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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Cited by 43 Publications

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 MmC1SpVv[3Srb36gRZN{[Xl? MmqxOVAuOTJ3MDDuUS=> NX:0dYNOOjRiaB?= M1zLPGROW09? NFOxToFqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZia3nuZZNmKCi2YYLn[ZQhd2ZibWTPVmMyMSCjbnSgbZR{KGSxd37zeJJm[W1idHHy[4V1KHCqb4PwbI8uWzcEoB?= Mn2xNlYyPzdyNUG=
U87vIII  M2rnXGZ2dmO2aX;uJGF{e2G7 M1jlTFAvODRvMj61JO69VQ>? NUnt[YwxOjRiaB?= MnfKbY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh MlTtNlYyOzR4MUe=
U87vIII  MWrGeY5kfGmxbjDBd5NigQ>? M4j6c|IvPS93IN88US=> MYmxNkBp Ml3JbY5pcWKrdIOg[4FxKGOub4PpcochcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NIe2cFAzPjF|NE[xOy=>
PC12  MlPWSpVv[3Srb36gRZN{[Xl? NGPmU281OMLibl2= NWT4fmJLcW6mdXPld{BtgXOxc3;tZYwh[mmxZ3Xu[ZNqeyCjbnSgZYxt\X[rYYTl[EDPuS2VWV6gZYNkfW23bHH0bY9vyqB? NF7CW24zPjByMU[xOC=>
3T3-L1 NIPjOZZHfW6ldHnvckBCe3OjeR?= NGfFNFAyPSEQvF2= NX3vVpMyPCCq NFrZOWJ{fXCycnXzd4V{KGW6cILld5Nqd25ib3[geIhmKEWpckGgdJJwfGWrbtMg MnPJNlU5OTR4NkK=
Rh30 NVXweY1oTnWwY4Tpc44hSXO|YYm= MV2xJO69VQ>? NWe3N5BKOiCq NUTyRVZkcW6qaXLpeJMh[m:2aDDtWG9TSzFvbXXkbYF1\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGO2T|Eh[W6mIH3UU3JEOi2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M3iyZ|I2PzZ{NkG5
HT29 MlXYSpVv[3Srb36gRZN{[Xl? M3O5NlEh|ryP NXH4TWdIOiCq NYTBXIg5cW6qaXLpeJMh[m:2aDDtWG9TSzFvbXXkbYF1\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGO2T|Eh[W6mIH3UU3JEOi2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M1:xV|I2PzZ{NkG5
Rh30 NUTFfZF7TnWwY4Tpc44hSXO|YYm= MWmxJO69VQ>? NXPtZmx5OiCq NITX[ll{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> NIfMRXUzPTd4Mk[xPS=>
HT29 MkjnSpVv[3Srb36gRZN{[Xl? MXexJO69VQ>? NHXLfoMzKGh? M1fmeZN2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> NU\mS49qOjV5NkK2NVk>
U87 MoT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XiclI2KG6P NFfXRXozPCCq MnHVbY5kemWjc3XzJGRWW1BzMDDrco9kc2WmLXTve44hcW6mdXPl[EBk\WyuIHnubIljcXSrb36= NXv2N|Q3OjV3Nki2OlU>
AGS NWrWPGVuS2WubDDWbYFjcWyrdImgRZN{[Xl? NVjn[ldQOC1zMECwJI5O M2TkelI1NzR6IHi= MWLEUXNQ MXLk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M1\oVFI2ODN3OU[x
MKN45 NXPEdHR3S2WubDDWbYFjcWyrdImgRZN{[Xl? MV[wMVExODBibl2= M3HjfVI1NzR6IHi= M3fhT2ROW09? NGnaZXBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M2nBcVI2ODN3OU[x
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KATO3 NVTEZmp{S2WubDDWbYFjcWyrdImgRZN{[Xl? M3vtNFAuOTByMDDuUS=> MXyyOE81QCCq MUjEUXNQ M4DoTIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NH7TbFQzPTB|NUm2NS=>
SGC7901 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmKxNE0yODByIH7N MVGyOE81QCCq MYrEUXNQ M33CfoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NWHaUIg3OjVyM{W5OlE>
N87 MkPQR4VtdCCYaXHibYxqfHliQYPzZZk> MnHTNE0yODByIH7N NH;FdWMzPC92ODDo MlXySG1UVw>? Mlv5[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M1LrN|I2ODN3OU[x
HMEC M4HrbGNmdGxiVnnhZoltcXS7IFHzd4F6 NW\2NGtbOC1zMECwJI5O MUWyOE81QCCq NXrQ[G1wTE2VTx?= MljZ[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NV3uNnhtOjVyM{W5OlE>
HUVEC NGO4RmRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1LwXFAuOTByMDDuUS=> NXuwUmc2OjRxNEigbC=> MlPuSG1UVw>? M4H1eIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Mn\MNlUxOzV7NkG=
MG63 Ml6zSpVv[3Srb36gRZN{[Xl? M1noSVUxNTFyMECgcm0> NEDjcncxNjViaB?= NXfOUmds\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 NWnLZYQyOjR6NECxN|Q>
U2OS  MnPjSpVv[3Srb36gRZN{[Xl? NG[2U5Y2OC1zMECwJI5O Mlu5NE42KGh? NXvMe2ZT\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 NF\kb4MzPDh2MEGzOC=>
Saos-2  MUDGeY5kfGmxbjDBd5NigQ>? MVS1NE0yODByIH7N MV:wMlUhcA>? M1v6ToRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NEXoV3QzPDh2MEGzOC=>
Saos-2 M{H3ZmZ2dmO2aX;uJGF{e2G7 MVKxNFAhdk1? M4H0[VAvPSCq MW\wdoV3\W62czDvd5Rmd3OjcnPvcYEh[2WubDDtbYdz[XSrb36= Mn3iNlQ5PDBzM{S=
MG63 NEPvOIFCeG:ydH;zbZMhSXO|YYm= M1jHOFExOCCwTR?= MlHSN|YhcA>? NGX2NI1xem:vb4Tld{BieG:ydH;zbZM> MXSyOFg1ODF|NB?=
U2OS  MXjBdI9xfG:|aYOgRZN{[Xl? NEPaZoEyODBibl2= NXXidYFoOzZiaB?= NFnzZ3Rxem:vb4Tld{BieG:ydH;zbZM> MYmyOFg1ODF|NB?=
Saos-2  MknwRZBweHSxc3nzJGF{e2G7 MlrWNVAxKG6P NV61clBFOzZiaB?= MkDudJJwdW:2ZYOgZZBweHSxc3nz NUHXZYtJOjR6NECxN|Q>
HT1376 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrwUVRKSzVyPUGuPFghyrFiMT6xJO69VQ>? MX6yOFA2PDh5MR?=
T24 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjENnFtUUN3ME2xMlM4KMLzIECuOEDPxE1? NFn1SYUzPDB3NEi3NS=>
UM-UC-3 MmPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDvOGtRUUN3ME2wMlY{KMLzMD6xJO69VQ>? M{nydFI1ODV2OEex
DLD-1 NFnufpFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVL2[mU4OC1zMECwJI5O NHfEU4czPCCq Mo[0bY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWXHOpc{OjN7OUGxO|k>
Caco2 NYfhUIlpS2WubDDWbYFjcWyrdImgRZN{[Xl? M1\NdVAuOTByMDDuUS=> M{ntO|I1KGh? M1Xke4lvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVWyN|k6OTF5OR?=
HT29 MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1n5PVAuOTByMDDuUS=> MXyyOEBp NEHoc3hqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXqyN|k6OTF5OR?=
H116 NHjlXIxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUewMVExODBibl2= M3\nOlI1KGh? M{HZWYlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVPXTHhrOjN7OUGxO|k>
Hct-8 NE\ncItE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NG\ITpAxNTFyMECgcm0> MVSyOEBp NYn6SnJ6cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4XwOlI{QTlzMUe5
Colo320 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1nkflAuOTByMDDuUS=> M3TKRVI1KGh? NIn3Z3FqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3fu[VI{QTlzMUe5
Sw948 MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUnKfHZxOC1zMECwJI5O NEPxZY4zPCCq M1jFNolvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2ryO|I{QTlzMUe5
Colo205 MljGR4VtdCCYaXHibYxqfHliQYPzZZk> MUiwMVExODBibl2= MoK2NlQhcA>? MWHpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2LoR|I{QTlzMUe5
Colo320 M{DNd2Z2dmO2aX;uJGF{e2G7 MVGxJO69VQ>? NGD3OJExNTJ2IHi= MnKyZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> NFfz[IgzOzl7MUG3PS=>
HT29 MmnMSpVv[3Srb36gRZN{[Xl? Mne1NUDPxE1? NIPw[GwxNTJ2IHi= M2XPV4Fjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> M1;lZlI{QTlzMUe5
Sw948 MmG1SpVv[3Srb36gRZN{[Xl? M2L3RVEh|ryP NEDEXY8xNTJ2IHi= MnHVZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> MXSyN|k6OTF5OR?=
DLD-1 MnT1SpVv[3Srb36gRZN{[Xl? MnPpNUDPxE1? MX[wMVI1KGh? M{fIcIFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> Mm[0NlM6QTFzN{m=
SW620 MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTBeXozUUN3ME23Mlgh|ryP NXLFd|hFOjN3NEKxO|g>
SW480 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7XdG9jUUN3ME20MlYh|ryP M2r4SFI{PTR{MUe4
SK-CO-1 NHLiXoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zMTWlEPTB;NDFOwG0> MmX6NlM2PDJzN{i=
LS-513 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XmXGlEPTB;Mz65JO69VQ>? NXvsVmw3OjN3NEKxO|g>
SW1116 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFX5XHNKSzVyPUCuPFQh|ryP NGDUZWEzOzV2MkG3PC=>
LS-174T NFjOTHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jrU2lEPTB;MD64OEDPxE1? M2L1fFI{PTR{MUe4
HCT 116 NIHKVZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\ITWlEPTB;MD60NUDPxE1? NGLyXpczOzV2MkG3PC=>
HCT 15 NGWzbnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nQc2lEPTB;MD6zJO69VQ>? MmXoNlM2PDJzN{i=
COLO 205 M1qyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;5[pNuUUN3ME2wMlI1KM7:TR?= NH\QUFgzOzV2MkG3PC=>
HT-29 NEf0NJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPYOWtmUUN3ME2wMlI{KM7:TR?= MnO5NlM2PDJzN{i=
COLO 201 Mor5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV61O2JVUUN3ME2wMlI{KM7:TR?= MWCyN|U1OjF5OB?=
Caco-2 M1Hie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ezb2lEPTB;MD6yNkDPxE1? NV;yOHdqOjN3NEKxO|g>
SW48 NXTiXWMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjDVpdKSzVyPUCuNFkh|ryP MojFNlM2PDJzN{i=
DND-1 M2nBeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG2cGMxNjJ3L{CuOU8yKM7:TR?= M4fzTWROW09? NVnxXIJCcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M2i5PFI{PDh{N{S4
TMD8 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnaeWo5OC5{NT:wMlUwOSEQvF2= M3\vTmROW09? Mlq4bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NULuVJJzOjN2OEK3OFg>
Jurkat NEDYblZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\ZTndZOC5{NT:wMlUwOSEQvF2= NWHwWWR4TE2VTx?= MVHpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NGLwPZkzOzR6Mke0PC=>
KOPT-K1 NGKze2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmwMlI2NzBwNT:xJO69VQ>? M1LrPGROW09? MnHQbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MljaNlM1QDJ5NEi=
TMD7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFqyR5UxNjJ3L{CuOU8yKM7:TR?= NWflfXU4TE2VTx?= MlnrbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NGDDbIIzOzR6Mke0PC=>
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786-O Mm\vSpVv[3Srb36gRZN{[Xl? MlmzNE0xNjVizszN NVvhfpFTOjRiaB?= MULEUXNQ Ml;5doV{fWy2czDpckBiKGSxc3Wg[IVx\W6mZX70JIlv[3KnYYPlJIlvKEVvY3HkbIVzcW5icILveIVqdiCneIDy[ZN{cW:wwrC= NX75[HlUOjNzNEeyOVE>
OCI-AML3 NFnHPFVCeG:ydH;zbZMhSXO|YYm= MXOyMlUh|ryP MnmyO|IhcA>? Moj1bY5lfWOnczDhdI9xfG:|aYO= NYfZUFVvOjJ6Mk[1OlU>
Jurkat M{\ycWZ2dmO2aX;uJGF{e2G7 NFnkfGEyODBxMkCwM|QxOCCwTR?= MlfYNVghcA>? MnX1bY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= M3zPRVIzPTZ4NkC0
p210 BCR-Abl MnPoSpVv[3Srb36gRZN{[Xl? NX;nVmx5OTByL{KwNE81ODBibl2= M3X3UVE5KGh? MXrpcohq[mm2czDtWG9TSzFvZHXw[Y5l\W62IGO2JHMzOzVxMkO2JJBpd3OyaH;yfYxifGmxbh?= MYKyNlU3PjZyNB?=
Jurkat MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\sdm14PDBybl2= NWeyZ5ZpOjRxNEigbC=> MWDzfY5memerenWge4l1cCBzNz3BRWchfG9ic4XwdJJme3NiY3XscEBxem:uaX\ldoF1cW:w MmnGNlI2PjZ4MES=
p210 BCR-Abl MoLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTCOFAxdk1? M4nmW|I1NzR6IHi= Mmn2d5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= Mlu4NlI2PjZ4MES=
8226 MYjGeY5kfGmxbjDBd5NigQ>? M33MVlExOC1zMECwJI5O MX[zNEBucW5? NETIW21FVVOR M{DKdoFkfGm4YYTld{BGWkwEoB?= NH7RTIgzOjV3NkSwPS=>
MM1.S  NXPsemtqTnWwY4Tpc44hSXO|YYm= M3vhb|ExOC1zMECwJI5O M{LTbFMxKG2rbh?= M2C2bGROW09? M1W3[oFkfGm4YYTld{BGWkwEoB?= NGrWUnczOjV3NkSwPS=>
8226 MnvoSpVv[3Srb36gRZN{[Xl? NUj4OYhjOC53IN88US=> MVSzNEBucW5? MkHPSG1UVw>? M1foZYlv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= MnLnNlI2PTZ2MEm=
MM1.S  NYmyO3pGTnWwY4Tpc44hSXO|YYm= NUPSbIU4OC53IN88US=> NX3s[XlYOzBibXnu NHnyVXdFVVOR M3TQZolv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= MnnsNlI2PTZ2MEm=
MCF-7 MUTGeY5kfGmxbjDBd5NigQ>? NX;sVWpGPTBxMkCwM|UxOCCwTR?= MVyzNEBucW5? NGXocoFld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? NFjp[VMzOjR5Nki1Ni=>
T47D MWDGeY5kfGmxbjDBd5NigQ>? NX;LR2tnPTBxMkCwM|UxOCCwTR?= MkXBN|AhdWmw M2jQbIRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MViyNlQ4Pjh3Mh?=
MDA-MB-231 MVLGeY5kfGmxbjDBd5NigQ>? M3;LT|UxNzJyMD:1NFAhdk1? MmrDN|AhdWmw M1m1[oRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MlLjNlI1PzZ6NUK=
Bcap-37 NWfZU|Z[TnWwY4Tpc44hSXO|YYm= NGnBWXg2OC9{MECvOVAxKG6P MoDKN|AhdWmw NUjtOpFx\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? NUXrSlJkOjJ2N{[4OVI>
MCF-7 NVK1coQzSXCxcITvd4l{KEG|c3H5 NUHEXndVOjBywrDuUS=> NHTPbVA{PiCq NVm0fmlUTE2VTx?= MnzvbY5lfWOnczDhdI9xfG:|aYO= MmjzNlI1PzZ6NUK=
MDA-MB-231 NILlRYpCeG:ydH;zbZMhSXO|YYm= NXjVbJp3OjBywrDuUS=> Ml7RN|YhcA>? NF\tOJJFVVOR NHrMU3pqdmS3Y3XzJIFxd3C2b4Ppdy=> Mlm5NlI1PzZ6NUK=
Bcap-37 NHLpdW1CeG:ydH;zbZMhSXO|YYm= NH3pV5YzODEEoH7N NEjqfXU{PiCq NEn6XoFFVVOR NWroRZNjcW6mdXPld{BieG:ydH;zbZM> M1HGPFIzPDd4OEWy
LS174T M{DvXmZ2dmO2aX;uJGF{e2G7 MVGxNE8yODBxMUCwNEBvVQ>? M1S4Z|YhcA>? Mlr4SG1UVw>? NEfHW|NqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv NVnUc|hSOjJ2MEGyPVQ>
DLD-1  M13LXmZ2dmO2aX;uJGF{e2G7 Mo\vNVAwOTByL{GwNFAhdk1? MoTPOkBp NYH1cY5zTE2VTx?= M3f5XolvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> MV6yNlQxOTJ7NB?=
SW480 NE\yNWdHfW6ldHnvckBCe3OjeR?= NXHxSpRVOTBxMUCwM|ExODBibl2= MWq2JIg> NFnNPIpFVVOR NHfvbYVqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv M4XOeFIzPDBzMkm0
SW-48 MlXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwMTFOwG0> MWCyNlI4ODJ3Nx?=
HCT-15 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXHTWM2OD1yLkOg{txO MlTtNlIzPzB{NUe=
HCT 116 Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:4TWM2OD1yLk[g{txO MnTjNlIzPzB{NUe=
SW620-R NFv5N4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLBTWM2OD1zLkOg{txO NEHjdZozOjJ5MEK1Oy=>
SK-CO-1 NV\jdGVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjnfJRSUUN3ME2yMlEh|ryP MlLNNlIzPzB{NUe=
SW620 M3HGbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTFzIN88US=> MmjVNlIzPzB{NUe=
BaF3 NGnNdW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnjS2k2OD1zLkS0PUDPxE1? NYDaU3RYOjJ{MkO2OFU>
NIH 3T3 NWfkWnBuTnWwY4Tpc44hSXO|YYm= MofKNkDPxE1? MUixPEBp M2\GOIlvcGmkaYTzJI1VV1KFMjDwbI9{eGixconsZZRqd25ib3[gRYt1KG:wIGPldlQ4OyCjbnSgcXRQWkNzIIDoc5NxcG:{eXzheIlwdiCxZjC0SU1DWDFib36gWIhzOzdxNE[= NVXvOIU{OjF6N{[xN|A>
HCT15 M1mxdGZ2dmO2aX;uJGF{e2G7 NX[5NmptOC53L{Kg{txO NHnTVnE1KGh? MnLOdJJmfmWwdIOgV|ZMOSCyaH;zdIhwenmuYYTpc44hd2Zicnnic5NwdWGuIIDyc5RmcW5iU{[gZZQhW2W{MkSwM|I1PCCjbnSgcXRQWkN{IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qh[XRiU3XyOFc{ NF3wO4szOTh5NkGzNC=>
SW620  NX7M[2xuTnWwY4Tpc44hSXO|YYm= MYmwMlUwOiEQvF2= MkH4OEBp MWficI9kc3NiYXzsJJRpemWnIH3UU3Ihd3W2cIX0dy=> NHLFdmMzOTh5NkGzNC=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-mTOR / mTOR / p-AKT / AKT / p-S6 / S6 / p-4E-BP1 / 4E-BP-1 ; 

PubMed: 23991179     


Each of the cell lines as indicated to the top of the panel were untreated or treated with PP242 (1 μM) for the indicated hours and then examined by western blotting using antibodies against the phosphorylated (p-) and unphosphorylated proteins as indicated to the left of the panel.

23991179
Growth inhibition assay
Cell viability ; 

PubMed: 23991179     


The colorectal carcinoma cell lines as indicated were treated with PP242 in the indicated concentrations and then subjected to cell viability assay. The experiment was repeated three times and the data presented as mean ± SD (standard deviation).

23991179
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]
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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:[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]
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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 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 (mg) = Concentration (mM) × Volume (mL) × 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.

  • * 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID