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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MYDGeY5kfGmxbjDBd5NigQ>? MVW1NE0yOjVyIH7N MYCyOEBp NFfOXFhFVVOR NHzL[pRqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZia3nuZZNmKCi2YYLn[ZQhd2ZibWTPVmMyMSCjbnSgbZR{KGSxd37zeJJm[W1idHHy[4V1KHCqb4PwbI8uWzcEoB?= NXHUWYtEOjZzN{ewOVE>
U87vIII  MlXaSpVv[3Srb36gRZN{[Xl? MVSwMlA1NTJwNTFOwG0> MkjpNlQhcA>? NX3RXW9scW6qaXLpeJMhdVSRUlOxJIFv\CCvVF;SR|Ih[WO2aY\peIlme8Li MoTyNlYyOzR4MUe=
U87vIII  MUTGeY5kfGmxbjDBd5NigQ>? NG\HPXYzNjVxNTFOwG0> NID0[JUyOiCq MlPHbY5pcWKrdIOg[4FxKGOub4PpcochcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHTudoszPjF|NE[xOy=>
PC12  NUfIb2MxTnWwY4Tpc44hSXO|YYm= NE\XV401OMLibl2= NXr5OFM3cW6mdXPld{BtgXOxc3;tZYwh[mmxZ3Xu[ZNqeyCjbnSgZYxt\X[rYYTl[EDPuS2VWV6gZYNkfW23bHH0bY9vyqB? MkTONlYxODF4MUS=
3T3-L1 NXTr[XhwTnWwY4Tpc44hSXO|YYm= NVjsXnRTOTVizszN M1q4WlQhcA>? MV3zeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGVoejFicILveIVqdsLi MnjkNlU5OTR4NkK=
Rh30 MUfGeY5kfGmxbjDBd5NigQ>? NVXLOWFYOSEQvF2= MUCyJIg> NED3eJJqdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= MWiyOVc3OjZzOR?=
HT29 NEC3ZZNHfW6ldHnvckBCe3OjeR?= MWWxJO69VQ>? M3PwOlIhcA>? NEmxXXpqdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= M1K3W|I2PzZ{NkG5
Rh30 Mkf3SpVv[3Srb36gRZN{[Xl? MnXrNUDPxE1? MoiwNkBp MkT3d5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u M4HQV|I2PzZ{NkG5
HT29 Mn\5SpVv[3Srb36gRZN{[Xl? MX[xJO69VQ>? NX7oVZN3OiCq MoTSd5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u MoLyNlU4PjJ4MUm=
U87 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrMOFEzPSCwTR?= NYDsZ5N4OjRiaB?= NXvX[mN7cW6lcnXhd4V{KESXU2CxNEBsdm:la3XkMYRwf25iaX7keYNm\CClZXzsJIlvcGmkaYTpc44> NEjtPI4zPTV4OE[2OS=>
AGS M4TDNmNmdGxiVnnhZoltcXS7IFHzd4F6 NVW4NYU1OC1zMECwJI5O NWPkfIFJOjRxNEigbC=> NULsVm5iTE2VTx?= M2fjO4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NF\odHEzPTB|NUm2NS=>
MKN45 NYHVd|NxS2WubDDWbYFjcWyrdImgRZN{[Xl? NELRSmMxNTFyMECgcm0> M1LyTVI1NzR6IHi= MlHxSG1UVw>? NFHtZnZl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M{H5XlI2ODN3OU[x
MKN28 M2K5[WNmdGxiVnnhZoltcXS7IFHzd4F6 MWSwMVExODBibl2= NInnbpozPC92ODDo MnLpSG1UVw>? NXHLTlBw\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M2e5OFI2ODN3OU[x
KATO3 M1;LXWNmdGxiVnnhZoltcXS7IFHzd4F6 NUjVZWpKOC1zMECwJI5O MVOyOE81QCCq NH75RYJFVVOR Mnux[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NFTJfIMzPTB|NUm2NS=>
SGC7901 MkTjR4VtdCCYaXHibYxqfHliQYPzZZk> NEXPNpkxNTFyMECgcm0> MYqyOE81QCCq MV7EUXNQ MV\k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MnzjNlUxOzV7NkG=
N87 NIrSXpBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXmwMVExODBibl2= NGGzdlQzPC92ODDo M1vFWWROW09? MonV[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NY\3b2JrOjVyM{W5OlE>
HMEC MlHlR4VtdCCYaXHibYxqfHliQYPzZZk> NH3SNowxNTFyMECgcm0> MojjNlQwPDhiaB?= NW[ze4ZbTE2VTx?= M3zuRYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXeyOVA{PTl4MR?=
HUVEC NW[0fYxtS2WubDDWbYFjcWyrdImgRZN{[Xl? MYSwMVExODBibl2= MX6yOE81QCCq M3;UcGROW09? NFXmPFNl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M1P1e|I2ODN3OU[x
MG63 M1P1TWZ2dmO2aX;uJGF{e2G7 MXS1NE0yODByIH7N MoXGNE42KGh? MlTw[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 MY[yOFg1ODF|NB?=
U2OS  MmfXSpVv[3Srb36gRZN{[Xl? NVG5bHJ[PTBvMUCwNEBvVQ>? NYPad4dDOC53IHi= MUjkc5NmKGSncHXu[IVvfGy7IDi1NQKBmzFyMECgcm0qKGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= Mn7LNlQ5PDBzM{S=
Saos-2  MXHGeY5kfGmxbjDBd5NigQ>? NHS1U|g2OC1zMECwJI5O M2fJWVAvPSCq M{LrOoRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MmLRNlQ5PDBzM{S=
Saos-2 MXTGeY5kfGmxbjDBd5NigQ>? MY[xNFAhdk1? NHjISVkxNjViaB?= M{TnNJBz\X[nboTzJI9{fGWxc3HyZ49u[SClZXzsJI1q\3KjdHnvci=> MWWyOFg1ODF|NB?=
MG63 NYnUVJFrSXCxcITvd4l{KEG|c3H5 MXGxNFAhdk1? NHnaS2U{PiCq NV76NlAyeHKxbX;0[ZMh[XCxcITvd4l{ M{TnTlI1QDRyMUO0
U2OS  MXvBdI9xfG:|aYOgRZN{[Xl? MYKxNFAhdk1? MXyzOkBp NXjKSXdveHKxbX;0[ZMh[XCxcITvd4l{ MUCyOFg1ODF|NB?=
Saos-2  M3G1bmFxd3C2b4Ppd{BCe3OjeR?= NGLYVW4yODBibl2= M124UlM3KGh? M3HBdZBzd22xdHXzJIFxd3C2b4Ppdy=> M{HMR|I1QDRyMUO0
HT1376 NY\0N|FUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPSTWM2OD1zLki4JOKyKDFwMTFOwG0> MkDJNlQxPTR6N{G=
T24 MnO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G4T2lEPTB;MT6zO{DDuSByLkSg{txO NUHRRZVNOjRyNUS4O|E>
UM-UC-3 MkXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjGdYlSUUN3ME2wMlY{KMLzMD6xJO69VQ>? NIDlbJMzPDB3NEi3NS=>
DLD-1 MmjXR4VtdCCYaXHibYxqfHliQYPzZZk> M3nYfFAuOTByMDDuUS=> M2CyPVI1KGh? MlfSbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYqyN|k6OTF5OR?=
Caco2 NX7lOGNXS2WubDDWbYFjcWyrdImgRZN{[Xl? MXiwMVExODBibl2= NVfBTlJwOjRiaB?= MUnpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NI\HVIQzOzl7MUG3PS=>
HT29 NYfEUndVS2WubDDWbYFjcWyrdImgRZN{[Xl? NI[yWm4xNTFyMECgcm0> MX[yOEBp NF\IeI1qdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEDYS2czOzl7MUG3PS=>
H116 NYC4cZdVS2WubDDWbYFjcWyrdImgRZN{[Xl? MmjsNE0yODByIH7N MkOwNlQhcA>? Mn[2bY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MVSyN|k6OTF5OR?=
Hct-8 NWPRfIhPS2WubDDWbYFjcWyrdImgRZN{[Xl? NGC1fpQxNTFyMECgcm0> MYiyOEBp NVPSU|VKcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1noR|I{QTlzMUe5
Colo320 M1HxfWNmdGxiVnnhZoltcXS7IFHzd4F6 M1zZeVAuOTByMDDuUS=> NFfpXIUzPCCq NYTEenJOcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{TLNFI{QTlzMUe5
Sw948 NV\4XoNDS2WubDDWbYFjcWyrdImgRZN{[Xl? NGjydpoxNTFyMECgcm0> M17rO|I1KGh? M1r0TolvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVSyN|k6OTF5OR?=
Colo205 NUnWRmtWS2WubDDWbYFjcWyrdImgRZN{[Xl? M1T1[lAuOTByMDDuUS=> NFjuSWczPCCq NHfIPHVqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFGwS4wzOzl7MUG3PS=>
Colo320 MnTCSpVv[3Srb36gRZN{[Xl? Mk\uNUDPxE1? Ml:xNE0zPCCq NFfnPGpi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 NGTGTHozOzl7MUG3PS=>
HT29 MX7GeY5kfGmxbjDBd5NigQ>? NXzCflNwOSEQvF2= M1izWFAuOjRiaB?= MVzhZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 Mn7RNlM6QTFzN{m=
Sw948 MojySpVv[3Srb36gRZN{[Xl? NHPlbnkyKM7:TR?= NIiyb3UxNTJ2IHi= NIDCWmpi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 MnfPNlM6QTFzN{m=
DLD-1 NFrnUmZHfW6ldHnvckBCe3OjeR?= NGr5XXcyKM7:TR?= NVnyb4QzOC1{NDDo MXPhZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 NVnCbmV1OjN7OUGxO|k>
SW620 NGDxSYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7VTWM2OD15Lkig{txO NV25S|VoOjN3NEKxO|g>
SW480 NUe3SZlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\sRmlEPTB;ND62JO69VQ>? NY\GRYV2OjN3NEKxO|g>
SK-CO-1 MkPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NED6T45KSzVyPUSg{txO MX2yN|U1OjF5OB?=
LS-513 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTNwOTFOwG0> NFzJb3kzOzV2MkG3PC=>
SW1116 NV\3enFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS5XoZyUUN3ME2wMlg1KM7:TR?= NHjk[nEzOzV2MkG3PC=>
LS-174T Mn3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\UXGg6UUN3ME2wMlg1KM7:TR?= NVW5UJFwOjN3NEKxO|g>
HCT 116 NE\YSoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnsN4VnUUN3ME2wMlQyKM7:TR?= NX\tN2w5OjN3NEKxO|g>
HCT 15 MnTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PvTWlEPTB;MD6zJO69VQ>? NFnlcGozOzV2MkG3PC=>
COLO 205 NEKwcZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{n2d2lEPTB;MD6yOEDPxE1? M2XvVVI{PTR{MUe4
HT-29 NYLtdYNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDZdopCUUN3ME2wMlI{KM7:TR?= M3;uVFI{PTR{MUe4
COLO 201 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnSWVVSUUN3ME2wMlI{KM7:TR?= NGDHcmszOzV2MkG3PC=>
Caco-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjRTWM2OD1yLkKyJO69VQ>? MUSyN|U1OjF5OB?=
SW48 NFXFdGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMEmg{txO M{[3O|I{PTR{MUe4
DND-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojxNE4zPS9yLkWvNUDPxE1? M3exPGROW09? NH\heIJqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NWi2[YZPOjN2OEK3OFg>
TMD8 NVnpcGZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzYd2kxNjJ3L{CuOU8yKM7:TR?= MWrEUXNQ MWTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MV2yN|Q5Ojd2OB?=
Jurkat MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;vZlAvOjVxMD61M|Eh|ryP M3ruVGROW09? NITlNWpqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NInDZ4ozOzR6Mke0PC=>
KOPT-K1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3tZpAxNjJ3L{CuOU8yKM7:TR?= M2jwbWROW09? Mm\ObY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MnzKNlM1QDJ5NEi=
TMD7 M1XjbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v5bFAvOjVxMD61M|Eh|ryP MkDFSG1UVw>? NYewZWVncW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MWiyN|Q5Ojd2OB?=
THP-1 NGHkbZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYixSpRROC5{NT:wMlUwOSEQvF2= NX3Fe25mTE2VTx?= MojRbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Ml7ONlM1QDJ5NEi=
786-O M3jt[WZ2dmO2aX;uJGF{e2G7 MY[wMlEwOC53IN88US=> M4nwNVI1KGh? MmSySG1UVw>? M1j4Xolv[3KnYYPld{BGNWOjZHjldolvKG2UTlGgcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHl? Mn7UNlMyPDd{NUG=
786-O M4TWSGZ2dmO2aX;uJGF{e2G7 M2K2flAuOC53IN88US=> MkDRNlQhcA>? Ml;XSG1UVw>? MlL4doV{fWy2czDpckBiKGSxc3Wg[IVx\W6mZX70JIlv[3KnYYPlJIlvKEVvY3HkbIVzcW5icILveIVqdiCneIDy[ZN{cW:wwrC= M{D6d|I{OTR5MkWx
OCI-AML3 NE\XZ4NCeG:ydH;zbZMhSXO|YYm= MmDTNk42KM7:TR?= NXu1N|RiPzJiaB?= NVPBd5dIcW6mdXPld{BieG:ydH;zbZM> MViyNlgzPjV4NR?=
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p210 BCR-Abl M1nsVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\BSXFVPDBybl2= NYH2UGNrOjRxNEigbC=> MlK5d5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= MUKyNlU3PjZyNB?=
8226 NUThN3JiTnWwY4Tpc44hSXO|YYm= NFqyXo4yODBvMUCwNEBvVQ>? M2HLcVMxKG2rbh?= MVrEUXNQ Ml\0ZYN1cX[jdHXzJGVTU8Li MUiyNlU2PjRyOR?=
MM1.S  Mn:1SpVv[3Srb36gRZN{[Xl? NGHzSVIyODBvMUCwNEBvVQ>? Ml3zN|AhdWmw NFjaNFVFVVOR MonFZYN1cX[jdHXzJGVTU8Li NX;zfmFzOjJ3NU[0NFk>
8226 M2LKeWZ2dmO2aX;uJGF{e2G7 M{\GdVAvPSEQvF2= NF7ufng{OCCvaX6= M1KxemROW09? MnTmbY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= Mmf3NlI2PTZ2MEm=
MM1.S  NEPMSIVHfW6ldHnvckBCe3OjeR?= NGrPfmIxNjVizszN NEHnUnE{OCCvaX6= M1\3UWROW09? M{WzS4lv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= NWXzRlh3OjJ3NU[0NFk>
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T47D MmfSSpVv[3Srb36gRZN{[Xl? NILDSVQ2OC9{MECvOVAxKG6P NV\vdVV5OzBibXnu NXGzN3hz\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? M{LyXlIzPDd4OEWy
MDA-MB-231 MYfGeY5kfGmxbjDBd5NigQ>? MUK1NE8zODBxNUCwJI5O M{L4elMxKG2rbh?= NHLR[mpld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? NX;6SWRGOjJ2N{[4OVI>
Bcap-37 MoDBSpVv[3Srb36gRZN{[Xl? MXu1NE8zODBxNUCwJI5O MojZN|AhdWmw M{LsWYRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 NIGxSWwzOjR5Nki1Ni=>
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MDA-MB-231 MWLBdI9xfG:|aYOgRZN{[Xl? MXqyNFDDqG6P MXyzOkBp NWPGOINlTE2VTx?= MkX6bY5lfWOnczDhdI9xfG:|aYO= MnPINlI1PzZ6NUK=
Bcap-37 MWfBdI9xfG:|aYOgRZN{[Xl? MlzqNlAxyqCwTR?= MnTmN|YhcA>? NGTkXoZFVVOR NWfYeoI1cW6mdXPld{BieG:ydH;zbZM> M1r5UFIzPDd4OEWy
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DLD-1  M1K2c2Z2dmO2aX;uJGF{e2G7 MUGxNE8yODBxMUCwNEBvVQ>? MVK2JIg> M2rZcWROW09? MXvpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu M2nG[lIzPDBzMkm0
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SW620 MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjlTWM2OD1zMTFOwG0> NUXldXZmOjJ{N{CyOVc>
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NIH 3T3 NH7qZ49HfW6ldHnvckBCe3OjeR?= MlzaNkDPxE1? M1H4T|E5KGh? MmDYbY5pcWKrdIOgcXRQWkN{IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qhd25iU3XyOFc{KGGwZDDtWG9TSzFicHjvd5Bpd3K7bHH0bY9vKG:oIETFMWJROSCxbjDUbJI{Py92Nh?= MnflNlE5PzZzM{C=
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... 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
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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
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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
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  • 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