ>? NGrs[VEzOjJ5MEK1Oy=>
BaF3 NVW1SGh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\oS2k2OD1zLkS0PUDPxE1? MVGyNlIzOzZ2NR?=
NIH 3T3 M{TkXmZ2dmO2aX;uJGF{e2G7 MVWyJO69VQ>? MmXUNVghcA>? MnfWbY5pcWKrdIOgcXRQWkN{IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qhd25iU3XyOFc{KGGwZDDtWG9TSzFicHjvd5Bpd3K7bHH0bY9vKG:oIETFMWJROSCxbjDUbJI{Py92Nh?= MXeyNVg4PjF|MB?=
HCT15 NFLRNG5HfW6ldHnvckBCe3OjeR?= NWjtTYV5OC53L{Kg{txO M2nveFQhcA>? NVe0U3l{eHKndnXueJMhWz[NMTDwbI9{eGixconsZZRqd25ib3[gdoljd3OxbXHsJJBzd3SnaX6gV|Yh[XRiU3XyNlQxNzJ2NDDhcoQhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3RiYYSgV4VzPDd| NH3uPWEzOTh5NkGzNC=>
SW620  MX7GeY5kfGmxbjDBd5NigQ>? NHLwTIwxNjVxMjFOwG0> NUjYXWdYPCCq MkKzZoxw[2u|IHHscEB1cHKnZTDtWG9TKG:3dID1eJM> M3TDdlIyQDd4MUOw

... Click to View More Cell Line Experimental Data

In vivo Administration of PP242 is able to completely inhibit the phosphorylation of Akt at S473 and T308 in fat and liver of mice. PP242 only partially inhibits the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite able to fully inhibit the phosphorylation of 4EBP1 and S6. [2] Oral administration PP242 potently delays the leukemia onset in the mice model, and induces leukemia regression by inhibiting mTORC2 and mTORC1 activation that correlates with loss in cell size. [3] PP242 treatment potently inhibits the growth of 8226 cells in mice. [4]

Protocol

Kinase Assay:[1]
+ Expand

In vitro mTOR (FRAP1) kinase assay:

Recombinant mTOR is incubated with PP242 at 2-fold dilutions over a concentration range of 50-0.001 μM in an assay containing 50 mM HEPES, pH 7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Tween, 10 μM ATP (2.5 μCi of γ-32P-ATP), and 3 μg/mL BSA. Rat recombinant PHAS-1/4EBP1 (2 mg/mL) is used as a substrate. Reactions are terminated by spotting onto nitrocellulose, which is washed with 1 M NaCl/1% phosphoric acid (approximately 6 times, 5-10 minutes each). Sheets are dried and the transferred radioactivity quantitated by phosphorimaging. IC50 value is calculated by fitting the data to a sigmoidal dose-response curve using the Prism software package.
Cell Research:[2]
+ Expand
  • Cell lines: MEFs
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method: Cells are treated with increasing concentrations of PP242 for 72 hours in 96-well plates. After 72 hours of treatment, 10 μL of 440 μM resazurin sodium salt is added to each well, and after 18 hours, the florescence intensity in each well is measured using a top-reading florescent plate reader with excitation at 530 nm and emission at 590 nm.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: Syngeneic (Balbc/J) mice with mouse p190-transformed BM cells to initiate leukemia, and female NSG mice injected (i.v.) with SUP-B15ffLuc cells or human Ph+ leukemia
  • Formulation: Dissolved in PEG400 (Carbowax polyethylene glycol)
  • Dosages: ~60 mg/kg/day
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (197.83 mM)
Ethanol 18 mg/mL (58.37 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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 308.34
Formula

C16H16N6O

CAS No. 1092351-67-1
Storage powder
in solvent
Synonyms N/A

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:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
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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).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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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.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Do you have any suggestions about potential candidates for vehicles that we could use for in vivo studies?

  • Answer:

    S2218 in the recommended solvent (30% PEG400 + 0.5% Tween80 + 5% Propylene glycol) is a suspension, and this formulation is for oral gavage. For IV injection, this compound can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5mg/ml as a clear solution.

mTOR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID