Torkinib (PP242)

For research use only.

Catalog No.S2218

68 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.

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Selleck's Torkinib (PP242) has been cited by 68 publications

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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. 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 NXXpb4RKTnWwY4Tpc44hSXO|YYm= MmfIOVAuOTJ3MDDuUS=> MViyOEBp MkCzSG1UVw>? MX\pcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Yhc2mwYYPlJEh1[XKpZYSgc4YhdVSRUlOxLUBidmRiaYTzJIRwf26|dILlZY0hfGG{Z3X0JJBpd3OyaH:tV|bDqA>? Mk[5NlYyPzdyNUG=
U87vIII  M4fCc2Z2dmO2aX;uJGF{e2G7 MmfmNE4xPC1{LkWg{txO M4T3R|I1KGh? Mmq4bY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh NHrxdGszPjF|NE[xOy=>
U87vIII  NXnBUGYyTnWwY4Tpc44hSXO|YYm= M2DjblIvPS93IN88US=> MXGxNkBp MlTMbY5pcWKrdIOg[4FxKGOub4PpcochcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUOyOlE{PDZzNx?=
PC12  M2nvWGZ2dmO2aX;uJGF{e2G7 MoLDOFDDqG6P NWLoXGxqcW6mdXPld{BtgXOxc3;tZYwh[mmxZ3Xu[ZNqeyCjbnSgZYxt\X[rYYTl[EDPuS2VWV6gZYNkfW23bHH0bY9vyqB? MYeyOlAxOTZzNB?=
3T3-L1 MoqxSpVv[3Srb36gRZN{[Xl? NH3xTWsyPSEQvF2= NIDHWY81KGh? MYLzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGVoejFicILveIVqdsLi Mn24NlU5OTR4NkK=
Rh30 NUfP[HpGTnWwY4Tpc44hSXO|YYm= MV2xJO69VQ>? MUeyJIg> Mn7MbY5pcWKrdIOgZo91cCCvVF;SR|EudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKFN4S{GgZY5lKG2WT2LDNk1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhSWu2 M2WxOVI2PzZ{NkG5
HT29 NGjlSllHfW6ldHnvckBCe3OjeR?= MmrQNUDPxE1? M{mwRlIhcA>? MXLpcohq[mm2czDic5RpKG2WT2LDNU1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhWz[NMTDhcoQhdVSRUlOyMY1m\GmjdHXkJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? NWix[2ZKOjV5NkK2NVk>
Rh30 NXzuXoJkTnWwY4Tpc44hSXO|YYm= M4LqSVEh|ryP M4TzWFIhcA>? M2\tTZN2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> MmjDNlU4PjJ4MUm=
HT29 NF3W[INHfW6ldHnvckBCe3OjeR?= NGm1PIMyKM7:TR?= MY[yJIg> M3r4c5N2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> MlX4NlU4PjJ4MUm=
U87 M3vrfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;IR3F1OjVibl2= MoLyNlQhcA>? NUj1VHJPcW6lcnXhd4V{KESXU2CxNEBsdm:la3XkMYRwf25iaX7keYNm\CClZXzsJIlvcGmkaYTpc44> M4TrU|I2PTZ6Nk[1
AGS MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlfLNE0yODByIH7N MkXYNlQwPDhiaB?= NWTnVYpxTE2VTx?= Mn;C[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUWyOVA{PTl4MR?=
MKN45 MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUOwMVExODBibl2= NITBNlIzPC92ODDo M3\Qb2ROW09? MlTs[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mor4NlUxOzV7NkG=
MKN28 MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVnpe3ExOC1zMECwJI5O MYGyOE81QCCq MlX0SG1UVw>? NUKzPFZp\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MX[yOVA{PTl4MR?=
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SGC7901 NEXTVZBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2rRNlAuOTByMDDuUS=> M4T4SFI1NzR6IHi= MnGzSG1UVw>? MXLk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MUGyOVA{PTl4MR?=
N87 MlXSR4VtdCCYaXHibYxqfHliQYPzZZk> NFGyRnkxNTFyMECgcm0> M{S1UlI1NzR6IHi= NWfWNnJPTE2VTx?= Mm\s[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MXeyOVA{PTl4MR?=
HMEC MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYPCVIlEOC1zMECwJI5O MmXjNlQwPDhiaB?= Mn:xSG1UVw>? MljE[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MXqyOVA{PTl4MR?=
HUVEC MnuyR4VtdCCYaXHibYxqfHliQYPzZZk> NHP0SoUxNTFyMECgcm0> NWTNNm5nOjRxNEigbC=> MonRSG1UVw>? M4P5fIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NEG2V|czPTB|NUm2NS=>
MG63 MoD1SpVv[3Srb36gRZN{[Xl? MkTMOVAuOTByMDDuUS=> NUK3SXpxOC53IHi= M{jNZYRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NHnJNFkzPDh2MEGzOC=>
U2OS  NGO5V2pHfW6ldHnvckBCe3OjeR?= NIXCTno2OC1zMECwJI5O MoG4NE42KGh? MlTI[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 MUWyOFg1ODF|NB?=
Saos-2  MV;GeY5kfGmxbjDBd5NigQ>? NXKwb3pvPTBvMUCwNEBvVQ>? NIHWPFExNjViaB?= NH\EdlBld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> M2rONVI1QDRyMUO0
Saos-2 NWjhUYFlTnWwY4Tpc44hSXO|YYm= NXz2eVNlOTByIH7N M3T0dVAvPSCq NUn6XItYeHKndnXueJMhd3O2ZX;zZZJkd22jIHPlcIwhdWmpcnH0bY9v NWj0VXQ5OjR6NECxN|Q>
MG63 Mlq5RZBweHSxc3nzJGF{e2G7 MYmxNFAhdk1? NFLQeZk{PiCq M3K2TZBzd22xdHXzJIFxd3C2b4Ppdy=> NYHse2NZOjR6NECxN|Q>
U2OS  MnqzRZBweHSxc3nzJGF{e2G7 MWGxNFAhdk1? NV3DbpV7OzZiaB?= MWDwdo9ud3SnczDhdI9xfG:|aYO= Mn\iNlQ5PDBzM{S=
Saos-2  NUH6To54SXCxcITvd4l{KEG|c3H5 MUixNFAhdk1? M4D4O|M3KGh? M2npOpBzd22xdHXzJIFxd3C2b4Ppdy=> NFzmWnkzPDh2MEGzOC=>
HT1376 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwOEigxtEhOS5zIN88US=> M3\ZflI1ODV2OEex
T24 M2iyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWT3Oo1UUUN3ME2xMlM4KMLzIECuOEDPxE1? NUnyUpp3OjRyNUS4O|E>
UM-UC-3 NYLXNIh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwNkOgxtExNjFizszN NUDtfIRjOjRyNUS4O|E>
DLD-1 NH7M[5pE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NV\jO|llOC1zMECwJI5O NEjrSHgzPCCq NWSyZWVJcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWnJ[4JLOjN7OUGxO|k>
Caco2 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUD6VoM1OC1zMECwJI5O NE\rd5ozPCCq M2HqfIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUTkb3pWOjN7OUGxO|k>
HT29 NEDnSXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVL1enhxOC1zMECwJI5O NUfONohZOjRiaB?= MV\pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlfyNlM6QTFzN{m=
H116 M4XXVGNmdGxiVnnhZoltcXS7IFHzd4F6 NWrqPJd6OC1zMECwJI5O MnnUNlQhcA>? NIfvbXBqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoPSNlM6QTFzN{m=
Hct-8 M{ixPWNmdGxiVnnhZoltcXS7IFHzd4F6 M17IXVAuOTByMDDuUS=> NInaeIYzPCCq MX7pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MYeyN|k6OTF5OR?=
Colo320 NYH5O2k3S2WubDDWbYFjcWyrdImgRZN{[Xl? NU\Vb|FTOC1zMECwJI5O M2XUOFI1KGh? MoTCbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4f5WFI{QTlzMUe5
Sw948 MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MY[wMVExODBibl2= M{HofVI1KGh? MlzrbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mlj6NlM6QTFzN{m=
Colo205 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoDINE0yODByIH7N Mn3uNlQhcA>? Mo[wbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NW[1V3V6OjN7OUGxO|k>
Colo320 MmfRSpVv[3Srb36gRZN{[Xl? MX6xJO69VQ>? MV6wMVI1KGh? NFXR[JNi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 MYmyN|k6OTF5OR?=
HT29 MUDGeY5kfGmxbjDBd5NigQ>? NWPXWo1KOSEQvF2= NGLBSoQxNTJ2IHi= MmPmZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> NWnGN|ZOOjN7OUGxO|k>
Sw948 MnrhSpVv[3Srb36gRZN{[Xl? M33mcVEh|ryP NVnsfIFbOC1{NDDo MW\hZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 NFjHVXYzOzl7MUG3PS=>
DLD-1 NHrMNpZHfW6ldHnvckBCe3OjeR?= NX\FOpF6OSEQvF2= MmjSNE0zPCCq M4GyOoFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> MVKyN|k6OTF5OR?=
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SW480 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrMTWM2OD12Lk[g{txO NEfDOZAzOzV2MkG3PC=>
SK-CO-1 NUnTSotNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTRizszN MVeyN|U1OjF5OB?=
LS-513 NVXmb5hLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWiyeVNkUUN3ME2zMlkh|ryP MViyN|U1OjF5OB?=
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LS-174T NEWyXYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NISxV4NKSzVyPUCuPFQh|ryP MVqyN|U1OjF5OB?=
HCT 116 NELjbG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PDTGlEPTB;MD60NUDPxE1? NX7NSnJjOjN3NEKxO|g>
HCT 15 NF7INllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zCc2lEPTB;MD6zJO69VQ>? NFmyWpAzOzV2MkG3PC=>
COLO 205 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnP5TWM2OD1yLkK0JO69VQ>? NVyzWJh2OjN3NEKxO|g>
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COLO 201 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrMZmlKSzVyPUCuNlMh|ryP NGPNW44zOzV2MkG3PC=>
Caco-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;OOWdKSzVyPUCuNlIh|ryP Moq0NlM2PDJzN{i=
SW48 NYnWPVg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwMEmg{txO Mn3YNlM2PDJzN{i=
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TMD8 NIrNeYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zZVlAvOjVxMD61M|Eh|ryP MV3EUXNQ NFzoSIFqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NVPMVVdIOjN2OEK3OFg>
Jurkat MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[0XI4xNjJ3L{CuOU8yKM7:TR?= M2P0WGROW09? M1O0[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MYSyN|Q5Ojd2OB?=
KOPT-K1 M4\tO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqwMlI2NzBwNT:xJO69VQ>? MoPrSG1UVw>? MY\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M{TnWFI{PDh{N{S4
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786-O MlvvSpVv[3Srb36gRZN{[Xl? M2fXTlAvOS9yLkWg{txO MXqyOEBp M{DDTGROW09? MYPpcoNz\WG|ZYOgSU1k[WSqZYLpckBuWk6DIHzleoVteyCmb4PlJIRmeGWwZHXueIx6 M1;kNFI{OTR5MkWx
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OCI-AML3 NFjocYlCeG:ydH;zbZMhSXO|YYm= NG\SfGUzNjVizszN MnPkO|IhcA>? MoPEbY5lfWOnczDhdI9xfG:|aYO= NYPLW3lOOjJ6Mk[1OlU>
Jurkat MoXPSpVv[3Srb36gRZN{[Xl? Mn[yNVAxNzJyMD:0NFAhdk1? NFXNb4MyQCCq NUf3c5YxcW6qaXLpeJMhdVSRUlOxMYRmeGWwZHXueEBUPiCVMkO1M|I{PiCyaH;zdIhwenmuYYTpc44> NGnDd3gzOjV4Nk[wOC=>
p210 BCR-Abl MV;GeY5kfGmxbjDBd5NigQ>? MYWxNFAwOjByL{SwNEBvVQ>? MVGxPEBp MkPkbY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= M2PjSVIzPTZ4NkC0
Jurkat M1nl[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUW0NFBvVQ>? NWfTVZdqOjRxNEigbC=> NHT2fJB{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u NILoVG0zOjV4Nk[wOC=>
p210 BCR-Abl NF\1VoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\YNlQxOG6P Mm\2NlQwPDhiaB?= MmPSd5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= NVPTOJJZOjJ3Nk[2NFQ>
8226 MmXNSpVv[3Srb36gRZN{[Xl? M1HMPVExOC1zMECwJI5O NUTvZVRwOzBibXnu NV3XTZZWTE2VTx?= Mo\5ZYN1cX[jdHXzJGVTU8Li NYrZO5N5OjJ3NU[0NFk>
MM1.S  M3;GU2Z2dmO2aX;uJGF{e2G7 NWqxc2FUOTByLUGwNFAhdk1? M1W1[lMxKG2rbh?= MnS1SG1UVw>? Mm\0ZYN1cX[jdHXzJGVTU8Li M4X4ZlIzPTV4NEC5
8226 MnziSpVv[3Srb36gRZN{[Xl? NWm3VFNyOC53IN88US=> MVqzNEBucW5? NFrXUmFFVVOR NIXUWHVqdmS3Y3XzJIFkfGm4YYTpc44hd2ZiUlHGJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiTVXL NHvNO4YzOjV3NkSwPS=>
MM1.S  M4rpOmZ2dmO2aX;uJGF{e2G7 MWewMlUh|ryP MVKzNEBucW5? NHTqc|FFVVOR MXPpcoR2[2W|IHHjeIl3[XSrb36gc4YhWkGIIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhVUWN NYDlUmZyOjJ3NU[0NFk>
MCF-7 NIHoS3RHfW6ldHnvckBCe3OjeR?= M3TJeFUxNzJyMD:1NFAhdk1? MUOzNEBucW5? NYDWVnpz\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? M33DN|IzPDd4OEWy
T47D NFXISWhHfW6ldHnvckBCe3OjeR?= MXe1NE8zODBxNUCwJI5O MkP6N|AhdWmw MWLkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NIHVN|gzOjR5Nki1Ni=>
MDA-MB-231 MmjrSpVv[3Srb36gRZN{[Xl? NV70[FJSPTBxMkCwM|UxOCCwTR?= NYHkRW5COzBibXnu NWry[HVk\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? NW\uU3Y2OjJ2N{[4OVI>
Bcap-37 M4ruSmZ2dmO2aX;uJGF{e2G7 NIfNRoM2OC9{MECvOVAxKG6P NYj5OJVIOzBibXnu MoCz[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MonzNlI1PzZ6NUK=
MCF-7 NGrDTW5CeG:ydH;zbZMhSXO|YYm= MYGyNFDDqG6P NWXxOI9EOzZiaB?= M{PIc2ROW09? NUTReJptcW6mdXPld{BieG:ydH;zbZM> M1fCW|IzPDd4OEWy
MDA-MB-231 M3rxW2Fxd3C2b4Ppd{BCe3OjeR?= MoPBNlAxyqCwTR?= MWWzOkBp MoDLSG1UVw>? NXLVNWdvcW6mdXPld{BieG:ydH;zbZM> M4jYU|IzPDd4OEWy
Bcap-37 MmDuRZBweHSxc3nzJGF{e2G7 MUKyNFDDqG6P MlnFN|YhcA>? MUDEUXNQ NIP5U2xqdmS3Y3XzJIFxd3C2b4Ppdy=> M4nMVlIzPDd4OEWy
LS174T Mk\kSpVv[3Srb36gRZN{[Xl? MkHONVAwOTByL{GwNFAhdk1? M{DXcFYhcA>? NVOzRmpmTE2VTx?= MVPpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu MVOyNlQxOTJ7NB?=
DLD-1  M2K0RmZ2dmO2aX;uJGF{e2G7 MUixNE8yODBxMUCwNEBvVQ>? MUi2JIg> M4GxfWROW09? MkSybY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> NUfKdotTOjJ2MEGyPVQ>
SW480 M37lfGZ2dmO2aX;uJGF{e2G7 MYmxNE8yODBxMUCwNEBvVQ>? MXO2JIg> MVvEUXNQ M3TaO4lvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> MVeyNlQxOTJ7NB?=
SW-48 Mn7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwMTFOwG0> MWCyNlI4ODJ3Nx?=
HCT-15 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfmeHNKSzVyPUCuN{DPxE1? MWeyNlI4ODJ3Nx?=
HCT 116 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPDNJN4UUN3ME2wMlYh|ryP NGHFS2MzOjJ5MEK1Oy=>
SW620-R NE\tU|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHexXWdKSzVyPUGuN{DPxE1? MWSyNlI4ODJ3Nx?=
SK-CO-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mne3TWM2OD1{LkGg{txO M1XwRlIzOjdyMkW3
SW620 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C4dGlEPTB;MUGg{txO MWGyNlI4ODJ3Nx?=
BaF3 NIfmSWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPOS2k2OD1zLkS0PUDPxE1? NGXTW|QzOjJ{M{[0OS=>
NIH 3T3 NWjnOoFNTnWwY4Tpc44hSXO|YYm= NVP0T3FsOiEQvF2= MkDwNVghcA>? MVfpcohq[mm2czDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBwdiCVZYK0O|Mh[W6mIH3UU3JEOSCyaH;zdIhwenmuYYTpc44hd2ZiNFWtRnAyKG:wIGTodlM4NzR4 MWSyNVg4PjF|MB?=
HCT15 NF72T5ZHfW6ldHnvckBCe3OjeR?= M1jKS|AvPS9{IN88US=> NYSz[JU5PCCq M2TybJBz\X[nboTzJHM3UzFicHjvd5Bpd3K7bHH0bY9vKG:oIILpZo9{d22jbDDwdo91\WmwIGO2JIF1KFOnckK0NE8zPDRiYX7kJI1VV1KFMjDwbI9{eGixconsZZRqd25ib3[gRYt1KGG2IGPldlQ4Ow>? MnHzNlE5PzZzM{C=
SW620  NF74[FBHfW6ldHnvckBCe3OjeR?= NG\6bogxNjVxMjFOwG0> MV:0JIg> M4LZd4Jtd2OtczDhcIwhfGi{ZXWgcXRQWiCxdYTweZR{ MnXhNlE5PzZzM{C=

... 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 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