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.

Size Price Stock Quantity  
In DMSO USD 91 In stock
USD 70 In stock
USD 120 In stock
USD 370 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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 NEHmT4ZHfW6ldHnvckBCe3OjeR?= NFLacJc2OC1zMkWwJI5O NGH2OVkzPCCq MVPEUXNQ NHXQW2JqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZia3nuZZNmKCi2YYLn[ZQhd2ZibWTPVmMyMSCjbnSgbZR{KGSxd37zeJJm[W1idHHy[4V1KHCqb4PwbI8uWzcEoB?= MWKyOlE4PzB3MR?=
U87vIII  MonKSpVv[3Srb36gRZN{[Xl? MmXONE4xPC1{LkWg{txO MkPJNlQhcA>? MlGwbY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh NYDZTZpCOjZzM{S2NVc>
U87vIII  MnzMSpVv[3Srb36gRZN{[Xl? M1P2WlIvPS93IN88US=> MVmxNkBp MmfybY5pcWKrdIOg[4FxKGOub4PpcochcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVuxRmJROjZzM{S2NVc>
PC12  NXrzbld4TnWwY4Tpc44hSXO|YYm= NYTlR3ZjPDEEoH7N M2m5OIlv\HWlZYOgcJl{d3OxbXHsJIJqd2enbnXzbZMh[W6mIHHscIV3cWG2ZXSg{tEuW1mQIHHjZ5VufWyjdHnvcuKh NWPpSHUzOjZyMEG2NVQ>
3T3-L1 M2f5NWZ2dmO2aX;uJGF{e2G7 NGfNdpYyPSEQvF2= NULGNlZTPCCq MWTzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGVoejFicILveIVqdsLi MW[yOVgyPDZ4Mh?=
Rh30 MUnGeY5kfGmxbjDBd5NigQ>? M1\GZVEh|ryP NHTwUmYzKGh? NH7EW21qdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= M{TodFI2PzZ{NkG5
HT29 Ml24SpVv[3Srb36gRZN{[Xl? MVOxJO69VQ>? NV\RNo54OiCq M{nFRolvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= MoLENlU4PjJ4MUm=
Rh30 MVXGeY5kfGmxbjDBd5NigQ>? Mn\CNUDPxE1? Ml3CNkBp MmTvd5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u MlfaNlU4PjJ4MUm=
HT29 NHjUT2xHfW6ldHnvckBCe3OjeR?= NVfEVJlZOSEQvF2= M1ruOVIhcA>? MU\zeZBxemW|c3XzJJRp\SCkYYPhcEBweiCLR1[tNU1{fGmvdXzheIVlKGOnbHygZYRp\XOrb36= MknlNlU4PjJ4MUm=
U87 NYnDUnN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\E[WMzPSCwTR?= M4iydlI1KGh? NHHrWIlqdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> NHT2dVQzPTV4OE[2OS=>
AGS NWLjUlFIS2WubDDWbYFjcWyrdImgRZN{[Xl? Mm\4NE0yODByIH7N M2LNRVI1NzR6IHi= M13JVWROW09? MkX2[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NH7sUXozPTB|NUm2NS=>
MKN45 NHfqc|dE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkntNE0yODByIH7N Mmr5NlQwPDhiaB?= NIDVbVBFVVOR M4fKZoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MVqyOVA{PTl4MR?=
MKN28 M3\tWGNmdGxiVnnhZoltcXS7IFHzd4F6 M4n3T|AuOTByMDDuUS=> M1TpU|I1NzR6IHi= NX;Ib|lbTE2VTx?= NGfNWZll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MW[yOVA{PTl4MR?=
KATO3 NITPSmFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2nHNFAuOTByMDDuUS=> NWn1V|lWOjRxNEigbC=> NXLuUZo2TE2VTx?= MW\k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MV[yOVA{PTl4MR?=
SGC7901 NIXC[2hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mlf5NE0yODByIH7N MorqNlQwPDhiaB?= MoK3SG1UVw>? M17vRoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MlrONlUxOzV7NkG=
N87 MmjCR4VtdCCYaXHibYxqfHliQYPzZZk> Mn7CNE0yODByIH7N NWLGXnZHOjRxNEigbC=> MYPEUXNQ MYfk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NUGwd4FrOjVyM{W5OlE>
HMEC M4\FNWNmdGxiVnnhZoltcXS7IFHzd4F6 MX6wMVExODBibl2= MknONlQwPDhiaB?= NWX6RlZITE2VTx?= NGq0dYFl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M1rYNVI2ODN3OU[x
HUVEC M1Psb2NmdGxiVnnhZoltcXS7IFHzd4F6 Mn\KNE0yODByIH7N M17nSlI1NzR6IHi= MkXWSG1UVw>? MUnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MnXJNlUxOzV7NkG=
MG63 MYHGeY5kfGmxbjDBd5NigQ>? MYe1NE0yODByIH7N NE\USHMxNjViaB?= M{L5b4Rwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NGO4dmYzPDh2MEGzOC=>
U2OS  NXvNT3RSTnWwY4Tpc44hSXO|YYm= M2LDUFUxNTFyMECgcm0> M2TuTlAvPSCq NHnRdVdld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MmnUNlQ5PDBzM{S=
Saos-2  MUTGeY5kfGmxbjDBd5NigQ>? MkLtOVAuOTByMDDuUS=> MlmyNE42KGh? MUXkc5NmKGSncHXu[IVvfGy7IDi1NQKBmzFyMECgcm0qKGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= NV3kbJU6OjR6NECxN|Q>
Saos-2 NFzuWFdHfW6ldHnvckBCe3OjeR?= Mk[1NVAxKG6P M4PJdVAvPSCq NULRbGl1eHKndnXueJMhd3O2ZX;zZZJkd22jIHPlcIwhdWmpcnH0bY9v MXKyOFg1ODF|NB?=
MG63 Moj0RZBweHSxc3nzJGF{e2G7 M3rLUVExOCCwTR?= M3Ha[FM3KGh? M{nk[pBzd22xdHXzJIFxd3C2b4Ppdy=> NGH3N5IzPDh2MEGzOC=>
U2OS  MkfZRZBweHSxc3nzJGF{e2G7 NVrqNIQ5OTByIH7N M1HDRVM3KGh? M1\o[pBzd22xdHXzJIFxd3C2b4Ppdy=> M2Xzd|I1QDRyMUO0
Saos-2  NUi5co5jSXCxcITvd4l{KEG|c3H5 M3HtRVExOCCwTR?= Mle3N|YhcA>? Mo[zdJJwdW:2ZYOgZZBweHSxc3nz MYSyOFg1ODF|NB?=
HT1376 NUC1WId[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD4eotUUUN3ME2xMlg5KMLzIEGuNUDPxE1? NF;zSGYzPDB3NEi3NS=>
T24 Ml3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXPTWM2OD1zLkO3JOKyKDBwNDFOwG0> MnjrNlQxPTR6N{G=
UM-UC-3 NVjSTo9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rCSWlEPTB;MD62N{DDuTBwMTFOwG0> M1mxeFI1ODV2OEex
DLD-1 NUnEN5VoS2WubDDWbYFjcWyrdImgRZN{[Xl? NUDV[Gd2OC1zMECwJI5O NHHFTHkzPCCq NHPPcXNqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXTC[GNNOjN7OUGxO|k>
Caco2 NGLwfpBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnG0NE0yODByIH7N M{nkV|I1KGh? NIWwdmdqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYPGXWozOjN7OUGxO|k>
HT29 NEXu[IFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{H3[VAuOTByMDDuUS=> NIPhPFAzPCCq MYLpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NYDuVnRVOjN7OUGxO|k>
H116 MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NF7OW4cxNTFyMECgcm0> M4rHU|I1KGh? NE[yc4tqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MljsNlM6QTFzN{m=
Hct-8 NX64XIR2S2WubDDWbYFjcWyrdImgRZN{[Xl? MWqwMVExODBibl2= MXuyOEBp MVPpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NIHkZVkzOzl7MUG3PS=>
Colo320 MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXiwMVExODBibl2= NYLzcWFoOjRiaB?= NXnzVG9QcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYKyN|k6OTF5OR?=
Sw948 NXvMU|hwS2WubDDWbYFjcWyrdImgRZN{[Xl? M2\KcVAuOTByMDDuUS=> NXLPVVh1OjRiaB?= MYTpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NWTHOVA1OjN7OUGxO|k>
Colo205 NHO5dmVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkLwNE0yODByIH7N M{fLV|I1KGh? NI\ZVmlqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHr0N3kzOzl7MUG3PS=>
Colo320 NETpWnFHfW6ldHnvckBCe3OjeR?= M3[wTFEh|ryP MoXYNE0zPCCq NV2zOJpX[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MX:yN|k6OTF5OR?=
HT29 M3X2PWZ2dmO2aX;uJGF{e2G7 NWfxWpBYOSEQvF2= MYewMVI1KGh? M2Txd4Fjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> MXGyN|k6OTF5OR?=
Sw948 M4nafGZ2dmO2aX;uJGF{e2G7 MkPsNUDPxE1? NILB[oIxNTJ2IHi= M1jUU4Fjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> M3zMeFI{QTlzMUe5
DLD-1 NUDLRlR1TnWwY4Tpc44hSXO|YYm= NXPNSmlUOSEQvF2= M4Hkb|AuOjRiaB?= NVrJZpZF[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MWiyN|k6OTF5OR?=
SW620 M{jpVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G4[mlEPTB;Nz64JO69VQ>? MWCyN|U1OjF5OB?=
SW480 NGjpVW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTRwNjFOwG0> M1u5SlI{PTR{MUe4
SK-CO-1 M2O1PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTRizszN NXXBRW9UOjN3NEKxO|g>
LS-513 NFPOdJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTNwOTFOwG0> NFfQdIQzOzV2MkG3PC=>
SW1116 NW\4[ZFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTUdVlyUUN3ME2wMlg1KM7:TR?= NHTKblIzOzV2MkG3PC=>
LS-174T NFjkR4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH2zOYVKSzVyPUCuPFQh|ryP NHrWPYUzOzV2MkG3PC=>
HCT 116 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjne3RkUUN3ME2wMlQyKM7:TR?= MUGyN|U1OjF5OB?=
HCT 15 Ml3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS5NGJKSzVyPUCuN{DPxE1? NVm1OW5UOjN3NEKxO|g>
COLO 205 NV7kemVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzsTWM2OD1yLkK0JO69VQ>? MnzuNlM2PDJzN{i=
HT-29 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny4TWM2OD1yLkKzJO69VQ>? MWCyN|U1OjF5OB?=
COLO 201 M2H3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVS1[oJ[UUN3ME2wMlI{KM7:TR?= NIfBOnIzOzV2MkG3PC=>
Caco-2 NVXiOWp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjSTWM2OD1yLkKyJO69VQ>? NF7OSokzOzV2MkG3PC=>
SW48 M17GNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHWU21{UUN3ME2wMlA6KM7:TR?= NIXGeVkzOzV2MkG3PC=>
DND-1 M1e3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPmNE4zPS9yLkWvNUDPxE1? NX:yV21xTE2VTx?= NGS5VZBqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MoHXNlM1QDJ5NEi=
TMD8 MlW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXGSpExNjJ3L{CuOU8yKM7:TR?= M1ywO2ROW09? Mof2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MUSyN|Q5Ojd2OB?=
Jurkat Mm\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;CUlAvOjVxMD61M|Eh|ryP M{\pUmROW09? MlizbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MUSyN|Q5Ojd2OB?=
KOPT-K1 MmflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfMNE4zPS9yLkWvNUDPxE1? Mn3TSG1UVw>? MkDObY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NHjMXYgzOzR6Mke0PC=>
TMD7 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWKwMlI2NzBwNT:xJO69VQ>? MlexSG1UVw>? NULG[pdzcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MkewNlM1QDJ5NEi=
THP-1 M4TXUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zjZ|AvOjVxMD61M|Eh|ryP MnjsSG1UVw>? M1jleolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> Mn[1NlM1QDJ5NEi=
786-O NFPTVZVHfW6ldHnvckBCe3OjeR?= NVnTPZVqOC5zL{CuOUDPxE1? NITwcpYzPCCq MX\EUXNQ MlvKbY5kemWjc3XzJGUu[2GmaHXybY4hdVKQQTDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgQ>? NF3UeJMzOzF2N{K1NS=>
786-O NETqcJJHfW6ldHnvckBCe3OjeR?= MViwMVAvPSEQvF2= NH3Jb3czPCCq NX3mTXFxTE2VTx?= NYrqOXJRemW|dXz0d{BqdiCjIHTvd4Uh\GWyZX7k[Y51KGmwY4LlZZNmKGmwIFWtZ4FlcGW{aX6gdJJwfGWrbjDlfJBz\XO|aX;uxsA> MoL6NlMyPDd{NUG=
OCI-AML3 MlLKRZBweHSxc3nzJGF{e2G7 MVeyMlUh|ryP NYLSWXBZPzJiaB?= MkX0bY5lfWOnczDhdI9xfG:|aYO= MXKyNlgzPjV4NR?=
Jurkat NXvIZldFTnWwY4Tpc44hSXO|YYm= MojvNVAxNzJyMD:0NFAhdk1? NWfI[5VpOThiaB?= M37M[IlvcGmkaYTzJI1VV1KFMT3k[ZBmdmSnboSgV|YhWzJ|NT:yN|YheGixc4Doc5J6dGG2aX;u MXKyNlU3PjZyNB?=
p210 BCR-Abl MkXkSpVv[3Srb36gRZN{[Xl? NIPGVZkyODBxMkCwM|QxOCCwTR?= MUKxPEBp MY\pcohq[mm2czDtWG9TSzFvZHXw[Y5l\W62IGO2JHMzOzVxMkO2JJBpd3OyaH;yfYxifGmxbh?= MWCyNlU3PjZyNB?=
Jurkat NXvTUolYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkj5OFAxdk1? M2TVfFI1NzR6IHi= NVr4eZE6e3mwZYLnbZpmKHerdHigNVcuSUGJIITvJJN2eHC{ZYPzJINmdGxicILvcIln\XKjdHnvci=> NED2Z3gzOjV4Nk[wOC=>
p210 BCR-Abl M17rSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3ROFAxdk1? MXeyOE81QCCq M2fvTJN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= M3HzXlIzPTZ4NkC0
8226 MX3GeY5kfGmxbjDBd5NigQ>? M{Di[FExOC1zMECwJI5O NWXXfYNsOzBibXnu M1LxeGROW09? NFfVN3li[3SrdnH0[ZMhTVKNwrC= NXvEeYt[OjJ3NU[0NFk>
MM1.S  NIrzdm5HfW6ldHnvckBCe3OjeR?= NFTnWmgyODBvMUCwNEBvVQ>? NHu5T|g{OCCvaX6= NYnvfoZkTE2VTx?= NIq1eVli[3SrdnH0[ZMhTVKNwrC= NUL1RpV[OjJ3NU[0NFk>
8226 NHrhXI9HfW6ldHnvckBCe3OjeR?= MoruNE42KM7:TR?= NHLGSXg{OCCvaX6= MmK4SG1UVw>? MkG5bY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= M2D6R|IzPTV4NEC5
MM1.S  MkS1SpVv[3Srb36gRZN{[Xl? MWqwMlUh|ryP M4jCS|MxKG2rbh?= NXzQ[oRlTE2VTx?= Mn;tbY5lfWOnczDhZ5RqfmG2aX;uJI9nKFKDRjDhcoQheGixc4Doc5J6dGG2aX;uJI9nKE2HSx?= MoHINlI2PTZ2MEm=
MCF-7 M1\wN2Z2dmO2aX;uJGF{e2G7 MVG1NE8zODBxNUCwJI5O MUmzNEBucW5? Mm\G[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NULXbItUOjJ2N{[4OVI>
T47D NWLtTZdiTnWwY4Tpc44hSXO|YYm= MXG1NE8zODBxNUCwJI5O MYSzNEBucW5? MYXkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MW[yNlQ4Pjh3Mh?=
MDA-MB-231 NHPCPI5HfW6ldHnvckBCe3OjeR?= MmHwOVAwOjByL{WwNEBvVQ>? Mn20N|AhdWmw Mlqx[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> Ml2wNlI1PzZ6NUK=
Bcap-37 NH;GZ|dHfW6ldHnvckBCe3OjeR?= M1fZUFUxNzJyMD:1NFAhdk1? NYH5c|ZCOzBibXnu Mnu0[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NYPXNnNQOjJ2N{[4OVI>
MCF-7 M{i0cmFxd3C2b4Ppd{BCe3OjeR?= MVyyNFDDqG6P NWXoS4xlOzZiaB?= MVjEUXNQ MWXpcoR2[2W|IHHwc5B1d3Orcx?= NX7ieWliOjJ2N{[4OVI>
MDA-MB-231 M37wN2Fxd3C2b4Ppd{BCe3OjeR?= MUCyNFDDqG6P NUW2[WtyOzZiaB?= NGP4RYNFVVOR NVHScHhPcW6mdXPld{BieG:ydH;zbZM> M4TRT|IzPDd4OEWy
Bcap-37 M4XSd2Fxd3C2b4Ppd{BCe3OjeR?= MXyyNFDDqG6P NHvuWGw{PiCq M1;YVGROW09? MULpcoR2[2W|IHHwc5B1d3Orcx?= MojWNlI1PzZ6NUK=
LS174T M16xWGZ2dmO2aX;uJGF{e2G7 M2rkblExNzFyMD:xNFAxKG6P M2f3VFYhcA>? Mki0SG1UVw>? NIG3eJJqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv M{\ldFIzPDBzMkm0
DLD-1  NGHhNG1HfW6ldHnvckBCe3OjeR?= MkLuNVAwOTByL{GwNFAhdk1? M{XsXFYhcA>? Mnr0SG1UVw>? NH;ofGRqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv M2HtNlIzPDBzMkm0
SW480 M1\4eGZ2dmO2aX;uJGF{e2G7 M3nETlExNzFyMD:xNFAxKG6P M1XpUlYhcA>? NGj0NWtFVVOR Mm\GbY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> MV2yNlQxOTJ7NB?=
SW-48 MkT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjITWM2OD1yLkGg{txO MoLrNlIzPzB{NUe=
HCT-15 NHi1RlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnuVG1KSzVyPUCuN{DPxE1? MWCyNlI4ODJ3Nx?=
HCT 116 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwNjFOwG0> NX6wdWg3OjJ{N{CyOVc>
SW620-R MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwMzFOwG0> NFrMeW8zOjJ5MEK1Oy=>
SK-CO-1 Mny0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1L2RWlEPTB;Mj6xJO69VQ>? MWCyNlI4ODJ3Nx?=
SW620 MljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTFzIN88US=> NYfRdYNnOjJ{N{CyOVc>
BaF3 NXXFU2s6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3HTVUxRTFwNES5JO69VQ>? M{HYTFIzOjJ|NkS1
NIH 3T3 MXnGeY5kfGmxbjDBd5NigQ>? Ml\zNkDPxE1? M{Szb|E5KGh? MU\pcohq[mm2czDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBwdiCVZYK0O|Mh[W6mIH3UU3JEOSCyaH;zdIhwenmuYYTpc44hd2ZiNFWtRnAyKG:wIGTodlM4NzR4 M1S3TFIyQDd4MUOw
HCT15 NInxUFFHfW6ldHnvckBCe3OjeR?= MUiwMlUwOiEQvF2= NX;RNYtxPCCq NX3EbFNTeHKndnXueJMhWz[NMTDwbI9{eGixconsZZRqd25ib3[gdoljd3OxbXHsJJBzd3SnaX6gV|Yh[XRiU3XyNlQxNzJ2NDDhcoQhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3RiYYSgV4VzPDd| MXWyNVg4PjF|MB?=
SW620  NUnsN3ZnTnWwY4Tpc44hSXO|YYm= NEm1OFAxNjVxMjFOwG0> M3K1eVQhcA>? M{nq[oJtd2OtczDhcIwhfGi{ZXWgcXRQWiCxdYTweZR{ NXXsV2xsOjF6N{[xN|A>

... 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.

Related Antibodies

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

Related mTOR Products

Tags: buy Torkinib (PP242) | Torkinib (PP242) supplier | purchase Torkinib (PP242) | Torkinib (PP242) cost | Torkinib (PP242) manufacturer | order Torkinib (PP242) | Torkinib (PP242) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID