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 29 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
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PC12  M{PzNmZ2dmO2aX;uJGF{e2G7 MmD2OFDDqG6P M3rvUYlv\HWlZYOgcJl{d3OxbXHsJIJqd2enbnXzbZMh[W6mIHHscIV3cWG2ZXSg{tEuW1mQIHHjZ5VufWyjdHnvcuKh NETIfIEzPjByMU[xOC=>
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U87 MmXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1OxbFI2KG6P MlWwNlQhcA>? NVfoc5hqcW6lcnXhd4V{KESXU2CxNEBsdm:la3XkMYRwf25iaX7keYNm\CClZXzsJIlvcGmkaYTpc44> MYGyOVU3QDZ4NR?=
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N87 NHHVO|RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFnzZ3gxNTFyMECgcm0> NHvGVpYzPC92ODDo MojCSG1UVw>? MYnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NWnzb|ZmOjVyM{W5OlE>
HMEC MofER4VtdCCYaXHibYxqfHliQYPzZZk> M2DNPVAuOTByMDDuUS=> NGTaUnYzPC92ODDo NUO1VJE2TE2VTx?= M3m4VYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NETt[3czPTB|NUm2NS=>
HUVEC M3XkZmNmdGxiVnnhZoltcXS7IFHzd4F6 NXrMXoo3OC1zMECwJI5O M2L0VlI1NzR6IHi= NET1XIFFVVOR MlvK[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NGr0[GgzPTB|NUm2NS=>
MG63 MXXGeY5kfGmxbjDBd5NigQ>? M4PTfVUxNTFyMECgcm0> NHWzU4oxNjViaB?= M{PVV4Rwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NIHCOYkzPDh2MEGzOC=>
U2OS  MX;GeY5kfGmxbjDBd5NigQ>? M4fyVlUxNTFyMECgcm0> MmDTNE42KGh? NEGwdIdld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MmTvNlQ5PDBzM{S=
Saos-2  NGnwW45HfW6ldHnvckBCe3OjeR?= Mkm0OVAuOTByMDDuUS=> NXPMcHJqOC53IHi= Mk[2[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 Mmm4NlQ5PDBzM{S=
Saos-2 M37lW2Z2dmO2aX;uJGF{e2G7 NV7weoo{OTByIH7N MlriNE42KGh? M4D2RZBz\X[nboTzJI9{fGWxc3HyZ49u[SClZXzsJI1q\3KjdHnvci=> MXuyOFg1ODF|NB?=
MG63 MmXKRZBweHSxc3nzJGF{e2G7 M1PRSVExOCCwTR?= MVmzOkBp MXrwdo9ud3SnczDhdI9xfG:|aYO= MWWyOFg1ODF|NB?=
U2OS  MoLTRZBweHSxc3nzJGF{e2G7 NH\UT3AyODBibl2= M4nMRlM3KGh? MVTwdo9ud3SnczDhdI9xfG:|aYO= M3nkd|I1QDRyMUO0
Saos-2  MkXzRZBweHSxc3nzJGF{e2G7 MlS2NVAxKG6P NGLxeGM{PiCq MkjTdJJwdW:2ZYOgZZBweHSxc3nz MoqyNlQ5PDBzM{S=
HT1376 M{S5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLXTWM2OD1zLki4JOKyKDFwMTFOwG0> M2XNPFI1ODV2OEex
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UM-UC-3 NIKwNHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLDbnBKSzVyPUCuOlMhyrFyLkGg{txO M1jHS|I1ODV2OEex
DLD-1 MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlvBNE0yODByIH7N MX:yOEBp Mlv1bY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MX6yN|k6OTF5OR?=
Caco2 M1LQXGNmdGxiVnnhZoltcXS7IFHzd4F6 NE[5bmoxNTFyMECgcm0> NFfKc5UzPCCq NF;YWmRqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Ml7sNlM6QTFzN{m=
HT29 NFjDbodE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEHURXAxNTFyMECgcm0> NGLmWmUzPCCq MWnpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NWLzU21GOjN7OUGxO|k>
H116 MUfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Ml[2NE0yODByIH7N MoHvNlQhcA>? NG[4Zm5qdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MW[yN|k6OTF5OR?=
Hct-8 M4LTe2NmdGxiVnnhZoltcXS7IFHzd4F6 NWjBb|dGOC1zMECwJI5O M4ixSVI1KGh? NHHnVI9qdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmX3NlM6QTFzN{m=
Colo320 NYP0NoVVS2WubDDWbYFjcWyrdImgRZN{[Xl? M13RV|AuOTByMDDuUS=> M1m1WlI1KGh? MYDpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NH\hUm4zOzl7MUG3PS=>
Sw948 NIfERlRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUmwMVExODBibl2= MUeyOEBp MnLqbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGO5WXozOzl7MUG3PS=>
Colo205 NYTH[GNmS2WubDDWbYFjcWyrdImgRZN{[Xl? NWPtNW15OC1zMECwJI5O MlHSNlQhcA>? MY\pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4mwelI{QTlzMUe5
Colo320 MUXGeY5kfGmxbjDBd5NigQ>? NUewXZd6OSEQvF2= NU\WSXRnOC1{NDDo MlPRZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> NW\zOHBDOjN7OUGxO|k>
HT29 NH[3UmNHfW6ldHnvckBCe3OjeR?= M3PwR|Eh|ryP MljSNE0zPCCq MV7hZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 M{nud|I{QTlzMUe5
Sw948 M2[yb2Z2dmO2aX;uJGF{e2G7 Mn\SNUDPxE1? M1L1elAuOjRiaB?= MXXhZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 MV[yN|k6OTF5OR?=
DLD-1 M33Nb2Z2dmO2aX;uJGF{e2G7 NFzDdG4yKM7:TR?= MlrDNE0zPCCq NUjyWVN7[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MnyyNlM6QTFzN{m=
SW620 NWrjUW0xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTdwODFOwG0> MXuyN|U1OjF5OB?=
SW480 NY\DOWtWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvMdHpKSzVyPUSuOkDPxE1? Ml7KNlM2PDJzN{i=
SK-CO-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHvS4JkUUN3ME20JO69VQ>? MWqyN|U1OjF5OB?=
LS-513 M3nqW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L6cmlEPTB;Mz65JO69VQ>? MX6yN|U1OjF5OB?=
SW1116 MnzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXS[YNWUUN3ME2wMlg1KM7:TR?= MXWyN|U1OjF5OB?=
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DND-1 NI\abmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHW4eVExNjJ3L{CuOU8yKM7:TR?= NHfqb4ZFVVOR NVPu[oxCcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mo[4NlM1QDJ5NEi=
TMD8 NXT3cJVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSwMlI2NzBwNT:xJO69VQ>? NFLuNXpFVVOR NIX2WlRqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 Mo\KNlM1QDJ5NEi=
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OCI-AML3 Mk\2RZBweHSxc3nzJGF{e2G7 MX2yMlUh|ryP NVzBRXJEPzJiaB?= NFvZUXVqdmS3Y3XzJIFxd3C2b4Ppdy=> NVPUVFVGOjJ6Mk[1OlU>
Jurkat MkHuSpVv[3Srb36gRZN{[Xl? M1vQVFExOC9{MECvOFAxKG6P NFfTRmcyQCCq M{Xk[4lvcGmkaYTzJI1VV1KFMT3k[ZBmdmSnboSgV|YhWzJ|NT:yN|YheGixc4Doc5J6dGG2aX;u NFHXSpgzOjV4Nk[wOC=>
p210 BCR-Abl NYjyWHVyTnWwY4Tpc44hSXO|YYm= NXPn[YU1OTByL{KwNE81ODBibl2= MkDiNVghcA>? Mn;sbY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= NH7GWFEzOjV4Nk[wOC=>
Jurkat NFjMenpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXSxVXUyPDBybl2= MVuyOE81QCCq Ml;md5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= MYWyNlU3PjZyNB?=
p210 BCR-Abl M3zXdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4m5WFQxOG6P NED3WYUzPC92ODDo M4ThcJN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= NHm1cYkzOjV4Nk[wOC=>
8226 Mk\jSpVv[3Srb36gRZN{[Xl? NGmzSGYyODBvMUCwNEBvVQ>? MoDkN|AhdWmw NFHKcWtFVVOR MWfhZ5RqfmG2ZYOgSXJMyqB? MVOyNlU2PjRyOR?=
MM1.S  MX3GeY5kfGmxbjDBd5NigQ>? NFfi[m4yODBvMUCwNEBvVQ>? NX3tbXh5OzBibXnu M335OGROW09? M{DlRoFkfGm4YYTld{BGWkwEoB?= NWXvc2ZEOjJ3NU[0NFk>
8226 NFX1[Y9HfW6ldHnvckBCe3OjeR?= MVWwMlUh|ryP NGXUc3U{OCCvaX6= MYTEUXNQ M4HzVolv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= MkXXNlI2PTZ2MEm=
MM1.S  MXXGeY5kfGmxbjDBd5NigQ>? MU[wMlUh|ryP M372[lMxKG2rbh?= MV;EUXNQ NU\wbpJMcW6mdXPld{Bi[3SrdnH0bY9vKG:oIGLBSkBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIF3FTy=> M13IPFIzPTV4NEC5
MCF-7 MYfGeY5kfGmxbjDBd5NigQ>? NXPlWItOPTBxMkCwM|UxOCCwTR?= MVyzNEBucW5? NH3WOYdld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? M3S1RVIzPDd4OEWy
T47D M{DaVGZ2dmO2aX;uJGF{e2G7 NXviOZJLPTBxMkCwM|UxOCCwTR?= MVezNEBucW5? M{LOVIRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 M3LzW|IzPDd4OEWy
MDA-MB-231 MXzGeY5kfGmxbjDBd5NigQ>? NHnpUlg2OC9{MECvOVAxKG6P M3PpZVMxKG2rbh?= Mk\z[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NF\4ZYszOjR5Nki1Ni=>
Bcap-37 M3vmNGZ2dmO2aX;uJGF{e2G7 M2XHTVUxNzJyMD:1NFAhdk1? NX30dlZYOzBibXnu M1LPVYRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 M3i5bVIzPDd4OEWy
MCF-7 NHLpd4hCeG:ydH;zbZMhSXO|YYm= NFTqTlIzODEEoH7N NUS1fHI6OzZiaB?= MlrQSG1UVw>? NG\PN2pqdmS3Y3XzJIFxd3C2b4Ppdy=> NYPvdG5GOjJ2N{[4OVI>
MDA-MB-231 MWfBdI9xfG:|aYOgRZN{[Xl? NGm2TG0zODEEoH7N M2XmNFM3KGh? M{XJSmROW09? M4P0UYlv\HWlZYOgZZBweHSxc3nz Mk\GNlI1PzZ6NUK=
Bcap-37 MVfBdI9xfG:|aYOgRZN{[Xl? NH;2NnEzODEEoH7N MYGzOkBp MlTYSG1UVw>? MXXpcoR2[2W|IHHwc5B1d3Orcx?= M33IUVIzPDd4OEWy
LS174T NGfseplHfW6ldHnvckBCe3OjeR?= NWjre2p3OTBxMUCwM|ExODBibl2= NUK3TlRuPiCq NVTpfZV2TE2VTx?= NYm5S28xcW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? M1rMeFIzPDBzMkm0
DLD-1  MmHSSpVv[3Srb36gRZN{[Xl? MUWxNE8yODBxMUCwNEBvVQ>? NULHbmhzPiCq M1nwZWROW09? MlXqbY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> NGPFSIgzOjRyMUK5OC=>
SW480 MVrGeY5kfGmxbjDBd5NigQ>? MVSxNE8yODBxMUCwNEBvVQ>? M1ewT|YhcA>? NGTybWJFVVOR NGHMNW5qdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv M13wRVIzPDBzMkm0
SW-48 M136S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljZTWM2OD1yLkGg{txO M3[zelIzOjdyMkW3
HCT-15 NWHSZo16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHDNnhKSzVyPUCuN{DPxE1? M4G0clIzOjdyMkW3
HCT 116 NXLaTYt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3NWmtKSzVyPUCuOkDPxE1? NGPJboEzOjJ5MEK1Oy=>
SW620-R MnLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3faZ2lEPTB;MT6zJO69VQ>? MkXJNlIzPzB{NUe=
SK-CO-1 M4j1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTJwMTFOwG0> NITLRWgzOjJ5MEK1Oy=>
SW620 M3nIR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnyTWM2OD1zMTFOwG0> NH7aUHYzOjJ5MEK1Oy=>
BaF3 MkS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4j1RmdKPTB;MT60OFkh|ryP MYGyNlIzOzZ2NR?=
NIH 3T3 MUTGeY5kfGmxbjDBd5NigQ>? M4TuOFIh|ryP M176eVE5KGh? NVH3Wop1cW6qaXLpeJMhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3Rib36gV4VzPDd|IHHu[EBuXE:UQ{GgdIhwe3Cqb4L5cIF1cW:wIH;mJFRGNUKSMTDvckBVcHJ|Nz:0Oi=> NFq1TXozOTh5NkGzNC=>
HCT15 MXLGeY5kfGmxbjDBd5NigQ>? MXiwMlUwOiEQvF2= M4T4NVQhcA>? NITWUG1xemW4ZX70d{BUPktzIIDoc5NxcG:{eXzheIlwdiCxZjDybYJwe2:vYXygdJJwfGWrbjDTOkBifCCVZYKyOFAwOjR2IHHu[EBuXE:UQ{KgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfCCjdDDT[ZI1PzN? NWjSNHpGOjF6N{[xN|A>
SW620  M{jPZmZ2dmO2aX;uJGF{e2G7 MlfuNE42NzJizszN NU\pT3hCPCCq NWT0Tplv[myxY3vzJIFtdCC2aILl[UBuXE:UIH;1eJB2fHN? M{P3c|IyQDd4MUOw

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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
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    Volume
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*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.

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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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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