Torkinib (PP242)

For research use only.

Catalog No.S2218

48 publications

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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Selleck's Torkinib (PP242) has been cited by 48 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 NXX5[5RjTnWwY4Tpc44hSXO|YYm= NGHmfYI2OC1zMkWwJI5O NUf5NJA5OjRiaB?= M{jybmROW09? MVzpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Yhc2mwYYPlJEh1[XKpZYSgc4YhdVSRUlOxLUBidmRiaYTzJIRwf26|dILlZY0hfGG{Z3X0JJBpd3OyaH:tV|bDqA>? NVu2N|VjOjZzN{ewOVE>
U87vIII  NGrw[4pHfW6ldHnvckBCe3OjeR?= M1vPbVAvODRvMj61JO69VQ>? M37F[|I1KGh? M2PvWolvcGmkaYTzJI1VV1KFMTDhcoQhdVSRUlOyJIFkfGm4aYTp[ZPDqA>? MmfkNlYyOzR4MUe=
U87vIII  M1nl[2Z2dmO2aX;uJGF{e2G7 NGXGcW8zNjVxNTFOwG0> MUOxNkBp NGLiZ25qdmirYnn0d{Bo[XBiY3zvd4lv\yCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXHhUI9IOjZzM{S2NVc>
PC12  Mm\kSpVv[3Srb36gRZN{[Xl? MV:0NOKhdk1? M4PMW4lv\HWlZYOgcJl{d3OxbXHsJIJqd2enbnXzbZMh[W6mIHHscIV3cWG2ZXSg{tEuW1mQIHHjZ5VufWyjdHnvcuKh NFfhXYQzPjByMU[xOC=>
3T3-L1 MmnOSpVv[3Srb36gRZN{[Xl? MmjMNVUh|ryP MlXHOEBp NXK0OnlYe3WycILld5NmeyCneIDy[ZN{cW:wIH;mJJRp\SCHZ4KxJJBzd3SnaX9CpC=> NULmRo9SOjV6MUS2OlI>
Rh30 MUDGeY5kfGmxbjDBd5NigQ>? NY\sU|VkOSEQvF2= NEjMeGMzKGh? M1:yZ4lvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= NVfYVGlCOjV5NkK2NVk>
HT29 NEXKVZFHfW6ldHnvckBCe3OjeR?= NWTlS5RMOSEQvF2= MYCyJIg> M4njb4lvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= MV6yOVc3OjZzOR?=
Rh30 NYLaUZBjTnWwY4Tpc44hSXO|YYm= M4PN[VEh|ryP NH\LenQzKGh? NUjMZZA4e3WycILld5NmeyC2aHWgZoF{[Wxib4KgTWdHNTFvc4TpcZVt[XSnZDDj[YxtKGGmaHXzbY9v MoDVNlU4PjJ4MUm=
HT29 MlTJSpVv[3Srb36gRZN{[Xl? MX[xJO69VQ>? MVWyJIg> MUfzeZBxemW|c3XzJJRp\SCkYYPhcEBweiCLR1[tNU1{fGmvdXzheIVlKGOnbHygZYRp\XOrb36= M2nhZ|I2PzZ{NkG5
U87 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfTV2FCOjVibl2= NHPN[JMzPCCq M{TvPIlv[3KnYYPld{BFXVOSMUCgb45w[2unZD3kc5dvKGmwZIXj[YQh[2WubDDpcohq[mm2aX;u NXfuS3ZCOjV3Nki2OlU>
AGS NVOyS29JS2WubDDWbYFjcWyrdImgRZN{[Xl? M4HZSFAuOTByMDDuUS=> Mk[yNlQwPDhiaB?= NWnON4JQTE2VTx?= M3Pp[IRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3fVb|I2ODN3OU[x
MKN45 NFjoOHNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEHLOXAxNTFyMECgcm0> M1LKZVI1NzR6IHi= NE\K[FZFVVOR MkXX[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHGzdW8zPTB|NUm2NS=>
MKN28 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmPWNE0yODByIH7N MVyyOE81QCCq MXrEUXNQ NUCxRVZs\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NGHTd5AzPTB|NUm2NS=>
KATO3 MnyxR4VtdCCYaXHibYxqfHliQYPzZZk> M4XIS|AuOTByMDDuUS=> M3uydFI1NzR6IHi= MV3EUXNQ NHm0fZJl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ Mn7iNlUxOzV7NkG=
SGC7901 M4j0VGNmdGxiVnnhZoltcXS7IFHzd4F6 Ml;LNE0yODByIH7N NF3uR2EzPC92ODDo NULhW2JuTE2VTx?= NVfnZ|Nz\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MVKyOVA{PTl4MR?=
N87 NGLHTFFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3;mWlAuOTByMDDuUS=> M2HZUVI1NzR6IHi= M4ftc2ROW09? MlHj[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MnT6NlUxOzV7NkG=
HMEC NUfofndwS2WubDDWbYFjcWyrdImgRZN{[Xl? NWCz[G02OC1zMECwJI5O M3j2T|I1NzR6IHi= M1S4NGROW09? Mmno[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M1XtdVI2ODN3OU[x
HUVEC M2fnTGNmdGxiVnnhZoltcXS7IFHzd4F6 MnXRNE0yODByIH7N NGXSRm0zPC92ODDo M1z3WGROW09? NUDBZ4tH\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NHrUXYozPTB|NUm2NS=>
MG63 MkXCSpVv[3Srb36gRZN{[Xl? M3vwelUxNTFyMECgcm0> NXnEOnFbOC53IHi= MkXZ[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 MoL6NlQ5PDBzM{S=
U2OS  NGPvZXlHfW6ldHnvckBCe3OjeR?= NYW3e4F3PTBvMUCwNEBvVQ>? MlW5NE42KGh? Mljq[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 MoXINlQ5PDBzM{S=
Saos-2  MUnGeY5kfGmxbjDBd5NigQ>? MkXxOVAuOTByMDDuUS=> MoHxNE42KGh? M1PyNIRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M37QeFI1QDRyMUO0
Saos-2 NV70RYJITnWwY4Tpc44hSXO|YYm= Mn\zNVAxKG6P NF;zdncxNjViaB?= Ml\wdJJmfmWwdIOgc5N1\W:|YYLjc41iKGOnbHygcYloemG2aX;u NUnh[pd7OjR6NECxN|Q>
MG63 M3TtPWFxd3C2b4Ppd{BCe3OjeR?= NYPaNlJ[OTByIH7N MUOzOkBp NHvheplxem:vb4Tld{BieG:ydH;zbZM> MkLwNlQ5PDBzM{S=
U2OS  Mnq5RZBweHSxc3nzJGF{e2G7 MWixNFAhdk1? NHTJfWs{PiCq MULwdo9ud3SnczDhdI9xfG:|aYO= MkjFNlQ5PDBzM{S=
Saos-2  NXnuSno3SXCxcITvd4l{KEG|c3H5 M{myUlExOCCwTR?= M{LYbFM3KGh? NXW2SGJNeHKxbX;0[ZMh[XCxcITvd4l{ MXWyOFg1ODF|NB?=
HT1376 NIXtR4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnmdVNKSzVyPUGuPFghyrFiMT6xJO69VQ>? MknKNlQxPTR6N{G=
T24 MoSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[3bZhKSzVyPUGuN|chyrFiMD60JO69VQ>? MV:yOFA2PDh5MR?=
UM-UC-3 NEjS[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:xTWM2OD1yLk[zJOKyOC5zIN88US=> M2nSXFI1ODV2OEex
DLD-1 MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MofHNE0yODByIH7N NWjSO45wOjRiaB?= NX7m[|UycW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVnRTGNoOjN7OUGxO|k>
Caco2 MmruR4VtdCCYaXHibYxqfHliQYPzZZk> MV[wMVExODBibl2= NGTCOHYzPCCq Mln4bY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUT2S|RKOjN7OUGxO|k>
HT29 M1nDcWNmdGxiVnnhZoltcXS7IFHzd4F6 M2O0bVAuOTByMDDuUS=> M4PTXVI1KGh? NWH6SYI3cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4XnSVI{QTlzMUe5
H116 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXvM[JAzOC1zMECwJI5O NXLnbG14OjRiaB?= NWLpUppqcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFPGNGQzOzl7MUG3PS=>
Hct-8 M4mwZmNmdGxiVnnhZoltcXS7IFHzd4F6 NHzxUFcxNTFyMECgcm0> NGGwdZMzPCCq MkPkbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2e1[lI{QTlzMUe5
Colo320 NUnqSnRGS2WubDDWbYFjcWyrdImgRZN{[Xl? NV3QfVFSOC1zMECwJI5O NGD1e|UzPCCq M2LqPYlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MX[yN|k6OTF5OR?=
Sw948 MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1fobFAuOTByMDDuUS=> NGThbIszPCCq NVT1NnhlcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVqyN|k6OTF5OR?=
Colo205 NFywd5RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NInpOlMxNTFyMECgcm0> NVL2cIFsOjRiaB?= MUXpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MmHtNlM6QTFzN{m=
Colo320 NX3ZR404TnWwY4Tpc44hSXO|YYm= MYKxJO69VQ>? MlLpNE0zPCCq NUS3[2ZJ[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MnPNNlM6QTFzN{m=
HT29 MVzGeY5kfGmxbjDBd5NigQ>? NWTSXFFsOSEQvF2= MnfFNE0zPCCq NEG2blVi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 NFrTfJMzOzl7MUG3PS=>
Sw948 NYfZZZhkTnWwY4Tpc44hSXO|YYm= MX[xJO69VQ>? M3HSSlAuOjRiaB?= M4G5NYFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> NEXpTFAzOzl7MUG3PS=>
DLD-1 NGi4PGpHfW6ldHnvckBCe3OjeR?= MXSxJO69VQ>? MY[wMVI1KGh? NX7XU5hv[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MnfXNlM6QTFzN{m=
SW620 NHv0eolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPXTWM2OD15Lkig{txO NGXiXoYzOzV2MkG3PC=>
SW480 NV\3Rlh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTRwNjFOwG0> NVjmdWFLOjN3NEKxO|g>
SK-CO-1 NF;ZfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3ve4UyUUN3ME20JO69VQ>? MmHnNlM2PDJzN{i=
LS-513 NU\yXnNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXG4S21CUUN3ME2zMlkh|ryP MUCyN|U1OjF5OB?=
SW1116 NIHxdHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXyTWM2OD1yLki0JO69VQ>? Mmn5NlM2PDJzN{i=
LS-174T MmfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWS3SHhGUUN3ME2wMlg1KM7:TR?= NE\kOGwzOzV2MkG3PC=>
HCT 116 MoPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33KNmlEPTB;MD60NUDPxE1? M3nBVFI{PTR{MUe4
HCT 15 NWHnVoFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFr3fnlKSzVyPUCuN{DPxE1? MXqyN|U1OjF5OB?=
COLO 205 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPNTINKSzVyPUCuNlQh|ryP M3HaTFI{PTR{MUe4
HT-29 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnCdYw5UUN3ME2wMlI{KM7:TR?= NUnrcpFGOjN3NEKxO|g>
COLO 201 Mn64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfEVmZKSzVyPUCuNlMh|ryP MViyN|U1OjF5OB?=
Caco-2 NHLBNGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPkclRiUUN3ME2wMlIzKM7:TR?= MUmyN|U1OjF5OB?=
SW48 MojRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwMEmg{txO NE\N[pozOzV2MkG3PC=>
DND-1 NWPORlM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:wMlI2NzBwNT:xJO69VQ>? NVHjb2M1TE2VTx?= MknzbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M{\yU|I{PDh{N{S4
TMD8 NUjnTFJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DNNVAvOjVxMD61M|Eh|ryP NHrpVW5FVVOR MX;pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NFvHSHUzOzR6Mke0PC=>
Jurkat NG\TPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfye5IxNjJ3L{CuOU8yKM7:TR?= MVPEUXNQ MWHpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MonLNlM1QDJ5NEi=
KOPT-K1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTENE4zPS9yLkWvNUDPxE1? MnjRSG1UVw>? MlS5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NULIRotXOjN2OEK3OFg>
TMD7 M37kfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjYPGFTOC5{NT:wMlUwOSEQvF2= MXfEUXNQ NHrTdY5qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NFjXU3AzOzR6Mke0PC=>
THP-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP4NE4zPS9yLkWvNUDPxE1? NGrVe5dFVVOR NWLCbIVHcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NH;2VYQzOzR6Mke0PC=>
786-O MkHkSpVv[3Srb36gRZN{[Xl? M3TDPFAvOS9yLkWg{txO NF;mV2czPCCq M{SwUmROW09? M4XzcIlv[3KnYYPld{BGNWOjZHjldolvKG2UTlGgcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHl? M3T5O|I{OTR5MkWx
786-O NHHBU5FHfW6ldHnvckBCe3OjeR?= M{nVblAuOC53IN88US=> MWWyOEBp NYj5RotkTE2VTx?= NX\mXG8yemW|dXz0d{BqdiCjIHTvd4Uh\GWyZX7k[Y51KGmwY4LlZZNmKGmwIFWtZ4FlcGW{aX6gdJJwfGWrbjDlfJBz\XO|aX;uxsA> NF30U5UzOzF2N{K1NS=>
OCI-AML3 NULpRnhTSXCxcITvd4l{KEG|c3H5 NXfXU2duOi53IN88US=> NXj4b3dYPzJiaB?= NU\0SodKcW6mdXPld{BieG:ydH;zbZM> NX;DNmlROjJ6Mk[1OlU>
Jurkat M{jrd2Z2dmO2aX;uJGF{e2G7 NF;uNYEyODBxMkCwM|QxOCCwTR?= MmPnNVghcA>? MleybY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= NX:yRWFnOjJ3Nk[2NFQ>
p210 BCR-Abl MVHGeY5kfGmxbjDBd5NigQ>? NULiPIZYOTByL{KwNE81ODBibl2= MmXsNVghcA>? MoTPbY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= MVmyNlU3PjZyNB?=
Jurkat M134Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;COFAxdk1? MWmyOE81QCCq NHnHXVh{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u MUmyNlU3PjZyNB?=
p210 BCR-Abl NV[1WlBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDSWoU{PDBybl2= M1nRNVI1NzR6IHi= M{P0NZN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= MYWyNlU3PjZyNB?=
8226 Mly0SpVv[3Srb36gRZN{[Xl? M{C5XFExOC1zMECwJI5O MYKzNEBucW5? NU\pWGt5TE2VTx?= MUnhZ5RqfmG2ZYOgSXJMyqB? NVrETG1bOjJ3NU[0NFk>
MM1.S  MWTGeY5kfGmxbjDBd5NigQ>? M3zGOVExOC1zMECwJI5O NHy1VY4{OCCvaX6= NYS1cXZvTE2VTx?= MnTGZYN1cX[jdHXzJGVTU8Li MoflNlI2PTZ2MEm=
8226 MYDGeY5kfGmxbjDBd5NigQ>? NEewT4gxNjVizszN NFLJfoE{OCCvaX6= MYLEUXNQ Mlv0bY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= Mlf2NlI2PTZ2MEm=
MM1.S  MorESpVv[3Srb36gRZN{[Xl? NF62TWkxNjVizszN MYqzNEBucW5? NFL6ZmJFVVOR MnOybY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= MXeyNlU2PjRyOR?=
MCF-7 MUXGeY5kfGmxbjDBd5NigQ>? NELsfHg2OC9{MECvOVAxKG6P MoPQN|AhdWmw Mlr5[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> M37hWFIzPDd4OEWy
T47D MXfGeY5kfGmxbjDBd5NigQ>? MnPxOVAwOjByL{WwNEBvVQ>? M2[1W|MxKG2rbh?= MoPx[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NXj2RWZ5OjJ2N{[4OVI>
MDA-MB-231 NF3leYpHfW6ldHnvckBCe3OjeR?= MnfnOVAwOjByL{WwNEBvVQ>? NIHuXms{OCCvaX6= NUe1[IFV\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MYCyNlQ4Pjh3Mh?=
Bcap-37 NGTqVJNHfW6ldHnvckBCe3OjeR?= MnXNOVAwOjByL{WwNEBvVQ>? NXfu[5R5OzBibXnu NX:wT4tM\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MXSyNlQ4Pjh3Mh?=
MCF-7 Mo\MRZBweHSxc3nzJGF{e2G7 NHX4OJEzODEEoH7N MnzVN|YhcA>? MnnCSG1UVw>? M{f4ZYlv\HWlZYOgZZBweHSxc3nz MXGyNlQ4Pjh3Mh?=
MDA-MB-231 NHPVXZhCeG:ydH;zbZMhSXO|YYm= NH\UO|YzODEEoH7N NGTseZQ{PiCq M4ftZWROW09? MX\pcoR2[2W|IHHwc5B1d3Orcx?= NXjDcG1GOjJ2N{[4OVI>
Bcap-37 NFS1SlNCeG:ydH;zbZMhSXO|YYm= MmCxNlAxyqCwTR?= NYLMNFYyOzZiaB?= NUfQTIlZTE2VTx?= MXPpcoR2[2W|IHHwc5B1d3Orcx?= MmnINlI1PzZ6NUK=
LS174T MXzGeY5kfGmxbjDBd5NigQ>? NH;RO20yOC9zMECvNVAxOCCwTR?= MXy2JIg> M2jWPGROW09? MYfpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu M33QVlIzPDBzMkm0
DLD-1  M2jTfmZ2dmO2aX;uJGF{e2G7 MnizNVAwOTByL{GwNFAhdk1? MVi2JIg> NWiw[pVsTE2VTx?= NWLkSWp1cW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? MV6yNlQxOTJ7NB?=
SW480 NUWyUWN4TnWwY4Tpc44hSXO|YYm= M3fUV|ExNzFyMD:xNFAxKG6P MUK2JIg> NXHDXFlMTE2VTx?= MUfpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu NUK1SIpsOjJ2MEGyPVQ>
SW-48 NVfPUGVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzDeHFKSzVyPUCuNUDPxE1? NYLseYpNOjJ{N{CyOVc>
HCT-15 Mnu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\POlVUUUN3ME2wMlMh|ryP MoLrNlIzPzB{NUe=
HCT 116 NFL3fpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwNjFOwG0> MW[yNlI4ODJ3Nx?=
SW620-R NULPOGM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPDUGdSUUN3ME2xMlMh|ryP NHPqWFMzOjJ5MEK1Oy=>
SK-CO-1 NVzWeHJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmX2TWM2OD1{LkGg{txO M2S2eFIzOjdyMkW3
SW620 NIf0c|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFzIN88US=> M37YTlIzOjdyMkW3
BaF3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XRb2dKPTB;MT60OFkh|ryP M4fUflIzOjJ|NkS1
NIH 3T3 MXjGeY5kfGmxbjDBd5NigQ>? NIL3T|gzKM7:TR?= NHXNXoMyQCCq MYLpcohq[mm2czDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBwdiCVZYK0O|Mh[W6mIH3UU3JEOSCyaH;zdIhwenmuYYTpc44hd2ZiNFWtRnAyKG:wIGTodlM4NzR4 NGjONIczOTh5NkGzNC=>
HCT15 MknhSpVv[3Srb36gRZN{[Xl? MWOwMlUwOiEQvF2= MmHtOEBp Ml3OdJJmfmWwdIOgV|ZMOSCyaH;zdIhwenmuYYTpc44hd2Zicnnic5NwdWGuIIDyc5RmcW5iU{[gZZQhW2W{MkSwM|I1PCCjbnSgcXRQWkN{IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qh[XRiU3XyOFc{ MVeyNVg4PjF|MB?=
SW620  M17EemZ2dmO2aX;uJGF{e2G7 M1nVWVAvPS9{IN88US=> Mn;COEBp M2XYc4Jtd2OtczDhcIwhfGi{ZXWgcXRQWiCxdYTweZR{ NHjBWWozOTh5NkGzNC=>

... 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
  • 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
Smiles CC(C)[N]1N=C(C2=CC3=C([NH]2)C=CC(=C3)O)C4=C(N)N=CN=C14

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

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