Torkinib (PP242)

Catalog No.S2218

For research use only.

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. Torkinib (PP242) induces mitophagy and apoptosis.

Torkinib (PP242) Chemical Structure

CAS No. 1092351-67-1

Selleck's Torkinib (PP242) has been cited by 80 publications

Purity & Quality Control

Choose Selective mTOR Inhibitors

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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. Torkinib (PP242) induces mitophagy and apoptosis.
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 M3P2b2Z2dmO2aX;uJGF{e2G7 NF7yPYQ2OC1zMkWwJI5O MUmyOEBp NXf4XpBUTE2VTx?= NFq4fVJqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZia3nuZZNmKCi2YYLn[ZQhd2ZibWTPVmMyMSCjbnSgbZR{KGSxd37zeJJm[W1idHHy[4V1KHCqb4PwbI8uWzcEoB?= Moe4NlYyPzdyNUG=
U87vIII  MnjOSpVv[3Srb36gRZN{[Xl? M4ixc|AvODRvMj61JO69VQ>? NGXncnkzPCCq NEH0UoVqdmirYnn0d{BuXE:UQ{GgZY5lKG2WT2LDNkBi[3Srdnn0bYV{yqB? NFzLeZgzPjF|NE[xOy=>
U87vIII  M2DhOWZ2dmO2aX;uJGF{e2G7 NVfh[2ZwOi53L{Wg{txO NXTVcJNJOTJiaB?= MlqwbY5pcWKrdIOg[4FxKGOub4PpcochcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGDFOYEzPjF|NE[xOy=>
PC12  MXXGeY5kfGmxbjDBd5NigQ>? MXG0NOKhdk1? MW\pcoR2[2W|IHz5d49{d22jbDDibY9o\W6nc3nzJIFv\CCjbHzleolifGWmIN8xMXN[ViCjY3P1cZVt[XSrb39CpC=> NULtN3c{OjZyMEG2NVQ>
3T3-L1 NUXhcldGTnWwY4Tpc44hSXO|YYm= NFHiPZQyPSEQvF2= MX20JIg> MVXzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGVoejFicILveIVqdsLi NWTTTHYyOjV6MUS2OlI>
Rh30 NGPEW4lHfW6ldHnvckBCe3OjeR?= MWKxJO69VQ>? M2Pp[VIhcA>? M3vFUYlvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= M17nclI2PzZ{NkG5
HT29 M3Pae2Z2dmO2aX;uJGF{e2G7 MYKxJO69VQ>? M3:5XlIhcA>? NH\RTHZqdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= MnzUNlU4PjJ4MUm=
Rh30 MXPGeY5kfGmxbjDBd5NigQ>? MWixJO69VQ>? NHPsNIgzKGh? NGS3OJN{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> MXuyOVc3OjZzOR?=
HT29 MWnGeY5kfGmxbjDBd5NigQ>? MYqxJO69VQ>? NYfFcFZbOiCq MVHzeZBxemW|c3XzJJRp\SCkYYPhcEBweiCLR1[tNU1{fGmvdXzheIVlKGOnbHygZYRp\XOrb36= NF72[pAzPTd4Mk[xPS=>
U87 NXz5PGVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2yOUBvVQ>? MkLtNlQhcA>? NXrjVppMcW6lcnXhd4V{KESXU2CxNEBsdm:la3XkMYRwf25iaX7keYNm\CClZXzsJIlvcGmkaYTpc44> MV[yOVU3QDZ4NR?=
AGS NVXLO|dKS2WubDDWbYFjcWyrdImgRZN{[Xl? M1vhPVAuOTByMDDuUS=> NGrlWmIzPC92ODDo NVTvcI5XTE2VTx?= NFP6T2Zl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MnXMNlUxOzV7NkG=
MKN45 M2LCeGNmdGxiVnnhZoltcXS7IFHzd4F6 Ml3wNE0yODByIH7N MYCyOE81QCCq M3fUVGROW09? MmLl[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M3HyU|I2ODN3OU[x
MKN28 Mn;KR4VtdCCYaXHibYxqfHliQYPzZZk> M3vwfVAuOTByMDDuUS=> MofGNlQwPDhiaB?= MnjwSG1UVw>? NXTIWmdR\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= Mlz5NlUxOzV7NkG=
KATO3 MkTFR4VtdCCYaXHibYxqfHliQYPzZZk> MofDNE0yODByIH7N MlXaNlQwPDhiaB?= M2LzNWROW09? Mmf1[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NXzIeWZqOjVyM{W5OlE>
SGC7901 M3qxfWNmdGxiVnnhZoltcXS7IFHzd4F6 NF7WeXMxNTFyMECgcm0> MnHBNlQwPDhiaB?= MV\EUXNQ NF3uR|Vl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NWT3eYVNOjVyM{W5OlE>
N87 NVjFcWdKS2WubDDWbYFjcWyrdImgRZN{[Xl? NYDKSmpEOC1zMECwJI5O NHPHNFUzPC92ODDo NYHQVlRtTE2VTx?= Mknv[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NYfkeFR7OjVyM{W5OlE>
HMEC MonlR4VtdCCYaXHibYxqfHliQYPzZZk> MmnzNE0yODByIH7N MUiyOE81QCCq NITnVFJFVVOR NXG5dpRb\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NHjVcoszPTB|NUm2NS=>
HUVEC MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnLGNE0yODByIH7N MoX3NlQwPDhiaB?= MkHaSG1UVw>? Mnv5[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MXqyOVA{PTl4MR?=
MG63 MWfGeY5kfGmxbjDBd5NigQ>? MoTyOVAuOTByMDDuUS=> NF3BZ24xNjViaB?= NHLiZlVld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> Mm[0NlQ5PDBzM{S=
U2OS  NW[0TZNtTnWwY4Tpc44hSXO|YYm= M1nhPFUxNTFyMECgcm0> MV[wMlUhcA>? NY\EbZZX\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 M1\4NVI1QDRyMUO0
Saos-2  NXHrb2xKTnWwY4Tpc44hSXO|YYm= M{nMV|UxNTFyMECgcm0> M3XxfFAvPSCq NXv4b3F[\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 M2Ds[|I1QDRyMUO0
Saos-2 M2Xj[mZ2dmO2aX;uJGF{e2G7 MYGxNFAhdk1? NV;jVHhKOC53IHi= Mn7OdJJmfmWwdIOgc5N1\W:|YYLjc41iKGOnbHygcYloemG2aX;u MYKyOFg1ODF|NB?=
MG63 MYPBdI9xfG:|aYOgRZN{[Xl? NXHKOmJoOTByIH7N M1O3dFM3KGh? MW\wdo9ud3SnczDhdI9xfG:|aYO= MYeyOFg1ODF|NB?=
U2OS  MorMRZBweHSxc3nzJGF{e2G7 MX:xNFAhdk1? M2n0RlM3KGh? MoHjdJJwdW:2ZYOgZZBweHSxc3nz MmDwNlQ5PDBzM{S=
Saos-2  MoG3RZBweHSxc3nzJGF{e2G7 NYDxXYdWOTByIH7N MXizOkBp NVTFSJlSeHKxbX;0[ZMh[XCxcITvd4l{ MVOyOFg1ODF|NB?=
HT1376 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEX6UXBKSzVyPUGuPFghyrFiMT6xJO69VQ>? NXLY[pdiOjRyNUS4O|E>
T24 M3vBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XQfWlEPTB;MT6zO{DDuSByLkSg{txO NXKzOmlvOjRyNUS4O|E>
UM-UC-3 M2TETmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLuWodKSzVyPUCuOlMhyrFyLkGg{txO NH7yS2QzPDB3NEi3NS=>
DLD-1 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M17zZlAuOTByMDDuUS=> NFLXNo8zPCCq NFvSb2NqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NG\Mb5MzOzl7MUG3PS=>
Caco2 MmDBR4VtdCCYaXHibYxqfHliQYPzZZk> NIm5dZUxNTFyMECgcm0> NVSwbXJ3OjRiaB?= MoPVbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYDMPZo1OjN7OUGxO|k>
HT29 NGHrUlRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1jiPVAuOTByMDDuUS=> NHnSdoYzPCCq NX3te|RFcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mln0NlM6QTFzN{m=
H116 MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2LkOVAuOTByMDDuUS=> NUXHXo05OjRiaB?= NFviT4ZqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGGwNY0zOzl7MUG3PS=>
Hct-8 M{faXWNmdGxiVnnhZoltcXS7IFHzd4F6 NXvNVlRKOC1zMECwJI5O NXTzU2lzOjRiaB?= NHfDTWxqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHLVSGszOzl7MUG3PS=>
Colo320 NV7IRms1S2WubDDWbYFjcWyrdImgRZN{[Xl? M3f3TFAuOTByMDDuUS=> MnXDNlQhcA>? MV3pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NGXIVHkzOzl7MUG3PS=>
Sw948 M37yTWNmdGxiVnnhZoltcXS7IFHzd4F6 M1XHW|AuOTByMDDuUS=> NH\qZ|AzPCCq MkDEbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXzwdHZjOjN7OUGxO|k>
Colo205 NU\xdJNbS2WubDDWbYFjcWyrdImgRZN{[Xl? NY\YfFZEOC1zMECwJI5O MlPVNlQhcA>? Ml3KbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{jlSVI{QTlzMUe5
Colo320 NVnkOGNlTnWwY4Tpc44hSXO|YYm= NWP3XHA2OSEQvF2= NH\2e24xNTJ2IHi= MYfhZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 MVWyN|k6OTF5OR?=
HT29 MXzGeY5kfGmxbjDBd5NigQ>? M3LUOFEh|ryP M3jUVlAuOjRiaB?= M3TscYFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> MofJNlM6QTFzN{m=
Sw948 M1PqUGZ2dmO2aX;uJGF{e2G7 NXzpd|VLOSEQvF2= M2DOSVAuOjRiaB?= M3XYcIFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> M2XtOVI{QTlzMUe5
DLD-1 MYHGeY5kfGmxbjDBd5NigQ>? MWmxJO69VQ>? MoDPNE0zPCCq NHPqRXVi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 M{[4c|I{QTlzMUe5
SW620 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTdwODFOwG0> MXWyN|U1OjF5OB?=
SW480 NV\1d4VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTRwNjFOwG0> NVTOeFlYOjN3NEKxO|g>
SK-CO-1 NWnm[Wh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjhTWM2OD12IN88US=> M3\HS|I{PTR{MUe4
LS-513 M1LLemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPremFGUUN3ME2zMlkh|ryP NGfwS|YzOzV2MkG3PC=>
SW1116 NWfnUI1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2G2OGlEPTB;MD64OEDPxE1? MU[yN|U1OjF5OB?=
LS-174T M{XiOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TEcWlEPTB;MD64OEDPxE1? M2nTUlI{PTR{MUe4
HCT 116 M4niNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXzTWM2OD1yLkSxJO69VQ>? NFLjfFQzOzV2MkG3PC=>
HCT 15 M2f5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG3TWM2OD1yLkOg{txO MmPlNlM2PDJzN{i=
COLO 205 NU\qdIVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;NTGlEPTB;MD6yOEDPxE1? NIHQU44zOzV2MkG3PC=>
HT-29 Ml:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rqWmlEPTB;MD6yN{DPxE1? M1fsU|I{PTR{MUe4
COLO 201 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXLTWM2OD1yLkKzJO69VQ>? M{m5WlI{PTR{MUe4
Caco-2 M2e0dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDFTWM2OD1yLkKyJO69VQ>? NVPKTXNOOjN3NEKxO|g>
SW48 NH;XPWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDZS4lDUUN3ME2wMlA6KM7:TR?= MkfvNlM2PDJzN{i=
DND-1 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuwMlI2NzBwNT:xJO69VQ>? NUfLSXV[TE2VTx?= MUXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M1rubVI{PDh{N{S4
TMD8 NV3HPYZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFv0dVgxNjJ3L{CuOU8yKM7:TR?= MVLEUXNQ M1[2UIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M{jKflI{PDh{N{S4
Jurkat MoL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PjfFAvOjVxMD61M|Eh|ryP MknCSG1UVw>? NYKxZ2VJcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MkHENlM1QDJ5NEi=
KOPT-K1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;XS|AvOjVxMD61M|Eh|ryP NXLVZpJHTE2VTx?= NHXlOIdqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NWrIRYpMOjN2OEK3OFg>
TMD7 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHIXlVFOC5{NT:wMlUwOSEQvF2= NETzNYNFVVOR NYnETHdscW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NELx[XozOzR6Mke0PC=>
THP-1 MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn0TIYxNjJ3L{CuOU8yKM7:TR?= M{HBdmROW09? Mk\wbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M4jrNFI{PDh{N{S4
786-O NEWwfVRHfW6ldHnvckBCe3OjeR?= MlPHNE4yNzBwNTFOwG0> MWWyOEBp MUnEUXNQ M3HWcolv[3KnYYPld{BGNWOjZHjldolvKG2UTlGgcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHl? MUWyN|E1PzJ3MR?=
786-O MnH4SpVv[3Srb36gRZN{[Xl? NFvwWWExNTBwNTFOwG0> Ml7xNlQhcA>? MXLEUXNQ NXPYb2NSemW|dXz0d{BqdiCjIHTvd4Uh\GWyZX7k[Y51KGmwY4LlZZNmKGmwIFWtZ4FlcGW{aX6gdJJwfGWrbjDlfJBz\XO|aX;uxsA> NF;MNlkzOzF2N{K1NS=>
OCI-AML3 NVrVd5Q1SXCxcITvd4l{KEG|c3H5 MUCyMlUh|ryP Mn3sO|IhcA>? NWXuVoxjcW6mdXPld{BieG:ydH;zbZM> NGXpXWUzOjh{NkW2OS=>
Jurkat NVrkRlI3TnWwY4Tpc44hSXO|YYm= MWGxNFAwOjByL{SwNEBvVQ>? M1fDZ|E5KGh? M1Hm[4lvcGmkaYTzJI1VV1KFMT3k[ZBmdmSnboSgV|YhWzJ|NT:yN|YheGixc4Doc5J6dGG2aX;u NXLVcYZtOjJ3Nk[2NFQ>
p210 BCR-Abl NGriXlBHfW6ldHnvckBCe3OjeR?= NIjj[IcyODBxMkCwM|QxOCCwTR?= NUHIZVg5OThiaB?= MXPpcohq[mm2czDtWG9TSzFvZHXw[Y5l\W62IGO2JHMzOzVxMkO2JJBpd3OyaH;yfYxifGmxbh?= NYCyU2s4OjJ3Nk[2NFQ>
Jurkat M{j5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj6OFAxdk1? NUD0b4V5OjRxNEigbC=> MVjzfY5memerenWge4l1cCBzNz3BRWchfG9ic4XwdJJme3NiY3XscEBxem:uaX\ldoF1cW:w M1LqblIzPTZ4NkC0
p210 BCR-Abl NXK3WJJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HZOVQxOG6P M1LQSFI1NzR6IHi= NHTYXFV{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u M4nYUlIzPTZ4NkC0
8226 MXzGeY5kfGmxbjDBd5NigQ>? M3WwcFExOC1zMECwJI5O MVuzNEBucW5? M2iyRmROW09? NWTGdW5D[WO2aY\heIV{KEWUS9Mg Mle4NlI2PTZ2MEm=
MM1.S  NHvsZ3dHfW6ldHnvckBCe3OjeR?= NG\5T4YyODBvMUCwNEBvVQ>? NH\VUGQ{OCCvaX6= M1XMNWROW09? NFLIbZdi[3SrdnH0[ZMhTVKNwrC= MkDGNlI2PTZ2MEm=
8226 NF\JPVFHfW6ldHnvckBCe3OjeR?= M{DvblAvPSEQvF2= NHPxXFY{OCCvaX6= M3HRVGROW09? MmTFbY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= NF[y[5kzOjV3NkSwPS=>
MM1.S  MUXGeY5kfGmxbjDBd5NigQ>? MlrpNE42KM7:TR?= M13sbVMxKG2rbh?= NX3KR4N3TE2VTx?= NIH2TGVqdmS3Y3XzJIFkfGm4YYTpc44hd2ZiUlHGJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiTVXL MlvtNlI2PTZ2MEm=
MCF-7 Ml;6SpVv[3Srb36gRZN{[Xl? NWf4NGRUPTBxMkCwM|UxOCCwTR?= MUCzNEBucW5? NI\VcIFld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? NWCxXoRQOjJ2N{[4OVI>
T47D MkTnSpVv[3Srb36gRZN{[Xl? M{TFdVUxNzJyMD:1NFAhdk1? M3zjVlMxKG2rbh?= M1K0WIRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 NEnhbVczOjR5Nki1Ni=>
MDA-MB-231 NXvPcmZ2TnWwY4Tpc44hSXO|YYm= NIDofWg2OC9{MECvOVAxKG6P MVWzNEBucW5? M4TWWoRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 NWOxUmIxOjJ2N{[4OVI>
Bcap-37 Ml:3SpVv[3Srb36gRZN{[Xl? NFvmeGs2OC9{MECvOVAxKG6P M2fTeVMxKG2rbh?= NWfkbWFY\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? NH;vcW0zOjR5Nki1Ni=>
MCF-7 NYP5eWVZSXCxcITvd4l{KEG|c3H5 NYHyWG5kOjBywrDuUS=> NFHqe3I{PiCq MXTEUXNQ M4DaR4lv\HWlZYOgZZBweHSxc3nz NYrEPGgxOjJ2N{[4OVI>
MDA-MB-231 MkT6RZBweHSxc3nzJGF{e2G7 MUOyNFDDqG6P MlfEN|YhcA>? NX7hRoZLTE2VTx?= M2nWT4lv\HWlZYOgZZBweHSxc3nz M{Ht[lIzPDd4OEWy
Bcap-37 NUXSd3RtSXCxcITvd4l{KEG|c3H5 NV;2RXEzOjBywrDuUS=> NX\6UpluOzZiaB?= MlLDSG1UVw>? NEXUNY5qdmS3Y3XzJIFxd3C2b4Ppdy=> MkfKNlI1PzZ6NUK=
LS174T MmnrSpVv[3Srb36gRZN{[Xl? MlrhNVAwOTByL{GwNFAhdk1? M2\nUlYhcA>? M3f2R2ROW09? NYjGNGwxcW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? NYHMfFV7OjJ2MEGyPVQ>
DLD-1  M4C4W2Z2dmO2aX;uJGF{e2G7 NHO3V3YyOC9zMECvNVAxOCCwTR?= NU[xc|I4PiCq MVjEUXNQ M2DOZ4lvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> NFfP[m0zOjRyMUK5OC=>
SW480 NHL6e5NHfW6ldHnvckBCe3OjeR?= MV2xNE8yODBxMUCwNEBvVQ>? M1O3OlYhcA>? MYLEUXNQ NF7aco5qdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv MknqNlI1ODF{OUS=
SW-48 Ml;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYW4bmJGUUN3ME2wMlEh|ryP MnnHNlIzPzB{NUe=
HCT-15 NFjtTGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjGNotJUUN3ME2wMlMh|ryP NYTGZWFPOjJ{N{CyOVc>
HCT 116 M1P4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfORW0{UUN3ME2wMlYh|ryP NIn3eJAzOjJ5MEK1Oy=>
SW620-R M3XZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTFwMzFOwG0> M3fkZVIzOjdyMkW3
SK-CO-1 NYDqSGhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr0TWM2OD1{LkGg{txO NEe0XFQzOjJ5MEK1Oy=>
SW620 NX\hTplwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTFzIN88US=> NX7WRVQ1OjJ{N{CyOVc>
BaF3 NF\jXXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTOS2k2OD1zLkS0PUDPxE1? M{Dy[|IzOjJ|NkS1
NIH 3T3 NELVXXlHfW6ldHnvckBCe3OjeR?= NIPxPZQzKM7:TR?= NFf5UngyQCCq NYS1Tm5GcW6qaXLpeJMhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3Rib36gV4VzPDd|IHHu[EBuXE:UQ{GgdIhwe3Cqb4L5cIF1cW:wIH;mJFRGNUKSMTDvckBVcHJ|Nz:0Oi=> M37q[FIyQDd4MUOw
HCT15 NHeyWZdHfW6ldHnvckBCe3OjeR?= NWTjUVRiOC53L{Kg{txO MonMOEBp M4jRV5Bz\X[nboTzJHM3UzFicHjvd5Bpd3K7bHH0bY9vKG:oIILpZo9{d22jbDDwdo91\WmwIGO2JIF1KFOnckK0NE8zPDRiYX7kJI1VV1KFMjDwbI9{eGixconsZZRqd25ib3[gRYt1KGG2IGPldlQ4Ow>? MWCyNVg4PjF|MB?=
SW620  NIDjeGZHfW6ldHnvckBCe3OjeR?= NX7P[HBsOC53L{Kg{txO NH3JWGE1KGh? NUPCV3FX[myxY3vzJIFtdCC2aILl[UBuXE:UIH;1eJB2fHN? M3[5XVIyQDd4MUOw
Assay
Methods Test Index PMID
Western blot p-mTOR / mTOR / p-AKT / AKT / p-S6 / S6 / p-4E-BP1 / 4E-BP-1 23991179
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[3]
  • 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

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

Chemical Information

Molecular Weight 308.34
Formula

C16H16N6O

CAS No. 1092351-67-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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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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