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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7 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.

  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
Hck [1]
(Cell-free assay)
8 nM 0.10 μM 0.41 μM 0.41 μM 1.2 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 MW\GeY5kfGmxbjDBd5NigQ>? NHu3PYs2OC1zMkWwJI5O Mn3QNlQhcA>? MnTGSG1UVw>? Mne3bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHM3KGurbnHz[UApfGG{Z3X0JI9nKG2WT2LDNUkh[W6mIHn0d{Bld3ewc4Ty[YFuKHSjcnfleEBxcG:|cHjvMXM3yqB? NVnQRlVWOjZzN{ewOVE>
U87vIII  MmfBSpVv[3Srb36gRZN{[Xl? NGXlOY8xNjB2LUKuOUDPxE1? NUHnSJlbOjRiaB?= MXHpcohq[mm2czDtWG9TSzFiYX7kJI1VV1KFMjDhZ5Rqfmm2aXXzxsA> NUPHdoFYOjZzM{S2NVc>
U87vIII  NEjHdZVHfW6ldHnvckBCe3OjeR?= MV2yMlUwPSEQvF2= NEfxb5AyOiCq NGnxSXVqdmirYnn0d{Bo[XBiY3zvd4lv\yCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUmyOlE{PDZzNx?=
PC12  NHfCUHJHfW6ldHnvckBCe3OjeR?= NITIbIg1OMLibl2= MmHLbY5lfWOnczDsfZNwe2:vYXygZolw\2WwZYPpd{BidmRiYXzs[ZZq[XSnZDFOtU1UYU5iYXPjeY12dGG2aX;uxsA> NFj0dnEzPjByMU[xOC=>
3T3-L1 MnnLSpVv[3Srb36gRZN{[Xl? NH25NXMyPSEQvF2= NUfYc4htPCCq MmXGd5VxeHKnc4Pld{BmgHC{ZYPzbY9vKG:oIITo[UBG\3JzIIDyc5RmcW8EoB?= MX:yOVgyPDZ4Mh?=
Rh30 M1PHN2Z2dmO2aX;uJGF{e2G7 MoLlNUDPxE1? NWf5OZN6OiCq MoLWbY5pcWKrdIOgZo91cCCvVF;SR|EudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKFN4S{GgZY5lKG2WT2LDNk1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhSWu2 NGnKc|UzPTd4Mk[xPS=>
HT29 MUDGeY5kfGmxbjDBd5NigQ>? NEO1WIcyKM7:TR?= MXOyJIg> NVK3R3VscW6qaXLpeJMh[m:2aDDtWG9TSzFvbXXkbYF1\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGO2T|Eh[W6mIH3UU3JEOi2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M3O1dFI2PzZ{NkG5
Rh30 NXzMcYx[TnWwY4Tpc44hSXO|YYm= MWixJO69VQ>? NIHCdWozKGh? NFfaUmp{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> MXuyOVc3OjZzOR?=
HT29 M{nQU2Z2dmO2aX;uJGF{e2G7 MVqxJO69VQ>? Moi4NkBp MV\zeZBxemW|c3XzJJRp\SCkYYPhcEBweiCLR1[tNU1{fGmvdXzheIVlKGOnbHygZYRp\XOrb36= NF\qUXEzPTd4Mk[xPS=>
U87 NGroOZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj6NlUhdk1? NImySFUzPCCq NH3uZoFqdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> MVGyOVU3QDZ4NR?=
AGS MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXqwMVExODBibl2= NH21OJAzPC92ODDo M3;YXmROW09? NWfFXY1I\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MnPBNlUxOzV7NkG=
MKN45 MXjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYWwMVExODBibl2= MVyyOE81QCCq NIrzdYZFVVOR MUDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NFq4XmEzPTB|NUm2NS=>
MKN28 NELOcINE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlLDNE0yODByIH7N M{DyTlI1NzR6IHi= MkH1SG1UVw>? NG[5TnBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NFvxcYszPTB|NUm2NS=>
KATO3 NU\sdYdRS2WubDDWbYFjcWyrdImgRZN{[Xl? M2P3dFAuOTByMDDuUS=> MmG2NlQwPDhiaB?= NHHzOZNFVVOR NHWzXY1l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M2C3NlI2ODN3OU[x
SGC7901 M1i4cWNmdGxiVnnhZoltcXS7IFHzd4F6 NHPHdIQxNTFyMECgcm0> MmP2NlQwPDhiaB?= Mm\SSG1UVw>? NXO0RVVu\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MUWyOVA{PTl4MR?=
N87 NEPKN|dE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{XrclAuOTByMDDuUS=> MoT4NlQwPDhiaB?= MYLEUXNQ NHqwRmhl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NHW5bIwzPTB|NUm2NS=>
HMEC M2Xre2NmdGxiVnnhZoltcXS7IFHzd4F6 M2jUe|AuOTByMDDuUS=> M3zzfVI1NzR6IHi= NIPa[4RFVVOR MXzk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NYm1eoYxOjVyM{W5OlE>
HUVEC NIf1V5RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUX1WmdpOC1zMECwJI5O M3XvW|I1NzR6IHi= MXjEUXNQ M122boRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MoPYNlUxOzV7NkG=
MG63 NVPH[WpuTnWwY4Tpc44hSXO|YYm= MmP4OVAuOTByMDDuUS=> M{DJRVAvPSCq MnPl[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NViweW1XOjR6NECxN|Q>
U2OS  MWLGeY5kfGmxbjDBd5NigQ>? M{PwVFUxNTFyMECgcm0> NUPkUWNYOC53IHi= M2fJ[YRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NFLVWpczPDh2MEGzOC=>
Saos-2  M2PpfWZ2dmO2aX;uJGF{e2G7 NWm4cItbPTBvMUCwNEBvVQ>? M1:3XFAvPSCq M3TReYRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M4rnWFI1QDRyMUO0
Saos-2 NGfO[o5HfW6ldHnvckBCe3OjeR?= MX6xNFAhdk1? NULJVW1EOC53IHi= M4XuXJBz\X[nboTzJI9{fGWxc3HyZ49u[SClZXzsJI1q\3KjdHnvci=> Ml;SNlQ5PDBzM{S=
MG63 MV\BdI9xfG:|aYOgRZN{[Xl? MoX1NVAxKG6P MmPON|YhcA>? MUTwdo9ud3SnczDhdI9xfG:|aYO= MnrJNlQ5PDBzM{S=
U2OS  M2PsVmFxd3C2b4Ppd{BCe3OjeR?= NVPPRmFGOTByIH7N NGHmUJQ{PiCq M33KS5Bzd22xdHXzJIFxd3C2b4Ppdy=> M{PkO|I1QDRyMUO0
Saos-2  MWrBdI9xfG:|aYOgRZN{[Xl? M3nITlExOCCwTR?= NXHhb4dQOzZiaB?= MWTwdo9ud3SnczDhdI9xfG:|aYO= NWKxO2dMOjR6NECxN|Q>
HT1376 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PU[mlEPTB;MT64PEDDuSBzLkGg{txO NH;3[nAzPDB3NEi3NS=>
T24 MoOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvoTWM2OD1zLkO3JOKyKDBwNDFOwG0> M3HYN|I1ODV2OEex
UM-UC-3 NInEOZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwNkOgxtExNjFizszN M2CySVI1ODV2OEex
DLD-1 M2\a[2NmdGxiVnnhZoltcXS7IFHzd4F6 NUfDcIVEOC1zMECwJI5O NHy4OoYzPCCq NYHte4ZEcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mor0NlM6QTFzN{m=
Caco2 MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M17lb|AuOTByMDDuUS=> M2r4SFI1KGh? NF7tWGJqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{nsOFI{QTlzMUe5
HT29 MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHqwXYwxNTFyMECgcm0> NVPENHhsOjRiaB?= MkjFbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEXEcZUzOzl7MUG3PS=>
H116 NEfpeXlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlL6NE0yODByIH7N M{WwS|I1KGh? M4HtdIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmiyNlM6QTFzN{m=
Hct-8 NGDVXmRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlvVNE0yODByIH7N M4XGdlI1KGh? Mm\kbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmO0NlM6QTFzN{m=
Colo320 M3GxUWNmdGxiVnnhZoltcXS7IFHzd4F6 NYPGNnFFOC1zMECwJI5O NWLSTppUOjRiaB?= NG\XXnZqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mne5NlM6QTFzN{m=
Sw948 MmfYR4VtdCCYaXHibYxqfHliQYPzZZk> Mm\6NE0yODByIH7N NWe3WVdWOjRiaB?= NWDoS5UzcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3KwXVI{QTlzMUe5
Colo205 NIGyXG5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYX2[WFxOC1zMECwJI5O M3XleVI1KGh? NVnQbWVncW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MkO1NlM6QTFzN{m=
Colo320 NELQTIZHfW6ldHnvckBCe3OjeR?= MkPwNUDPxE1? M4XoXlAuOjRiaB?= MnXmZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> MV:yN|k6OTF5OR?=
HT29 MW\GeY5kfGmxbjDBd5NigQ>? MWixJO69VQ>? NH\mO4sxNTJ2IHi= NIPoOmdi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 M3z4WFI{QTlzMUe5
Sw948 NHmzRWpHfW6ldHnvckBCe3OjeR?= M3e0dVEh|ryP MoTHNE0zPCCq M{HmS4Fjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> NIjCd4ozOzl7MUG3PS=>
DLD-1 MmO5SpVv[3Srb36gRZN{[Xl? NGTlVHIyKM7:TR?= NHLCRmsxNTJ2IHi= MV;hZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 M3XvR|I{QTlzMUe5
SW620 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fSUGlEPTB;Nz64JO69VQ>? NWfkfmxLOjN3NEKxO|g>
SW480 NXfN[ZZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3TTWM2OD12Lk[g{txO NEjTdXEzOzV2MkG3PC=>
SK-CO-1 MmTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\FOFNKSzVyPUSg{txO MoW1NlM2PDJzN{i=
LS-513 NXrUWlc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T5NGlEPTB;Mz65JO69VQ>? MXWyN|U1OjF5OB?=
SW1116 NWPLNpV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfKZ5NKSzVyPUCuPFQh|ryP NFrq[ZozOzV2MkG3PC=>
LS-174T MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwOESg{txO NFuwRpQzOzV2MkG3PC=>
HCT 116 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fnT2lEPTB;MD60NUDPxE1? MlPkNlM2PDJzN{i=
HCT 15 NVrKVmpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jlNmlEPTB;MD6zJO69VQ>? NFHlbVIzOzV2MkG3PC=>
COLO 205 NEG4fmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLOTWM2OD1yLkK0JO69VQ>? MXqyN|U1OjF5OB?=
HT-29 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M16wUWlEPTB;MD6yN{DPxE1? MVyyN|U1OjF5OB?=
COLO 201 NHLOTVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwMkOg{txO NHntWJEzOzV2MkG3PC=>
Caco-2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrqbnpnUUN3ME2wMlIzKM7:TR?= M3jESFI{PTR{MUe4
SW48 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D3W2lEPTB;MD6wPUDPxE1? NVrHZlkxOjN3NEKxO|g>
DND-1 NYXhNo1vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXywMlI2NzBwNT:xJO69VQ>? Mn3wSG1UVw>? MmTrbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NUfqb|RbOjN2OEK3OFg>
TMD8 NGf6ZmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHW3WZYxNjJ3L{CuOU8yKM7:TR?= MoTESG1UVw>? M3XGW4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M3PtZlI{PDh{N{S4
Jurkat MlL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX3NE4zPS9yLkWvNUDPxE1? Ml;XSG1UVw>? MUfpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MXqyN|Q5Ojd2OB?=
KOPT-K1 NUe0NohpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXGwMlI2NzBwNT:xJO69VQ>? MUHEUXNQ NWDEV286cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MkXsNlM1QDJ5NEi=
TMD7 NUnKfpNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWwMlI2NzBwNT:xJO69VQ>? MXHEUXNQ MnvUbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M{PkUVI{PDh{N{S4
THP-1 NXnVWWEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjhNE4zPS9yLkWvNUDPxE1? Ml3MSG1UVw>? MUnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MWGyN|Q5Ojd2OB?=
786-O NG\BTGlHfW6ldHnvckBCe3OjeR?= NH7UVmkxNjFxMD61JO69VQ>? NWLibYVuOjRiaB?= MVrEUXNQ M2DHSolv[3KnYYPld{BGNWOjZHjldolvKG2UTlGgcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHl? Mn3RNlMyPDd{NUG=
786-O MnHqSpVv[3Srb36gRZN{[Xl? MmXxNE0xNjVizszN MlnrNlQhcA>? M{W3S2ROW09? NH;wOIFz\XO3bITzJIlvKGFiZH;z[UBl\XCnbnTlcpQhcW6lcnXhd4UhcW5iRT3jZYRp\XKrbjDwdo91\WmwIHX4dJJme3Orb39CpC=> M2LSelI{OTR5MkWx
OCI-AML3 NE\Y[o1CeG:ydH;zbZMhSXO|YYm= MkDHNk42KM7:TR?= MX23NkBp MUDpcoR2[2W|IHHwc5B1d3Orcx?= MoSyNlI5OjZ3NkW=
Jurkat MlrsSpVv[3Srb36gRZN{[Xl? NGnPSZgyODBxMkCwM|QxOCCwTR?= NFPMR40yQCCq M1nKW4lvcGmkaYTzJI1VV1KFMT3k[ZBmdmSnboSgV|YhWzJ|NT:yN|YheGixc4Doc5J6dGG2aX;u NEXxZ|AzOjV4Nk[wOC=>
p210 BCR-Abl MULGeY5kfGmxbjDBd5NigQ>? M2PLXVExOC9{MECvOFAxKG6P MWWxPEBp NFXTOZdqdmirYnn0d{BuXE:UQ{Gt[IVx\W6mZX70JHM3KFN{M{WvNlM3KHCqb4PwbI9zgWyjdHnvci=> NGPYOpMzOjV4Nk[wOC=>
Jurkat NEexeGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\BVoNCPDBybl2= Mk[5NlQwPDhiaB?= NEnCVGV{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u NYK2fHRkOjJ3Nk[2NFQ>
p210 BCR-Abl NFP3R|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnlUpk1ODCwTR?= MonjNlQwPDhiaB?= M3zUXpN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= M1\CSFIzPTZ4NkC0
8226 M4nPSWZ2dmO2aX;uJGF{e2G7 NGLBRWoyODBvMUCwNEBvVQ>? MoLGN|AhdWmw M4LEZWROW09? MVPhZ5RqfmG2ZYOgSXJMyqB? NXXEUm1TOjJ3NU[0NFk>
MM1.S  NYLZUIJxTnWwY4Tpc44hSXO|YYm= MVmxNFAuOTByMDDuUS=> Mn7DN|AhdWmw M{\iWGROW09? M2LndoFkfGm4YYTld{BGWkwEoB?= NGfhOWMzOjV3NkSwPS=>
8226 NGT2dFhHfW6ldHnvckBCe3OjeR?= MkTrNE42KM7:TR?= NV\6W2dKOzBibXnu NWnkdG9ETE2VTx?= NUHJ[WVVcW6mdXPld{Bi[3SrdnH0bY9vKG:oIGLBSkBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIF3FTy=> M2LZTVIzPTV4NEC5
MM1.S  MYPGeY5kfGmxbjDBd5NigQ>? MXuwMlUh|ryP MV[zNEBucW5? M3rLWmROW09? NUe5[phIcW6mdXPld{Bi[3SrdnH0bY9vKG:oIGLBSkBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIF3FTy=> M3v2fVIzPTV4NEC5
MCF-7 MlfRSpVv[3Srb36gRZN{[Xl? MnLHOVAwOjByL{WwNEBvVQ>? M2j0XlMxKG2rbh?= NW\ObmlL\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MUCyNlQ4Pjh3Mh?=
T47D Ml7NSpVv[3Srb36gRZN{[Xl? NFvWTXI2OC9{MECvOVAxKG6P MXuzNEBucW5? NITTSoRld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? MWSyNlQ4Pjh3Mh?=
MDA-MB-231 MmHUSpVv[3Srb36gRZN{[Xl? NHnnSpc2OC9{MECvOVAxKG6P MUezNEBucW5? MYPkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MVWyNlQ4Pjh3Mh?=
Bcap-37 M1e0fmZ2dmO2aX;uJGF{e2G7 NVr6[FN[PTBxMkCwM|UxOCCwTR?= MoT0N|AhdWmw MVLkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NGWzdGUzOjR5Nki1Ni=>
MCF-7 NUfnNmx{SXCxcITvd4l{KEG|c3H5 NFjJdWszODEEoH7N MXizOkBp MVfEUXNQ NHn1e|JqdmS3Y3XzJIFxd3C2b4Ppdy=> NIrYdYQzOjR5Nki1Ni=>
MDA-MB-231 MojoRZBweHSxc3nzJGF{e2G7 M1z0WVIxOMLibl2= NWDmdGhzOzZiaB?= NHOzO3BFVVOR M2LtbYlv\HWlZYOgZZBweHSxc3nz MkPoNlI1PzZ6NUK=
Bcap-37 MVrBdI9xfG:|aYOgRZN{[Xl? NF;GRXgzODEEoH7N NIr6XJI{PiCq NIDnOWpFVVOR MnPJbY5lfWOnczDhdI9xfG:|aYO= MnjLNlI1PzZ6NUK=
LS174T MXjGeY5kfGmxbjDBd5NigQ>? M{fUR|ExNzFyMD:xNFAxKG6P M3vNZVYhcA>? MkThSG1UVw>? M3HhXolvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> NX75cYxnOjJ2MEGyPVQ>
DLD-1  NHLZWYtHfW6ldHnvckBCe3OjeR?= NHLuSWwyOC9zMECvNVAxOCCwTR?= MnPFOkBp Ml\vSG1UVw>? M4rlU4lvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> MnfUNlI1ODF{OUS=
SW480 NESyT3hHfW6ldHnvckBCe3OjeR?= MVWxNE8yODBxMUCwNEBvVQ>? NFvXTI43KGh? M3X6XmROW09? NUjZNVdxcW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? MV2yNlQxOTJ7NB?=
SW-48 NV7Hc3R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\qO2tKSzVyPUCuNUDPxE1? M3jK[FIzOjdyMkW3
HCT-15 M2PEPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DlNWlEPTB;MD6zJO69VQ>? M2Pw[|IzOjdyMkW3
HCT 116 NX7qVnU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HLOGlEPTB;MD62JO69VQ>? NFLiTVUzOjJ5MEK1Oy=>
SW620-R Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTFwMzFOwG0> M3z3OlIzOjdyMkW3
SK-CO-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTJwMTFOwG0> M4LLbFIzOjdyMkW3
SW620 NGLBSnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLOTWM2OD1zMTFOwG0> MoTsNlIzPzB{NUe=
BaF3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\RS2k2OD1zLkS0PUDPxE1? NIPo[lczOjJ{M{[0OS=>
NIH 3T3 MVrGeY5kfGmxbjDBd5NigQ>? M4rUPVIh|ryP M3jEZ|E5KGh? MWXpcohq[mm2czDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBwdiCVZYK0O|Mh[W6mIH3UU3JEOSCyaH;zdIhwenmuYYTpc44hd2ZiNFWtRnAyKG:wIGTodlM4NzR4 MlHSNlE5PzZzM{C=
HCT15 Ml3xSpVv[3Srb36gRZN{[Xl? MVKwMlUwOiEQvF2= NI\iXmU1KGh? MYTwdoV3\W62czDTOmsyKHCqb4PwbI9zgWyjdHnvckBw\iC{aXLvd49u[WxicILveIVqdiCVNjDheEBU\XJ{NECvNlQ1KGGwZDDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBifCCVZYK0O|M> NETacmczOTh5NkGzNC=>
SW620  NVj1XHN2TnWwY4Tpc44hSXO|YYm= M{mzTVAvPS9{IN88US=> MXu0JIg> MlLUZoxw[2u|IHHscEB1cHKnZTDtWG9TKG:3dID1eJM> NFjjdoQzOTh5NkGzNC=>

... 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 62 mg/mL (201.07 mM)
Ethanol 18 mg/mL (58.37 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 (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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID