Torkinib (PP242)

For research use only.

Catalog No.S2218

72 publications

Torkinib (PP242) Chemical Structure

CAS No. 1092351-67-1

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.

Selleck's Torkinib (PP242) has been cited by 72 publications

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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 MmnSSpVv[3Srb36gRZN{[Xl? MUW1NE0yOjVyIH7N NEP3e2YzPCCq NF;BSHlFVVOR NYL6cJJ4cW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFN4IHvpcoF{\SBqdHHy[4V1KG:oIH3UU3JEOSliYX7kJIl1eyCmb4fud5Rz\WGvIIThdodmfCCyaH;zdIhwNVN4wrC= NHi2XpIzPjF5N{C1NS=>
U87vIII  MlrkSpVv[3Srb36gRZN{[Xl? NWeyPINnOC5yND2yMlUh|ryP M3HZXVI1KGh? MkW2bY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh M3PQTlI3OTN2NkG3
U87vIII  MlPBSpVv[3Srb36gRZN{[Xl? NXfNV4Y1Oi53L{Wg{txO NUTmWGYyOTJiaB?= NX3FV4sycW6qaXLpeJMh\2GyIHPsc5NqdmdiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWeyOlE{PDZzNx?=
PC12  MXzGeY5kfGmxbjDBd5NigQ>? NHjZb|E1OMLibl2= NXLNUZA3cW6mdXPld{BtgXOxc3;tZYwh[mmxZ3Xu[ZNqeyCjbnSgZYxt\X[rYYTl[EDPuS2VWV6gZYNkfW23bHH0bY9vyqB? MknnNlYxODF4MUS=
3T3-L1 MnHRSpVv[3Srb36gRZN{[Xl? NYjTPHB5OTVizszN NYLjSmdXPCCq M1HzWJN2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhTWe{MTDwdo91\WmwwrC= M2ThVVI2QDF2Nk[y
Rh30 NFrWXIhHfW6ldHnvckBCe3OjeR?= NXzXUmFSOSEQvF2= NFnHOGszKGh? NFv5UW9qdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= MoK0NlU4PjJ4MUm=
HT29 MmPDSpVv[3Srb36gRZN{[Xl? MlzFNUDPxE1? NWS2eG45OiCq M3nBPIlvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= NXK0U2ptOjV5NkK2NVk>
Rh30 M4r1XmZ2dmO2aX;uJGF{e2G7 M1\FWlEh|ryP MYmyJIg> MkP4d5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u NH2wVmQzPTd4Mk[xPS=>
HT29 NHnyeYpHfW6ldHnvckBCe3OjeR?= MUWxJO69VQ>? M3zCNlIhcA>? MmjLd5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u NV23PIh3OjV5NkK2NVk>
U87 NGLFSpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjub45DOjVibl2= M1q4W|I1KGh? MV7pcoNz\WG|ZYOgSHVUWDFyIHvuc4Ns\WRvZH;3ckBqdmS3Y3XkJINmdGxiaX7obYJqfGmxbh?= MVeyOVU3QDZ4NR?=
AGS NUn4WIpUS2WubDDWbYFjcWyrdImgRZN{[Xl? NFHDb2wxNTFyMECgcm0> NWWwUnNDOjRxNEigbC=> MlvxSG1UVw>? MmTt[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M{nDelI2ODN3OU[x
MKN45 MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUTMdHlTOC1zMECwJI5O NF3NNZkzPC92ODDo MWnEUXNQ NInJSmdl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NWfKcpE2OjVyM{W5OlE>
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KATO3 MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEHyZXUxNTFyMECgcm0> MXWyOE81QCCq MUTEUXNQ NV7wV3RL\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M{PXVFI2ODN3OU[x
SGC7901 NHXCZm9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGr1ZZExNTFyMECgcm0> NUfTPGJkOjRxNEigbC=> NFf0RY5FVVOR Mmji[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NEjlWm0zPTB|NUm2NS=>
N87 MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUTW[HdOOC1zMECwJI5O NXeybVl1OjRxNEigbC=> MV7EUXNQ NGfSWpdl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MlHwNlUxOzV7NkG=
HMEC NYK4NmRZS2WubDDWbYFjcWyrdImgRZN{[Xl? M3:xfVAuOTByMDDuUS=> NUnVeG9tOjRxNEigbC=> MWnEUXNQ MWPk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NFz5d5IzPTB|NUm2NS=>
HUVEC M1u1ZWNmdGxiVnnhZoltcXS7IFHzd4F6 MmrENE0yODByIH7N M2\1flI1NzR6IHi= M3TZ[WROW09? M{[yb4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NVfsfG9vOjVyM{W5OlE>
MG63 NXvjPWtKTnWwY4Tpc44hSXO|YYm= NG\lRm02OC1zMECwJI5O MUKwMlUhcA>? NUS5bXVk\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 MljNNlQ5PDBzM{S=
U2OS  M3\FcWZ2dmO2aX;uJGF{e2G7 MYS1NE0yODByIH7N M2TwU|AvPSCq NGjjWoxld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MUeyOFg1ODF|NB?=
Saos-2  M4KyXWZ2dmO2aX;uJGF{e2G7 MkXsOVAuOTByMDDuUS=> MW[wMlUhcA>? MWDkc5NmKGSncHXu[IVvfGy7IDi1NQKBmzFyMECgcm0qKGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= NYntdWhxOjR6NECxN|Q>
Saos-2 NUPsUnFZTnWwY4Tpc44hSXO|YYm= NWrucVNTOTByIH7N MnTMNE42KGh? NXizcIRGeHKndnXueJMhd3O2ZX;zZZJkd22jIHPlcIwhdWmpcnH0bY9v NGXyemUzPDh2MEGzOC=>
MG63 M{fwSmFxd3C2b4Ppd{BCe3OjeR?= NVrJ[G93OTByIH7N NYm5dmROOzZiaB?= NYL2d212eHKxbX;0[ZMh[XCxcITvd4l{ Mmn3NlQ5PDBzM{S=
U2OS  M2GwWWFxd3C2b4Ppd{BCe3OjeR?= M3rwSFExOCCwTR?= MlHsN|YhcA>? NHTje5Vxem:vb4Tld{BieG:ydH;zbZM> M13PflI1QDRyMUO0
Saos-2  MlnuRZBweHSxc3nzJGF{e2G7 MVGxNFAhdk1? MXezOkBp MnL4dJJwdW:2ZYOgZZBweHSxc3nz M4Hs[FI1QDRyMUO0
HT1376 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTRVXhlUUN3ME2xMlg5KMLzIEGuNUDPxE1? NVWzWoloOjRyNUS4O|E>
T24 NYL6OWF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwM{egxtEhOC52IN88US=> Mn;MNlQxPTR6N{G=
UM-UC-3 M1vBe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwNkOgxtExNjFizszN M2DDclI1ODV2OEex
DLD-1 MkfDR4VtdCCYaXHibYxqfHliQYPzZZk> NFrqXZcxNTFyMECgcm0> M4XTT|I1KGh? MUjpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlviNlM6QTFzN{m=
Caco2 NILFSXhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1m1WFAuOTByMDDuUS=> NInQWWQzPCCq MWLpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NXy0d3lkOjN7OUGxO|k>
HT29 M3;FRWNmdGxiVnnhZoltcXS7IFHzd4F6 MWKwMVExODBibl2= NWnZ[GdYOjRiaB?= M4TPfIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVXjXXI1OjN7OUGxO|k>
H116 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWGz[G9COC1zMECwJI5O NH\sXJMzPCCq M1S2VIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1W5S|I{QTlzMUe5
Hct-8 NFL0flZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mo\NNE0yODByIH7N NYW3enF5OjRiaB?= MXfpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlPLNlM6QTFzN{m=
Colo320 NFTXb2JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVfBXnllOC1zMECwJI5O M1i1SFI1KGh? NHnMd|FqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX:5UWRSOjN7OUGxO|k>
Sw948 NF3N[mJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2ThO|AuOTByMDDuUS=> MVeyOEBp NYHES2IycW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUKyN|k6OTF5OR?=
Colo205 MoPmR4VtdCCYaXHibYxqfHliQYPzZZk> Mn[yNE0yODByIH7N NEjPdIYzPCCq Ml20bY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWCyN|k6OTF5OR?=
Colo320 M3vOVGZ2dmO2aX;uJGF{e2G7 NYPvTYE2OSEQvF2= NX7lS3hrOC1{NDDo MV3hZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 NH\0ZYQzOzl7MUG3PS=>
HT29 NGHoeplHfW6ldHnvckBCe3OjeR?= NWfW[WY3OSEQvF2= MlXNNE0zPCCq NW[0RXVi[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MXWyN|k6OTF5OR?=
Sw948 MoT0SpVv[3Srb36gRZN{[Xl? MWixJO69VQ>? M33ZfVAuOjRiaB?= MmXDZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> M4HMS|I{QTlzMUe5
DLD-1 MmPsSpVv[3Srb36gRZN{[Xl? MVmxJO69VQ>? NX\tXHBXOC1{NDDo MX;hZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 MmLTNlM6QTFzN{m=
SW620 M{DWeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrMZ2FzUUN3ME23Mlgh|ryP MVWyN|U1OjF5OB?=
SW480 NIjwO5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP5TWM2OD12Lk[g{txO MmLiNlM2PDJzN{i=
SK-CO-1 NIHheGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGL0dpRKSzVyPUSg{txO NH7XZW0zOzV2MkG3PC=>
LS-513 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkezTWM2OD1|Lkmg{txO NIW0O2EzOzV2MkG3PC=>
SW1116 NEPKNFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwOESg{txO MW[yN|U1OjF5OB?=
LS-174T MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnq0TWM2OD1yLki0JO69VQ>? NH3EU2gzOzV2MkG3PC=>
HCT 116 M1XCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrJRWZCUUN3ME2wMlQyKM7:TR?= NYLRcIVpOjN3NEKxO|g>
HCT 15 M4jQXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[5dlhXUUN3ME2wMlMh|ryP NEm3UHYzOzV2MkG3PC=>
COLO 205 NWDIOIt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Cy[mlEPTB;MD6yOEDPxE1? MnnJNlM2PDJzN{i=
HT-29 NYmzPYZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;ne4V3UUN3ME2wMlI{KM7:TR?= M1jJfFI{PTR{MUe4
COLO 201 NUjQVIRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwMkOg{txO M165TlI{PTR{MUe4
Caco-2 NYjQR2FYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7YTWM2OD1yLkKyJO69VQ>? MlXtNlM2PDJzN{i=
SW48 MmP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXqS4hKSzVyPUCuNFkh|ryP NGnaeYMzOzV2MkG3PC=>
DND-1 NH7BS4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;pOFAvOjVxMD61M|Eh|ryP NHqxc5FFVVOR NV;sPY5ycW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NFzoeokzOzR6Mke0PC=>
TMD8 NHfEXopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLQNE4zPS9yLkWvNUDPxE1? M4jjNGROW09? MVjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M4T0[VI{PDh{N{S4
Jurkat NG\vN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4m4UVAvOjVxMD61M|Eh|ryP M4DZXmROW09? M3fFfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MU[yN|Q5Ojd2OB?=
KOPT-K1 NVrTRWxRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEj1W2QxNjJ3L{CuOU8yKM7:TR?= Moj5SG1UVw>? NYDudZdCcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NFO1b4szOzR6Mke0PC=>
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THP-1 NXy0NGdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEP4O4gxNjJ3L{CuOU8yKM7:TR?= MVTEUXNQ NXfnWJpicW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mkj3NlM1QDJ5NEi=
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786-O M{Py[GZ2dmO2aX;uJGF{e2G7 NXrJd3V2OC1yLkWg{txO NWHke2pwOjRiaB?= MYnEUXNQ NVO5e4NiemW|dXz0d{BqdiCjIHTvd4Uh\GWyZX7k[Y51KGmwY4LlZZNmKGmwIFWtZ4FlcGW{aX6gdJJwfGWrbjDlfJBz\XO|aX;uxsA> NXG1bpJvOjNzNEeyOVE>
OCI-AML3 Mmj0RZBweHSxc3nzJGF{e2G7 MnPpNk42KM7:TR?= NVv5XFZmPzJiaB?= M4jP[Ylv\HWlZYOgZZBweHSxc3nz Ml[zNlI5OjZ3NkW=
Jurkat NHnm[YJHfW6ldHnvckBCe3OjeR?= MYWxNFAwOjByL{SwNEBvVQ>? MkfWNVghcA>? NXX0W2tqcW6qaXLpeJMhdVSRUlOxMYRmeGWwZHXueEBUPiCVMkO1M|I{PiCyaH;zdIhwenmuYYTpc44> NUOzcItpOjJ3Nk[2NFQ>
p210 BCR-Abl NXXLflZXTnWwY4Tpc44hSXO|YYm= NIjQfY4yODBxMkCwM|QxOCCwTR?= MVyxPEBp NGD2NWJqdmirYnn0d{BuXE:UQ{Gt[IVx\W6mZX70JHM3KFN{M{WvNlM3KHCqb4PwbI9zgWyjdHnvci=> NWD1e2I6OjJ3Nk[2NFQ>
Jurkat NGG1WlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFn6TIw1ODCwTR?= MnnmNlQwPDhiaB?= M{fHUpN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= Ml\RNlI2PjZ4MES=
p210 BCR-Abl MkDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXO0NFBvVQ>? M37mT|I1NzR6IHi= NVzsNGZUe3mwZYLnbZpmKHerdHigNVcuSUGJIITvJJN2eHC{ZYPzJINmdGxicILvcIln\XKjdHnvci=> NHflWokzOjV4Nk[wOC=>
8226 MULGeY5kfGmxbjDBd5NigQ>? MmTDNVAxNTFyMECgcm0> MYqzNEBucW5? NXLBR5ZJTE2VTx?= NIfOfJdi[3SrdnH0[ZMhTVKNwrC= MluxNlI2PTZ2MEm=
MM1.S  NFnVZWpHfW6ldHnvckBCe3OjeR?= NWfCbGNnOTByLUGwNFAhdk1? MlrCN|AhdWmw Mn\kSG1UVw>? NWjlOXdx[WO2aY\heIV{KEWUS9Mg NYCyVZFSOjJ3NU[0NFk>
8226 MWnGeY5kfGmxbjDBd5NigQ>? MUCwMlUh|ryP M3HaV|MxKG2rbh?= NVH2Rph7TE2VTx?= Ml7xbY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= M4DGTVIzPTV4NEC5
MM1.S  NIXV[|VHfW6ldHnvckBCe3OjeR?= NX3CXFhlOC53IN88US=> NI[zW|E{OCCvaX6= NIrxeXZFVVOR MnW4bY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= M4rmUVIzPTV4NEC5
MCF-7 MXvGeY5kfGmxbjDBd5NigQ>? NVHkO2REPTBxMkCwM|UxOCCwTR?= NXe2[WdNOzBibXnu M3PBOIRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 M1j3bVIzPDd4OEWy
T47D NXPqVYlJTnWwY4Tpc44hSXO|YYm= Mkm0OVAwOjByL{WwNEBvVQ>? MnPPN|AhdWmw NFnnPXFld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? NEKydIwzOjR5Nki1Ni=>
MDA-MB-231 MVHGeY5kfGmxbjDBd5NigQ>? NYLBNIdnPTBxMkCwM|UxOCCwTR?= MYCzNEBucW5? NGfhTIxld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? NWfQXpVbOjJ2N{[4OVI>
Bcap-37 NXzZc|NUTnWwY4Tpc44hSXO|YYm= MlzNOVAwOjByL{WwNEBvVQ>? NIDWbWs{OCCvaX6= MX;kc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M{fSZVIzPDd4OEWy
MCF-7 NGrvT2lCeG:ydH;zbZMhSXO|YYm= M17GR|IxOMLibl2= MkezN|YhcA>? M4i2eWROW09? MkLMbY5lfWOnczDhdI9xfG:|aYO= NEfwU2EzOjR5Nki1Ni=>
MDA-MB-231 NHK2[|lCeG:ydH;zbZMhSXO|YYm= MXWyNFDDqG6P NGPUVGY{PiCq MnHUSG1UVw>? NEn2bmZqdmS3Y3XzJIFxd3C2b4Ppdy=> MlLvNlI1PzZ6NUK=
Bcap-37 MYDBdI9xfG:|aYOgRZN{[Xl? Mlm1NlAxyqCwTR?= M4O1WVM3KGh? NIX0fJNFVVOR NXSwTYFwcW6mdXPld{BieG:ydH;zbZM> M{HpSFIzPDd4OEWy
LS174T M3PmcWZ2dmO2aX;uJGF{e2G7 NYOw[Fh3OTBxMUCwM|ExODBibl2= MlzxOkBp NHrEdI1FVVOR NEjjW3lqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv NGLF[4QzOjRyMUK5OC=>
DLD-1  NXH6bJg1TnWwY4Tpc44hSXO|YYm= M4LpWVExNzFyMD:xNFAxKG6P MnXROkBp NIDkV4tFVVOR MVTpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu M3jhUFIzPDBzMkm0
SW480 M2DIVWZ2dmO2aX;uJGF{e2G7 NXXL[XRHOTBxMUCwM|ExODBibl2= Mnz0OkBp NYLrdnllTE2VTx?= M33yUolvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> NUnEPHpyOjJ2MEGyPVQ>
SW-48 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljkTWM2OD1yLkGg{txO NH\3[2szOjJ5MEK1Oy=>
HCT-15 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfMTWM2OD1yLkOg{txO MYCyNlI4ODJ3Nx?=
HCT 116 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTidnhyUUN3ME2wMlYh|ryP NFe4OJgzOjJ5MEK1Oy=>
SW620-R NYXZcIgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnUTWM2OD1zLkOg{txO MkTGNlIzPzB{NUe=
SK-CO-1 NEnjb|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJwMTFOwG0> NWPH[Ww1OjJ{N{CyOVc>
SW620 NInSOJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rIVGlEPTB;MUGg{txO MXiyNlI4ODJ3Nx?=
BaF3 NVrDTFBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\oS2k2OD1zLkS0PUDPxE1? NFSwNGEzOjJ{M{[0OS=>
NIH 3T3 M1;qS2Z2dmO2aX;uJGF{e2G7 Ml3YNkDPxE1? M4DY[FE5KGh? MVjpcohq[mm2czDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBwdiCVZYK0O|Mh[W6mIH3UU3JEOSCyaH;zdIhwenmuYYTpc44hd2ZiNFWtRnAyKG:wIGTodlM4NzR4 MnfiNlE5PzZzM{C=
HCT15 M1rafWZ2dmO2aX;uJGF{e2G7 MlT3NE42NzJizszN MYe0JIg> MV7wdoV3\W62czDTOmsyKHCqb4PwbI9zgWyjdHnvckBw\iC{aXLvd49u[WxicILveIVqdiCVNjDheEBU\XJ{NECvNlQ1KGGwZDDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBifCCVZYK0O|M> NVToWW5{OjF6N{[xN|A>
SW620  NHf1UGVHfW6ldHnvckBCe3OjeR?= M37UUlAvPS9{IN88US=> MlWzOEBp NXfHR5N4[myxY3vzJIFtdCC2aILl[UBuXE:UIH;1eJB2fHN? NWLHeplbOjF6N{[xN|A>

... 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)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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% 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 SDS / 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 SDS / 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