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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7 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.

  • 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)
Hck [1]
(Cell-free assay)
8 nM 0.10 μM 0.41 μM 0.41 μM 1.2 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 NXLDWHByTnWwY4Tpc44hSXO|YYm= NH;oWlM2OC1zMkWwJI5O NITOc2ozPCCq NVPOfGdVTE2VTx?= NXHaOWNvcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFN4IHvpcoF{\SBqdHHy[4V1KG:oIH3UU3JEOSliYX7kJIl1eyCmb4fud5Rz\WGvIIThdodmfCCyaH;zdIhwNVN4wrC= NVq2foc{OjZzN{ewOVE>
U87vIII  MoPySpVv[3Srb36gRZN{[Xl? MXmwMlA1NTJwNTFOwG0> M1jNeFI1KGh? MYDpcohq[mm2czDtWG9TSzFiYX7kJI1VV1KFMjDhZ5Rqfmm2aXXzxsA> MYGyOlE{PDZzNx?=
U87vIII  NU\2bXFoTnWwY4Tpc44hSXO|YYm= MVOyMlUwPSEQvF2= M3zYNVEzKGh? NF6zepJqdmirYnn0d{Bo[XBiY3zvd4lv\yCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnjXNlYyOzR4MUe=
PC12  NEfzdGhHfW6ldHnvckBCe3OjeR?= NUDDZoVlPDEEoH7N M1u0c4lv\HWlZYOgcJl{d3OxbXHsJIJqd2enbnXzbZMh[W6mIHHscIV3cWG2ZXSg{tEuW1mQIHHjZ5VufWyjdHnvcuKh M1;3OFI3ODBzNkG0
3T3-L1 Ml3TSpVv[3Srb36gRZN{[Xl? NVHid4hEOTVizszN M1zQSlQhcA>? NH\2U3V{fXCycnXzd4V{KGW6cILld5Nqd25ib3[geIhmKEWpckGgdJJwfGWrbtMg MXqyOVgyPDZ4Mh?=
Rh30 NXjnTpNFTnWwY4Tpc44hSXO|YYm= NXfsV|M6OSEQvF2= M1nteVIhcA>? M4TLTolvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= NF7nbnozPTd4Mk[xPS=>
HT29 NFHtdlFHfW6ldHnvckBCe3OjeR?= NHHJcJEyKM7:TR?= MnnRNkBp M1LYS4lvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= MlO3NlU4PjJ4MUm=
Rh30 M1LCRWZ2dmO2aX;uJGF{e2G7 NULtN|UyOSEQvF2= Ml\sNkBp MlvOd5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u Mk\TNlU4PjJ4MUm=
HT29 NFTuZplHfW6ldHnvckBCe3OjeR?= NHXTOYMyKM7:TR?= M3mzUFIhcA>? MX7zeZBxemW|c3XzJJRp\SCkYYPhcEBweiCLR1[tNU1{fGmvdXzheIVlKGOnbHygZYRp\XOrb36= M{jJ[|I2PzZ{NkG5
U87 MkHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NImyOoMzPSCwTR?= MomwNlQhcA>? NHW0N5BqdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> NWL6OHVVOjV3Nki2OlU>
AGS NH;Pb3pE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHPoT|ExNTFyMECgcm0> M1;LWVI1NzR6IHi= NGG0NnRFVVOR NV20VWFR\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M{HGZlI2ODN3OU[x
MKN45 Ml3PR4VtdCCYaXHibYxqfHliQYPzZZk> M3fs[|AuOTByMDDuUS=> NULTbWVPOjRxNEigbC=> NXzSfoRuTE2VTx?= NWDXOFN{\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NEPUXZczPTB|NUm2NS=>
MKN28 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVrSbWtTOC1zMECwJI5O NFX3W2EzPC92ODDo NHHHTHpFVVOR MnXt[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MYOyOVA{PTl4MR?=
KATO3 MmfNR4VtdCCYaXHibYxqfHliQYPzZZk> MXKwMVExODBibl2= NXLlPVRmOjRxNEigbC=> Ml;lSG1UVw>? NH7kV5Fl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M{nGWlI2ODN3OU[x
SGC7901 NXrEXGhTS2WubDDWbYFjcWyrdImgRZN{[Xl? MYOwMVExODBibl2= M{TzZlI1NzR6IHi= NXrIVno5TE2VTx?= NFnSVZhl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M4XLdVI2ODN3OU[x
N87 NVvUOIVIS2WubDDWbYFjcWyrdImgRZN{[Xl? NFr4dXAxNTFyMECgcm0> M17qXlI1NzR6IHi= NHnRSGdFVVOR M2TlRYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MVeyOVA{PTl4MR?=
HMEC NWjHemNqS2WubDDWbYFjcWyrdImgRZN{[Xl? NEXPd|QxNTFyMECgcm0> MVKyOE81QCCq M2jiUWROW09? MUTk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MVGyOVA{PTl4MR?=
HUVEC MnrYR4VtdCCYaXHibYxqfHliQYPzZZk> MX[wMVExODBibl2= NFyybpkzPC92ODDo MVXEUXNQ M2XsZYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MYKyOVA{PTl4MR?=
MG63 MnLkSpVv[3Srb36gRZN{[Xl? NVLUOpZvPTBvMUCwNEBvVQ>? M3nnb|AvPSCq NXjOOIh7\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 MlzwNlQ5PDBzM{S=
U2OS  NWPQeXNyTnWwY4Tpc44hSXO|YYm= NVrERoFlPTBvMUCwNEBvVQ>? NXnBUI1FOC53IHi= MoHu[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NY\ROXpIOjR6NECxN|Q>
Saos-2  NWrWfHZvTnWwY4Tpc44hSXO|YYm= NV;ZfYZlPTBvMUCwNEBvVQ>? MUOwMlUhcA>? MnnC[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NUjncYYxOjR6NECxN|Q>
Saos-2 NU[1eWl2TnWwY4Tpc44hSXO|YYm= NIr2NIYyODBibl2= NI\rcZQxNjViaB?= NVrDcI42eHKndnXueJMhd3O2ZX;zZZJkd22jIHPlcIwhdWmpcnH0bY9v MY[yOFg1ODF|NB?=
MG63 MmjWRZBweHSxc3nzJGF{e2G7 MYCxNFAhdk1? MVizOkBp MWjwdo9ud3SnczDhdI9xfG:|aYO= M{fOUlI1QDRyMUO0
U2OS  NUm5NZpKSXCxcITvd4l{KEG|c3H5 NHPpbVUyODBibl2= M2fmS|M3KGh? NYTERWxieHKxbX;0[ZMh[XCxcITvd4l{ NV32N21OOjR6NECxN|Q>
Saos-2  NUT5bYRiSXCxcITvd4l{KEG|c3H5 NXTEXIdxOTByIH7N M3zzdVM3KGh? MmHxdJJwdW:2ZYOgZZBweHSxc3nz NWDNZoNJOjR6NECxN|Q>
HT1376 NIXpTnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\BW4ZxUUN3ME2xMlg5KMLzIEGuNUDPxE1? NFzIXWQzPDB3NEi3NS=>
T24 NE[zN4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz3OXZ3UUN3ME2xMlM4KMLzIECuOEDPxE1? NU\PT5Z1OjRyNUS4O|E>
UM-UC-3 NV7Lb41DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwNkOgxtExNjFizszN MVuyOFA2PDh5MR?=
DLD-1 MVLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVuwMVExODBibl2= M37PZlI1KGh? M4XYPIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NI\EeYgzOzl7MUG3PS=>
Caco2 NUD2SGZ2S2WubDDWbYFjcWyrdImgRZN{[Xl? NICzS3kxNTFyMECgcm0> NEP1WnMzPCCq NFHzdoVqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmHRNlM6QTFzN{m=
HT29 NE[3NmVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4nGXlAuOTByMDDuUS=> M1K4SVI1KGh? NV[3[49qcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVmyN|k6OTF5OR?=
H116 NUTWTlNkS2WubDDWbYFjcWyrdImgRZN{[Xl? Mk\mNE0yODByIH7N NHzNb3IzPCCq MYnpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4XIdVI{QTlzMUe5
Hct-8 NGqwZo9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEnjNGIxNTFyMECgcm0> MXOyOEBp NV7WdFNjcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{[yS|I{QTlzMUe5
Colo320 NEPwbldE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MX[wMVExODBibl2= M1P1eFI1KGh? NELJdXlqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NV[zeGxDOjN7OUGxO|k>
Sw948 MVPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWXE[5NzOC1zMECwJI5O Ml7kNlQhcA>? NYjZe3ZZcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFXBXGEzOzl7MUG3PS=>
Colo205 M1fTWWNmdGxiVnnhZoltcXS7IFHzd4F6 NIHCXXQxNTFyMECgcm0> MWGyOEBp MWXpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NFLvdnQzOzl7MUG3PS=>
Colo320 M{LUVGZ2dmO2aX;uJGF{e2G7 NHjnenEyKM7:TR?= NFjQPGwxNTJ2IHi= NWHTTXdT[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? NF3kcGczOzl7MUG3PS=>
HT29 M3jUeWZ2dmO2aX;uJGF{e2G7 MkP4NUDPxE1? MXiwMVI1KGh? Mo\FZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> Mn\hNlM6QTFzN{m=
Sw948 MXHGeY5kfGmxbjDBd5NigQ>? M3zleFEh|ryP NFTv[2QxNTJ2IHi= NH;ROpVi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 M{GyWVI{QTlzMUe5
DLD-1 MnHUSpVv[3Srb36gRZN{[Xl? NVe0T|B4OSEQvF2= NFv5e2oxNTJ2IHi= M13HSIFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> M3;TblI{QTlzMUe5
SW620 M2X2bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfYSVRKSzVyPUeuPEDPxE1? NIq0T2MzOzV2MkG3PC=>
SW480 NHW0OnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljxTWM2OD12Lk[g{txO NUj2XVloOjN3NEKxO|g>
SK-CO-1 NULDeIxUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3oXYtjUUN3ME20JO69VQ>? M3TPO|I{PTR{MUe4
LS-513 MoTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnnfFBFUUN3ME2zMlkh|ryP NUfLRmhVOjN3NEKxO|g>
SW1116 NVfTc3BKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrLXZhKUUN3ME2wMlg1KM7:TR?= NHzRPWgzOzV2MkG3PC=>
LS-174T M{HoO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzTXlZKSzVyPUCuPFQh|ryP NYK1fY4yOjN3NEKxO|g>
HCT 116 MkDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETaZZpKSzVyPUCuOFEh|ryP Moj4NlM2PDJzN{i=
HCT 15 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrLTWM2OD1yLkOg{txO NGTiRoQzOzV2MkG3PC=>
COLO 205 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwMkSg{txO MX2yN|U1OjF5OB?=
HT-29 NEfsRVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn5TWM2OD1yLkKzJO69VQ>? NX\iWlVoOjN3NEKxO|g>
COLO 201 MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfwTFVKSzVyPUCuNlMh|ryP NVHNdJZ1OjN3NEKxO|g>
Caco-2 NFvmW|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwMkKg{txO NXnDZWRjOjN3NEKxO|g>
SW48 M4H2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPreJhKSzVyPUCuNFkh|ryP MUCyN|U1OjF5OB?=
DND-1 NXnoNYF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjnbGF1OC5{NT:wMlUwOSEQvF2= M2DZO2ROW09? NHHWeWhqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NWLhWIFFOjN2OEK3OFg>
TMD8 NF;ofFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[wMlI2NzBwNT:xJO69VQ>? MmPUSG1UVw>? MY\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M{nIelI{PDh{N{S4
Jurkat Mn\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHiwZ5UxNjJ3L{CuOU8yKM7:TR?= M4PGTmROW09? Mly2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Ml;mNlM1QDJ5NEi=
KOPT-K1 MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LJWVAvOjVxMD61M|Eh|ryP NUfL[5hNTE2VTx?= M{\k[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NH\kNpczOzR6Mke0PC=>
TMD7 M2[5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3viZlAvOjVxMD61M|Eh|ryP M3rtcWROW09? NYTW[mJOcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NYrHfHRsOjN2OEK3OFg>
THP-1 M1jhfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTZNE4zPS9yLkWvNUDPxE1? NV7GUFAzTE2VTx?= NID5N5BqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MonDNlM1QDJ5NEi=
786-O NIXiW5BHfW6ldHnvckBCe3OjeR?= MWqwMlEwOC53IN88US=> NXG1WIFSOjRiaB?= MX7EUXNQ NVmxNphlcW6lcnXhd4V{KEVvY3HkbIVzcW5ibWLORUBt\X[nbIOg[I9{\SCmZYDlcoRmdnSueR?= NXvWcotOOjNzNEeyOVE>
786-O MYLGeY5kfGmxbjDBd5NigQ>? NXXMV3Q4OC1yLkWg{txO MVmyOEBp MUTEUXNQ MoLkdoV{fWy2czDpckBiKGSxc3Wg[IVx\W6mZX70JIlv[3KnYYPlJIlvKEVvY3HkbIVzcW5icILveIVqdiCneIDy[ZN{cW:wwrC= Ml\uNlMyPDd{NUG=
OCI-AML3 NVzhRnI2SXCxcITvd4l{KEG|c3H5 MlG1Nk42KM7:TR?= MUW3NkBp NGLxeYlqdmS3Y3XzJIFxd3C2b4Ppdy=> NIfTOmozOjh{NkW2OS=>
Jurkat M2\xd2Z2dmO2aX;uJGF{e2G7 M1noV|ExOC9{MECvOFAxKG6P NHLXblgyQCCq MmHEbY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= Mn:2NlI2PjZ4MES=
p210 BCR-Abl NXzLN5VyTnWwY4Tpc44hSXO|YYm= NV;yWpdjOTByL{KwNE81ODBibl2= NGXodXUyQCCq NVrQ[ZNGcW6qaXLpeJMhdVSRUlOxMYRmeGWwZHXueEBUPiCVMkO1M|I{PiCyaH;zdIhwenmuYYTpc44> NEnMPZozOjV4Nk[wOC=>
Jurkat NVfZb|d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfZfJI1ODCwTR?= MnzMNlQwPDhiaB?= MVTzfY5memerenWge4l1cCBzNz3BRWchfG9ic4XwdJJme3NiY3XscEBxem:uaX\ldoF1cW:w MmfQNlI2PjZ4MES=
p210 BCR-Abl MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;zN|QxOG6P NWrYSZB7OjRxNEigbC=> MoOyd5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= M2nCNVIzPTZ4NkC0
8226 NFTN[nJHfW6ldHnvckBCe3OjeR?= NXrYbZlxOTByLUGwNFAhdk1? M2TlNFMxKG2rbh?= MnPGSG1UVw>? NGfESYFi[3SrdnH0[ZMhTVKNwrC= MY[yNlU2PjRyOR?=
MM1.S  Mm\pSpVv[3Srb36gRZN{[Xl? Mm\sNVAxNTFyMECgcm0> NGmzWXo{OCCvaX6= NG\kXpJFVVOR NYLO[|By[WO2aY\heIV{KEWUS9Mg NHvTeI0zOjV3NkSwPS=>
8226 MWrGeY5kfGmxbjDBd5NigQ>? MmH1NE42KM7:TR?= MXOzNEBucW5? MU\EUXNQ MmjzbY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= NFO5VY0zOjV3NkSwPS=>
MM1.S  Mn\2SpVv[3Srb36gRZN{[Xl? MoH6NE42KM7:TR?= NVnYTJh4OzBibXnu M3r5W2ROW09? M1vYU4lv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= M4rYfFIzPTV4NEC5
MCF-7 NE[zdVRHfW6ldHnvckBCe3OjeR?= MVO1NE8zODBxNUCwJI5O NUTTSWJROzBibXnu M3zwV4Rwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MYKyNlQ4Pjh3Mh?=
T47D MULGeY5kfGmxbjDBd5NigQ>? MmXVOVAwOjByL{WwNEBvVQ>? M2r1elMxKG2rbh?= MXnkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NW\WNIlpOjJ2N{[4OVI>
MDA-MB-231 MVXGeY5kfGmxbjDBd5NigQ>? NIjTN2c2OC9{MECvOVAxKG6P MnvoN|AhdWmw M1P2foRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 NX\EbYs6OjJ2N{[4OVI>
Bcap-37 NVf1dJZjTnWwY4Tpc44hSXO|YYm= MXO1NE8zODBxNUCwJI5O M{DqO|MxKG2rbh?= NX3YT2Vx\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MUeyNlQ4Pjh3Mh?=
MCF-7 M4\uXWFxd3C2b4Ppd{BCe3OjeR?= NUSzc5oxOjBywrDuUS=> M3TNe|M3KGh? NIDkSGtFVVOR MkfqbY5lfWOnczDhdI9xfG:|aYO= NFnoOFczOjR5Nki1Ni=>
MDA-MB-231 MX3BdI9xfG:|aYOgRZN{[Xl? M1XkS|IxOMLibl2= NEm2ZXA{PiCq NYDVZ5RMTE2VTx?= NWDiOWs5cW6mdXPld{BieG:ydH;zbZM> NF3GZnkzOjR5Nki1Ni=>
Bcap-37 NUf4So5lSXCxcITvd4l{KEG|c3H5 NV7YclFDOjBywrDuUS=> NEXGU4c{PiCq NYrJUXZ4TE2VTx?= MX;pcoR2[2W|IHHwc5B1d3Orcx?= NHX2WYEzOjR5Nki1Ni=>
LS174T NIS2coFHfW6ldHnvckBCe3OjeR?= MXmxNE8yODBxMUCwNEBvVQ>? NFi1NXA3KGh? MoLMSG1UVw>? M4r3VIlvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> M3n0VFIzPDBzMkm0
DLD-1  MUjGeY5kfGmxbjDBd5NigQ>? MWCxNE8yODBxMUCwNEBvVQ>? NWD4S411PiCq NFi3U4hFVVOR NG[ze4FqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv MXGyNlQxOTJ7NB?=
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SW620-R NF\1OnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjXbGxpUUN3ME2xMlMh|ryP NXvOZXRUOjJ{N{CyOVc>
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NIH 3T3 MV7GeY5kfGmxbjDBd5NigQ>? NYPuU2cxOiEQvF2= M1PlcVE5KGh? NGj1ZpNqdmirYnn0d{BuXE:UQ{KgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfCCxbjDT[ZI1PzNiYX7kJI1VV1KFMTDwbI9{eGixconsZZRqd25ib3[gOGUuSlBzIH;uJHRpejN5L{S2 M4TwbVIyQDd4MUOw
HCT15 Ml63SpVv[3Srb36gRZN{[Xl? M3;6NlAvPS9{IN88US=> MUe0JIg> M4flNpBz\X[nboTzJHM3UzFicHjvd5Bpd3K7bHH0bY9vKG:oIILpZo9{d22jbDDwdo91\WmwIGO2JIF1KFOnckK0NE8zPDRiYX7kJI1VV1KFMjDwbI9{eGixconsZZRqd25ib3[gRYt1KGG2IGPldlQ4Ow>? MWeyNVg4PjF|MB?=
SW620  NWjJbWZsTnWwY4Tpc44hSXO|YYm= M4HN[FAvPS9{IN88US=> MXK0JIg> MkfuZoxw[2u|IHHscEB1cHKnZTDtWG9TKG:3dID1eJM> M3jqOVIyQDd4MUOw

... 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]
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  • 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 62 mg/mL (201.07 mM)
Ethanol 18 mg/mL (58.37 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/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.

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
    Volume
    Molecular Weight

*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

Mass Concentration Volume Molecular Weight

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