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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8 Customer Reviews

  • MTORC1 regulates the subcellular distribution of TFEB. Immunofluorescence confocal microscopy showing nuclear localization of recombinant TFEB-Flag in ARPE-19 cells incubated with MTORC1 inhibitors (PP242, LY294002, Wortmannin).

    Autophagy 2012 8(6), 903-14. Torkinib (PP242) purchased from Selleck.

    Pharmacological PP242 induces transport of TFEB to the nucleus. HeLa cells stably expressing TFEB (CF7) were incubated with the indicated kinase inhibitors and the electrophoretic mobility of TFEB was monitored by immunoblotting.

    Autophagy 2012 8(6), 903-14. Torkinib (PP242) purchased from Selleck.

  • AKT protein kinase activity controls protein synthesis by regulating the multistep process of mRNA translation at multiple stages from ribosome biogenesis to translation initiation and elongation. PC3-LN4 cells were treated with GSK690693 (5 uM) alone, or in combination with PP242 (2 uM) or AZD8055 (1 uM) for 24 h, and immunoblotting performed.

    Cancer Res 2013 73(11), 3402-11. Torkinib (PP242) purchased from Selleck.

    Synergistic effect of BMS-777607 with mTOR inhibitors in reduction of CSCs+24/44/ESA viability. CSCs+24/44/ESA at 5,000 cells per well with stem cell culture media in triplicate in an ultra-low adhesion plate were treated with 5 umol/L BMS-777607, 1 umol/L AZD8055, 1 umol/L RAD001, and 1 umol/L PP242 alone, or in their different combinations. Cells were cultured for 72 hours. Percentages of polyploid cells were determined by counting 300 cells from two different regions. Results shown here were from one of two experiments with similar results.

    Mol Cancer Ther 2014 13(1), 37-48. Torkinib (PP242) purchased from Selleck.

  • (A) MEF and PC3-LN4 cells were treated with GNE-652 or LGB321 in a dose dependent manner and PP242 (1 µmol/L) for 16 hr

    Oncotarget, 2016, 7(15):20152-65. Torkinib (PP242) purchased from Selleck.

    HeLa cells were treated with MK2206 (1 uM), rapamycin (Rapa; 100 nM), PP242 (1 uM), BEZ235 (0.5 uM), U0126 (U0; 15 uM), BI-D1870 (BI; 10 uM), GNE-652 (1 uM), AZD1208 (3 uM), and the indicated inhibitor combinations for 3 h. Cell lysates were analyzed by immunoblot assays using indicated antibodies.

    Mol Cell Biol 2014 34(13), 2517-32. Torkinib (PP242) purchased from Selleck.

  • Torkinib (PP242) purchased from Selleck.

    A549 cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of  PP242 for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. Torkinib (PP242) purchased from Selleck.

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
HT-p21 NX;aTFlbTnWwY4Tpc44hSXO|YYm= NFzNPI82OC1zMkWwJI5O MW[yOEBp NVn2dJh4TE2VTx?= MY\pcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Yhc2mwYYPlJEh1[XKpZYSgc4YhdVSRUlOxLUBidmRiaYTzJIRwf26|dILlZY0hfGG{Z3X0JJBpd3OyaH:tV|bDqA>? MnvCNlYyPzdyNUG=
U87vIII  NFXUWpBHfW6ldHnvckBCe3OjeR?= MV[wMlA1NTJwNTFOwG0> NH\jW4gzPCCq M{fhV4lvcGmkaYTzJI1VV1KFMTDhcoQhdVSRUlOyJIFkfGm4aYTp[ZPDqA>? M3frXVI3OTN2NkG3
U87vIII  M{DUbmZ2dmO2aX;uJGF{e2G7 MkLVNk42NzVizszN NYiwbGtyOTJiaB?= NVrLcYNkcW6qaXLpeJMh\2GyIHPsc5NqdmdiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYiyOlE{PDZzNx?=
PC12  MnPTSpVv[3Srb36gRZN{[Xl? Mmj0OFDDqG6P NWLiV4Y3cW6mdXPld{BtgXOxc3;tZYwh[mmxZ3Xu[ZNqeyCjbnSgZYxt\X[rYYTl[EDPuS2VWV6gZYNkfW23bHH0bY9vyqB? MXOyOlAxOTZzNB?=
3T3-L1 M2LqXGZ2dmO2aX;uJGF{e2G7 NHrXZpAyPSEQvF2= MnXDOEBp MWfzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGVoejFicILveIVqdsLi M3;QN|I2QDF2Nk[y
Rh30 MUHGeY5kfGmxbjDBd5NigQ>? M2rvN|Eh|ryP NHLtTG4zKGh? MlHzbY5pcWKrdIOgZo91cCCvVF;SR|EudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKFN4S{GgZY5lKG2WT2LDNk1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhSWu2 NU\2WnJYOjV5NkK2NVk>
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Rh30 NUXKZoxCTnWwY4Tpc44hSXO|YYm= MVmxJO69VQ>? MoLXNkBp Ml\Id5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u M1XuS|I2PzZ{NkG5
HT29 MXrGeY5kfGmxbjDBd5NigQ>? M3PKTVEh|ryP NFj2W4gzKGh? M1;BZZN2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> MUGyOVc3OjZzOR?=
U87 NFvUVVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzQdWUzPSCwTR?= Ml7JNlQhcA>? M13wVYlv[3KnYYPld{BFXVOSMUCgb45w[2unZD3kc5dvKGmwZIXj[YQh[2WubDDpcohq[mm2aX;u MXWyOVU3QDZ4NR?=
AGS NIrqdWVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NI\WbGQxNTFyMECgcm0> MnTnNlQwPDhiaB?= M{jnRmROW09? M160doRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MmjYNlUxOzV7NkG=
MKN45 Mly3R4VtdCCYaXHibYxqfHliQYPzZZk> NH;VSVUxNTFyMECgcm0> MnS0NlQwPDhiaB?= MVHEUXNQ NVPOeFJR\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NEflPXUzPTB|NUm2NS=>
MKN28 NX\hUG03S2WubDDWbYFjcWyrdImgRZN{[Xl? NHLBboExNTFyMECgcm0> MVWyOE81QCCq M17NdGROW09? NHfSRnFl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M{HpUlI2ODN3OU[x
KATO3 MnLtR4VtdCCYaXHibYxqfHliQYPzZZk> MoPSNE0yODByIH7N Mke2NlQwPDhiaB?= MonHSG1UVw>? NHTmPZVl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M4XOZlI2ODN3OU[x
SGC7901 MmS1R4VtdCCYaXHibYxqfHliQYPzZZk> NGOxVFUxNTFyMECgcm0> NIfOfWMzPC92ODDo MXnEUXNQ M4XSWoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M4L4bVI2ODN3OU[x
N87 Mm\KR4VtdCCYaXHibYxqfHliQYPzZZk> MUWwMVExODBibl2= NEfYZnEzPC92ODDo M{j1OWROW09? MYPk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NIO4bFczPTB|NUm2NS=>
HMEC MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUGwMVExODBibl2= MkPuNlQwPDhiaB?= NWjseVF5TE2VTx?= MUDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MYiyOVA{PTl4MR?=
HUVEC NHr6boFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlyzNE0yODByIH7N NIfhO2szPC92ODDo NFHTfotFVVOR NHzUeFll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NHrJ[XgzPTB|NUm2NS=>
MG63 NGTj[phHfW6ldHnvckBCe3OjeR?= NW\6fWI3PTBvMUCwNEBvVQ>? NH7FPIgxNjViaB?= MnWw[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M1nTSlI1QDRyMUO0
U2OS  MV\GeY5kfGmxbjDBd5NigQ>? NIHqWYc2OC1zMECwJI5O MXmwMlUhcA>? NFPvVFBld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NELDUVUzPDh2MEGzOC=>
Saos-2  NV\PfJlOTnWwY4Tpc44hSXO|YYm= NXi4OGs3PTBvMUCwNEBvVQ>? NH\XcJUxNjViaB?= NViyOppw\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 MWKyOFg1ODF|NB?=
Saos-2 MWDGeY5kfGmxbjDBd5NigQ>? M4C5fFExOCCwTR?= M2fBUVAvPSCq NFzYNVFxemW4ZX70d{Bwe3Snb4PhdoNwdWFiY3XscEBucWe{YYTpc44> M2T4WFI1QDRyMUO0
MG63 MYTBdI9xfG:|aYOgRZN{[Xl? MlK2NVAxKG6P NG\sOmk{PiCq M2HBNJBzd22xdHXzJIFxd3C2b4Ppdy=> MkXINlQ5PDBzM{S=
U2OS  NHL2c3VCeG:ydH;zbZMhSXO|YYm= M{jUdlExOCCwTR?= NEfaSmM{PiCq NWK1XJJDeHKxbX;0[ZMh[XCxcITvd4l{ M2rtdVI1QDRyMUO0
Saos-2  NWKzWlM2SXCxcITvd4l{KEG|c3H5 Ml3kNVAxKG6P NILJZ5I{PiCq MomydJJwdW:2ZYOgZZBweHSxc3nz MWeyOFg1ODF|NB?=
HT1376 MkTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTFwOEigxtEhOS5zIN88US=> MWqyOFA2PDh5MR?=
T24 NYrySpB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;J[5RKSzVyPUGuN|chyrFiMD60JO69VQ>? Ml\SNlQxPTR6N{G=
UM-UC-3 M1zx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;OWWpKSzVyPUCuOlMhyrFyLkGg{txO M3LjR|I1ODV2OEex
DLD-1 NFu1ZXdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUGwMVExODBibl2= M4PJS|I1KGh? NHvi[WdqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4LGUVI{QTlzMUe5
Caco2 Ml7JR4VtdCCYaXHibYxqfHliQYPzZZk> NISzU|AxNTFyMECgcm0> NWf5N|BkOjRiaB?= M3Xq[IlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3ToOFI{QTlzMUe5
HT29 MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{HjdFAuOTByMDDuUS=> MUGyOEBp NEXUTFlqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1;yd|I{QTlzMUe5
H116 NVm3TG9DS2WubDDWbYFjcWyrdImgRZN{[Xl? MYCwMVExODBibl2= MXSyOEBp NIe3UI1qdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3WzVlI{QTlzMUe5
Hct-8 MnzPR4VtdCCYaXHibYxqfHliQYPzZZk> NHe5XIkxNTFyMECgcm0> MYiyOEBp MX7pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M170UlI{QTlzMUe5
Colo320 NYTieYlQS2WubDDWbYFjcWyrdImgRZN{[Xl? NEfBTVcxNTFyMECgcm0> M{jDb|I1KGh? MV;pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MVGyN|k6OTF5OR?=
Sw948 NYK5O3R6S2WubDDWbYFjcWyrdImgRZN{[Xl? NVvJeXlLOC1zMECwJI5O NH7ndpkzPCCq NYfhN|RHcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWKyN|k6OTF5OR?=
Colo205 NIi0NFhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIrL[GQxNTFyMECgcm0> MnP1NlQhcA>? M3fZWolvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHXBSm0zOzl7MUG3PS=>
Colo320 NEfJRZpHfW6ldHnvckBCe3OjeR?= MlT2NUDPxE1? MXywMVI1KGh? MVLhZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 NHHMSI4zOzl7MUG3PS=>
HT29 NX7RT2NWTnWwY4Tpc44hSXO|YYm= NY[1SpVrOSEQvF2= NGnMcWIxNTJ2IHi= MnfCZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> NWf6bYE{OjN7OUGxO|k>
Sw948 M{DK[WZ2dmO2aX;uJGF{e2G7 MWqxJO69VQ>? M1e4[lAuOjRiaB?= NWrHWFBM[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MlzVNlM6QTFzN{m=
DLD-1 MUTGeY5kfGmxbjDBd5NigQ>? MYixJO69VQ>? NX6xO2dqOC1{NDDo M4njW4Fjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> NH7OdoMzOzl7MUG3PS=>
SW620 NHr0VZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXjSZZKSzVyPUeuPEDPxE1? NUDjUYdxOjN3NEKxO|g>
SW480 Mn3aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorkTWM2OD12Lk[g{txO M4PRU|I{PTR{MUe4
SK-CO-1 M{TNSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXSOoNKSzVyPUSg{txO M1zZN|I{PTR{MUe4
LS-513 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlT5TWM2OD1|Lkmg{txO NVfpe4p6OjN3NEKxO|g>
SW1116 NX\2e5p7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPwNWxKSzVyPUCuPFQh|ryP Ml:2NlM2PDJzN{i=
LS-174T MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUO3NIhbUUN3ME2wMlg1KM7:TR?= NFfaXFgzOzV2MkG3PC=>
HCT 116 M1;SNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwNEGg{txO NH7Eco4zOzV2MkG3PC=>
HCT 15 M4r0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rxd2lEPTB;MD6zJO69VQ>? MnfjNlM2PDJzN{i=
COLO 205 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwMkSg{txO NWfKPHZ2OjN3NEKxO|g>
HT-29 NIfodFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYntXHpxUUN3ME2wMlI{KM7:TR?= MYWyN|U1OjF5OB?=
COLO 201 NVK2eHZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLWWpg1UUN3ME2wMlI{KM7:TR?= MoTMNlM2PDJzN{i=
Caco-2 MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PUbmlEPTB;MD6yNkDPxE1? NGGwc3MzOzV2MkG3PC=>
SW48 Mki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXpTWM2OD1yLkC5JO69VQ>? MU[yN|U1OjF5OB?=
DND-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vkUVAvOjVxMD61M|Eh|ryP NIHNeJVFVVOR MnHLbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MV2yN|Q5Ojd2OB?=
TMD8 M1ztXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vjbVAvOjVxMD61M|Eh|ryP M3\RSmROW09? M{HVfIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NE\GSoMzOzR6Mke0PC=>
Jurkat Mlz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXzNE4zPS9yLkWvNUDPxE1? MUDEUXNQ NFvPOItqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NWfie5kyOjN2OEK3OFg>
KOPT-K1 M{DkT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\rPVAvOjVxMD61M|Eh|ryP Mn\NSG1UVw>? MVnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M1rkSlI{PDh{N{S4
TMD7 MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDSPWUxNjJ3L{CuOU8yKM7:TR?= M2DifGROW09? M33XRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NIHRcFEzOzR6Mke0PC=>
THP-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMlI2NzBwNT:xJO69VQ>? MmXySG1UVw>? NGXTeJdqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NGjnbIczOzR6Mke0PC=>
786-O M3\DN2Z2dmO2aX;uJGF{e2G7 M{XReVAvOS9yLkWg{txO MnTJNlQhcA>? MUDEUXNQ MW\pcoNz\WG|ZYOgSU1k[WSqZYLpckBuWk6DIHzleoVteyCmb4PlJIRmeGWwZHXueIx6 NX25Oo1JOjNzNEeyOVE>
786-O NYPzdHB3TnWwY4Tpc44hSXO|YYm= M4joNlAuOC53IN88US=> M3jLXVI1KGh? M2DOXmROW09? NWfKeIlkemW|dXz0d{BqdiCjIHTvd4Uh\GWyZX7k[Y51KGmwY4LlZZNmKGmwIFWtZ4FlcGW{aX6gdJJwfGWrbjDlfJBz\XO|aX;uxsA> NIfVNI4zOzF2N{K1NS=>
OCI-AML3 NFm0NFlCeG:ydH;zbZMhSXO|YYm= M3nac|IvPSEQvF2= M3[yc|czKGh? M1nVPYlv\HWlZYOgZZBweHSxc3nz NYDXOWVROjJ6Mk[1OlU>
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p210 BCR-Abl M2nmUWZ2dmO2aX;uJGF{e2G7 MkjZNVAxNzJyMD:0NFAhdk1? M4GxXVE5KGh? NXnR[nlwcW6qaXLpeJMhdVSRUlOxMYRmeGWwZHXueEBUPiCVMkO1M|I{PiCyaH;zdIhwenmuYYTpc44> M4DqR|IzPTZ4NkC0
Jurkat NVzOfoUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHCdY5TPDBybl2= MWGyOE81QCCq MVvzfY5memerenWge4l1cCBzNz3BRWchfG9ic4XwdJJme3NiY3XscEBxem:uaX\ldoF1cW:w MlHhNlI2PjZ4MES=
p210 BCR-Abl MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrBOFAxdk1? NVK1N3JROjRxNEigbC=> Mn\Xd5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= NEXXcI4zOjV4Nk[wOC=>
8226 MWrGeY5kfGmxbjDBd5NigQ>? M{nyS|ExOC1zMECwJI5O Mn\JN|AhdWmw MoLnSG1UVw>? NEC3WVZi[3SrdnH0[ZMhTVKNwrC= NXjrXm94OjJ3NU[0NFk>
MM1.S  NFS1U3VHfW6ldHnvckBCe3OjeR?= MWmxNFAuOTByMDDuUS=> NF3ISY4{OCCvaX6= NXi3fnNsTE2VTx?= M{PMVYFkfGm4YYTld{BGWkwEoB?= NWDxVmhiOjJ3NU[0NFk>
8226 MYDGeY5kfGmxbjDBd5NigQ>? MmHENE42KM7:TR?= MUKzNEBucW5? M2fnRmROW09? MUDpcoR2[2W|IHHjeIl3[XSrb36gc4YhWkGIIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhVUWN M4\4c|IzPTV4NEC5
MM1.S  M13QW2Z2dmO2aX;uJGF{e2G7 Mn7aNE42KM7:TR?= NEXXfnc{OCCvaX6= NVLoTohwTE2VTx?= MVLpcoR2[2W|IHHjeIl3[XSrb36gc4YhWkGIIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhVUWN M2DDcFIzPTV4NEC5
MCF-7 NUTYV3pyTnWwY4Tpc44hSXO|YYm= M3q4fFUxNzJyMD:1NFAhdk1? MXOzNEBucW5? MlTD[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> M1jWdlIzPDd4OEWy
T47D MmTOSpVv[3Srb36gRZN{[Xl? NYfWOJF{PTBxMkCwM|UxOCCwTR?= M{\aVlMxKG2rbh?= Ml35[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> Mmq1NlI1PzZ6NUK=
MDA-MB-231 NFXzS2NHfW6ldHnvckBCe3OjeR?= M3TVW|UxNzJyMD:1NFAhdk1? NHjoSmM{OCCvaX6= M1fMToRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 M1zUZVIzPDd4OEWy
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MCF-7 NEnNUoZCeG:ydH;zbZMhSXO|YYm= M2jjPFIxOMLibl2= NUT2bJhNOzZiaB?= MWXEUXNQ NVL5OGdrcW6mdXPld{BieG:ydH;zbZM> MUiyNlQ4Pjh3Mh?=
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SW620 NGjGUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXueIJKSzVyPUGxJO69VQ>? M3K0[|IzOjdyMkW3
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... Click to View More Cell Line Experimental Data

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:
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
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 (g) = Concentration (mol/L) × Volume (L) × 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