Torkinib (PP242)

For research use only.

Catalog No.S2218

63 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 63 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 NXjMS|ZzTnWwY4Tpc44hSXO|YYm= MVi1NE0yOjVyIH7N MlfiNlQhcA>? MYTEUXNQ NFvPT3ZqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZia3nuZZNmKCi2YYLn[ZQhd2ZibWTPVmMyMSCjbnSgbZR{KGSxd37zeJJm[W1idHHy[4V1KHCqb4PwbI8uWzcEoB?= MYKyOlE4PzB3MR?=
U87vIII  M{Cwc2Z2dmO2aX;uJGF{e2G7 MV6wMlA1NTJwNTFOwG0> MVqyOEBp MmHTbY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh M{S5UVI3OTN2NkG3
U87vIII  M2\5T2Z2dmO2aX;uJGF{e2G7 NGPoXlIzNjVxNTFOwG0> NF33UpYyOiCq M2n5SIlvcGmkaYTzJIdieCClbH;zbY5oKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MV6yOlE{PDZzNx?=
PC12  Ml\pSpVv[3Srb36gRZN{[Xl? NHfXXVc1OMLibl2= M{XUeolv\HWlZYOgcJl{d3OxbXHsJIJqd2enbnXzbZMh[W6mIHHscIV3cWG2ZXSg{tEuW1mQIHHjZ5VufWyjdHnvcuKh MYGyOlAxOTZzNB?=
3T3-L1 M{PPT2Z2dmO2aX;uJGF{e2G7 M{fkWFE2KM7:TR?= M{CybFQhcA>? M4nSN5N2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhTWe{MTDwdo91\WmwwrC= NWHES2RiOjV6MUS2OlI>
Rh30 MmDVSpVv[3Srb36gRZN{[Xl? NVnrRWZ7OSEQvF2= NI[w[lUzKGh? M1HNcYlvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= NVfrXos{OjV5NkK2NVk>
HT29 MnO3SpVv[3Srb36gRZN{[Xl? MmnyNUDPxE1? NXfXXXhDOiCq MYTpcohq[mm2czDic5RpKG2WT2LDNU1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhWz[NMTDhcoQhdVSRUlOyMY1m\GmjdHXkJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MofENlU4PjJ4MUm=
Rh30 NF;XNVBHfW6ldHnvckBCe3OjeR?= MknJNUDPxE1? NF3XOIUzKGh? MmDVd5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u MXyyOVc3OjZzOR?=
HT29 NVfRWHp3TnWwY4Tpc44hSXO|YYm= NVvsXHBtOSEQvF2= M33C[lIhcA>? M4PiOZN2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> MmDHNlU4PjJ4MUm=
U87 NVzwNZJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXkbZgzPSCwTR?= MnnZNlQhcA>? M4jCcolv[3KnYYPld{BFXVOSMUCgb45w[2unZD3kc5dvKGmwZIXj[YQh[2WubDDpcohq[mm2aX;u NVvRbJh6OjV3Nki2OlU>
AGS MojNR4VtdCCYaXHibYxqfHliQYPzZZk> M4SxfFAuOTByMDDuUS=> M1LwR|I1NzR6IHi= MlzrSG1UVw>? NWWwTFJq\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NVL5Nol[OjVyM{W5OlE>
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SGC7901 M3n3VWNmdGxiVnnhZoltcXS7IFHzd4F6 MmLRNE0yODByIH7N MkTvNlQwPDhiaB?= M2j3NmROW09? MljQ[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUeyOVA{PTl4MR?=
N87 M4DJXGNmdGxiVnnhZoltcXS7IFHzd4F6 MVSwMVExODBibl2= MmT1NlQwPDhiaB?= Mm[wSG1UVw>? M4LxdYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MkLtNlUxOzV7NkG=
HMEC MnzwR4VtdCCYaXHibYxqfHliQYPzZZk> NXGyTYhROC1zMECwJI5O MmG1NlQwPDhiaB?= MYHEUXNQ MV7k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M3;mclI2ODN3OU[x
HUVEC M3TqU2NmdGxiVnnhZoltcXS7IFHzd4F6 M12zPFAuOTByMDDuUS=> NIXnPJYzPC92ODDo NI\IXlFFVVOR MlLN[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MYGyOVA{PTl4MR?=
MG63 NGm4XZlHfW6ldHnvckBCe3OjeR?= Mnn2OVAuOTByMDDuUS=> MofvNE42KGh? NF:xcZRld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MWSyOFg1ODF|NB?=
U2OS  MlfFSpVv[3Srb36gRZN{[Xl? M2\ETVUxNTFyMECgcm0> NIW5fGsxNjViaB?= M1\TRYRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M3HCU|I1QDRyMUO0
Saos-2  MV;GeY5kfGmxbjDBd5NigQ>? Mk\jOVAuOTByMDDuUS=> MXSwMlUhcA>? MoPC[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NVLUXWVjOjR6NECxN|Q>
Saos-2 MXzGeY5kfGmxbjDBd5NigQ>? MYCxNFAhdk1? NGDNb3YxNjViaB?= M4PtfpBz\X[nboTzJI9{fGWxc3HyZ49u[SClZXzsJI1q\3KjdHnvci=> NIrBVXUzPDh2MEGzOC=>
MG63 MW\BdI9xfG:|aYOgRZN{[Xl? M4jKUlExOCCwTR?= MlzMN|YhcA>? MV7wdo9ud3SnczDhdI9xfG:|aYO= MX:yOFg1ODF|NB?=
U2OS  MmH2RZBweHSxc3nzJGF{e2G7 M{P0bFExOCCwTR?= M3q2W|M3KGh? NHnpUmVxem:vb4Tld{BieG:ydH;zbZM> NVrYb|VsOjR6NECxN|Q>
Saos-2  M{\2RmFxd3C2b4Ppd{BCe3OjeR?= MmDBNVAxKG6P M3fsclM3KGh? MWfwdo9ud3SnczDhdI9xfG:|aYO= MmPhNlQ5PDBzM{S=
HT1376 M{DrTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHUWpJwUUN3ME2xMlg5KMLzIEGuNUDPxE1? MmK1NlQxPTR6N{G=
T24 MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTFwM{egxtEhOC52IN88US=> NVPSO4xnOjRyNUS4O|E>
UM-UC-3 NI\PVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjMbJBrUUN3ME2wMlY{KMLzMD6xJO69VQ>? NV\wRnc4OjRyNUS4O|E>
DLD-1 Moi2R4VtdCCYaXHibYxqfHliQYPzZZk> NHnN[m4xNTFyMECgcm0> MnnRNlQhcA>? M3;HSIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVWwdFNrOjN7OUGxO|k>
Caco2 Mm\qR4VtdCCYaXHibYxqfHliQYPzZZk> NG[wU|IxNTFyMECgcm0> NIrZUnMzPCCq NWGz[ZducW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmH1NlM6QTFzN{m=
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H116 M{jLcGNmdGxiVnnhZoltcXS7IFHzd4F6 NV[3XYM1OC1zMECwJI5O MYKyOEBp NGrCZYhqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2PyO|I{QTlzMUe5
Hct-8 NF\VVW9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYnLTIg6OC1zMECwJI5O NGnQe3QzPCCq M4fLZ4lvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NX7IZ|l3OjN7OUGxO|k>
Colo320 NE\nfmZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXXYXIw3OC1zMECwJI5O M3;TT|I1KGh? NHPTcpVqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlLrNlM6QTFzN{m=
Sw948 NG[0NVRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUHR[ZZ4OC1zMECwJI5O MmnONlQhcA>? NV\JVYtPcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1rBO|I{QTlzMUe5
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Colo320 M{PCb2Z2dmO2aX;uJGF{e2G7 NEjYfnAyKM7:TR?= NUT3eVJtOC1{NDDo M4LPWIFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> NU[3dY8zOjN7OUGxO|k>
HT29 MX3GeY5kfGmxbjDBd5NigQ>? M{\UbVEh|ryP M3:wc|AuOjRiaB?= NXm2c|lD[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? NFXBd5UzOzl7MUG3PS=>
Sw948 MkXtSpVv[3Srb36gRZN{[Xl? M3jKcFEh|ryP NV75c25[OC1{NDDo M2fIR4Fjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> Mo[5NlM6QTFzN{m=
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SW620 M2LSOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrSeHpKSzVyPUeuPEDPxE1? MoDiNlM2PDJzN{i=
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SK-CO-1 NGnIbWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTYTWM2OD12IN88US=> MX2yN|U1OjF5OB?=
LS-513 NEj2OohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTNwOTFOwG0> MUeyN|U1OjF5OB?=
SW1116 NICzZVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{T1bWlEPTB;MD64OEDPxE1? NYCyfYNFOjN3NEKxO|g>
LS-174T NY\Cc4h4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fMO2lEPTB;MD64OEDPxE1? NWXpUWh6OjN3NEKxO|g>
HCT 116 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TpV2lEPTB;MD60NUDPxE1? MoPXNlM2PDJzN{i=
HCT 15 NYTN[3lLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPUTWM2OD1yLkOg{txO NHnQNVUzOzV2MkG3PC=>
COLO 205 NGT0WIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml6wTWM2OD1yLkK0JO69VQ>? M364ZlI{PTR{MUe4
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COLO 201 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TKbWlEPTB;MD6yN{DPxE1? MljsNlM2PDJzN{i=
Caco-2 MnfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrxTWM2OD1yLkKyJO69VQ>? MYSyN|U1OjF5OB?=
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DND-1 NFjOVmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3VTYoxNjJ3L{CuOU8yKM7:TR?= MUTEUXNQ NVPTTWtJcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NIX3d5QzOzR6Mke0PC=>
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Jurkat MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjBcZNnOC5{NT:wMlUwOSEQvF2= M1LMbWROW09? NHzJ[m9qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NFnwRnkzOzR6Mke0PC=>
KOPT-K1 NFrET5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfXWIcxNjJ3L{CuOU8yKM7:TR?= NVXHfWtJTE2VTx?= NWezW4tmcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NEPobVEzOzR6Mke0PC=>
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Jurkat M2nCdmZ2dmO2aX;uJGF{e2G7 NGjVfnkyODBxMkCwM|QxOCCwTR?= NUSyUoFnOThiaB?= M165TIlvcGmkaYTzJI1VV1KFMT3k[ZBmdmSnboSgV|YhWzJ|NT:yN|YheGixc4Doc5J6dGG2aX;u MoezNlI2PjZ4MES=
p210 BCR-Abl NV3OTHFRTnWwY4Tpc44hSXO|YYm= M3K1OVExOC9{MECvOFAxKG6P MUKxPEBp NUDNSZNEcW6qaXLpeJMhdVSRUlOxMYRmeGWwZHXueEBUPiCVMkO1M|I{PiCyaH;zdIhwenmuYYTpc44> NWTDVo1KOjJ3Nk[2NFQ>
Jurkat MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvnOFAxdk1? NGPkc|gzPC92ODDo NGLyeot{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u MnHJNlI2PjZ4MES=
p210 BCR-Abl NYGweFJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P2T|QxOG6P MkfyNlQwPDhiaB?= NIjSbVV{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u NEnIeHIzOjV4Nk[wOC=>
8226 MlnKSpVv[3Srb36gRZN{[Xl? MUSxNFAuOTByMDDuUS=> NXHMRnVsOzBibXnu MWrEUXNQ MW\hZ5RqfmG2ZYOgSXJMyqB? MUCyNlU2PjRyOR?=
MM1.S  NFzxV2lHfW6ldHnvckBCe3OjeR?= NYPZ[3FUOTByLUGwNFAhdk1? NUnYcWQ3OzBibXnu M1j0ZWROW09? NV7YcoRN[WO2aY\heIV{KEWUS9Mg NGfQW4UzOjV3NkSwPS=>
8226 NXrBU|lETnWwY4Tpc44hSXO|YYm= MYmwMlUh|ryP M4jBTFMxKG2rbh?= M3XBRWROW09? M1Ty[Ilv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= MlSwNlI2PTZ2MEm=
MM1.S  Ml:zSpVv[3Srb36gRZN{[Xl? NUjIe29NOC53IN88US=> NWPVV5dQOzBibXnu M4qyemROW09? M1vkPYlv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= MUiyNlU2PjRyOR?=
MCF-7 MUDGeY5kfGmxbjDBd5NigQ>? NXPpUo1QPTBxMkCwM|UxOCCwTR?= MYCzNEBucW5? MnjR[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MXSyNlQ4Pjh3Mh?=
T47D MoLrSpVv[3Srb36gRZN{[Xl? MX:1NE8zODBxNUCwJI5O MmTuN|AhdWmw Mn\z[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NES4XIwzOjR5Nki1Ni=>
MDA-MB-231 M1q0emZ2dmO2aX;uJGF{e2G7 NHjGZpI2OC9{MECvOVAxKG6P MW[zNEBucW5? NEXHeIZld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? M1jrXFIzPDd4OEWy
Bcap-37 NIDkUVdHfW6ldHnvckBCe3OjeR?= MVi1NE8zODBxNUCwJI5O MoHEN|AhdWmw MXzkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NGjwNo8zOjR5Nki1Ni=>
MCF-7 MlPGRZBweHSxc3nzJGF{e2G7 MXyyNFDDqG6P MYqzOkBp NYKyR5pETE2VTx?= M3SzW4lv\HWlZYOgZZBweHSxc3nz NWXQRnBvOjJ2N{[4OVI>
MDA-MB-231 NF21bXVCeG:ydH;zbZMhSXO|YYm= NETI[WIzODEEoH7N NFLxZoY{PiCq M2fiOmROW09? M4nXbYlv\HWlZYOgZZBweHSxc3nz NF\vbIszOjR5Nki1Ni=>
Bcap-37 M1W1VmFxd3C2b4Ppd{BCe3OjeR?= MV:yNFDDqG6P M4PSSVM3KGh? NGW5fo5FVVOR MXPpcoR2[2W|IHHwc5B1d3Orcx?= MmrLNlI1PzZ6NUK=
LS174T M4rDc2Z2dmO2aX;uJGF{e2G7 M4\WNlExNzFyMD:xNFAxKG6P NGnkNWg3KGh? NHj1VIJFVVOR NUTWZY5KcW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? NUfs[2hmOjJ2MEGyPVQ>
DLD-1  Mkf5SpVv[3Srb36gRZN{[Xl? MWSxNE8yODBxMUCwNEBvVQ>? MU[2JIg> NUPtflZ{TE2VTx?= NITuOIFqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv NGnqcHgzOjRyMUK5OC=>
SW480 MW\GeY5kfGmxbjDBd5NigQ>? NFXKTY4yOC9zMECvNVAxOCCwTR?= Mnv0OkBp MWjEUXNQ MmPBbY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> NGPwdpQzOjRyMUK5OC=>
SW-48 MlXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\G[GZHUUN3ME2wMlEh|ryP MkW2NlIzPzB{NUe=
HCT-15 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nTemlEPTB;MD6zJO69VQ>? NWfpSoxQOjJ{N{CyOVc>
HCT 116 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwNjFOwG0> MXmyNlI4ODJ3Nx?=
SW620-R NGTMb2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH0TWM2OD1zLkOg{txO MUKyNlI4ODJ3Nx?=
SK-CO-1 NITDNZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\KZmlEPTB;Mj6xJO69VQ>? MYeyNlI4ODJ3Nx?=
SW620 NIruU4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjhNnFKSzVyPUGxJO69VQ>? MnrWNlIzPzB{NUe=
BaF3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fS[GdKPTB;MT60OFkh|ryP NHTpO3kzOjJ{M{[0OS=>
NIH 3T3 MoD4SpVv[3Srb36gRZN{[Xl? MYOyJO69VQ>? M1TndFE5KGh? MoKzbY5pcWKrdIOgcXRQWkN{IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qhd25iU3XyOFc{KGGwZDDtWG9TSzFicHjvd5Bpd3K7bHH0bY9vKG:oIETFMWJROSCxbjDUbJI{Py92Nh?= NXH3VFRkOjF6N{[xN|A>
HCT15 NGTXXXVHfW6ldHnvckBCe3OjeR?= M2XrNlAvPS9{IN88US=> Ml3OOEBp NV:xZ5FGeHKndnXueJMhWz[NMTDwbI9{eGixconsZZRqd25ib3[gdoljd3OxbXHsJJBzd3SnaX6gV|Yh[XRiU3XyNlQxNzJ2NDDhcoQhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3RiYYSgV4VzPDd| M1zLWVIyQDd4MUOw
SW620  MV\GeY5kfGmxbjDBd5NigQ>? NH\1WFQxNjVxMjFOwG0> NYT4VXBjPCCq NIn2O2xjdG:la4OgZYxtKHSqcnXlJI1VV1Jib4X0dJV1ew>? MkHKNlE5PzZzM{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