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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In DMSO USD 91 In stock
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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 MYnGeY5kfGmxbjDBd5NigQ>? MXK1NE0yOjVyIH7N M1L4V|I1KGh? NE[yXpZFVVOR NWjY[Fl5cW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFN4IHvpcoF{\SBqdHHy[4V1KG:oIH3UU3JEOSliYX7kJIl1eyCmb4fud5Rz\WGvIIThdodmfCCyaH;zdIhwNVN4wrC= NULRVmtIOjZzN{ewOVE>
U87vIII  NFjUVYZHfW6ldHnvckBCe3OjeR?= NF;0bXkxNjB2LUKuOUDPxE1? NXjDd4xMOjRiaB?= NGfQc49qdmirYnn0d{BuXE:UQ{GgZY5lKG2WT2LDNkBi[3Srdnn0bYV{yqB? MknDNlYyOzR4MUe=
U87vIII  M1j6XWZ2dmO2aX;uJGF{e2G7 MnT3Nk42NzVizszN M2nWR|EzKGh? NVH0VWVTcW6qaXLpeJMh\2GyIHPsc5NqdmdiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYWyOlE{PDZzNx?=
PC12  M1vjSmZ2dmO2aX;uJGF{e2G7 MW[0NOKhdk1? NFX3VWZqdmS3Y3XzJIx6e2:|b33hcEBjcW:pZX7ld4l{KGGwZDDhcIxmfmmjdHXkJO6yNVO\TjDhZ4N2dXWuYYTpc47DqA>? MkC5NlYxODF4MUS=
3T3-L1 MWXGeY5kfGmxbjDBd5NigQ>? M37Nb|E2KM7:TR?= M1OwflQhcA>? MmfKd5VxeHKnc4Pld{BmgHC{ZYPzbY9vKG:oIITo[UBG\3JzIIDyc5RmcW8EoB?= M1nGO|I2QDF2Nk[y
Rh30 MmnhSpVv[3Srb36gRZN{[Xl? MojuNUDPxE1? MnLYNkBp NH3zU49qdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= NX[5XoFOOjV5NkK2NVk>
HT29 MY\GeY5kfGmxbjDBd5NigQ>? NEDJWGEyKM7:TR?= MoLUNkBp MU\pcohq[mm2czDic5RpKG2WT2LDNU1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhWz[NMTDhcoQhdVSRUlOyMY1m\GmjdHXkJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MlzFNlU4PjJ4MUm=
Rh30 M{L5fGZ2dmO2aX;uJGF{e2G7 M4q3RVEh|ryP M{jVd|IhcA>? Mnz1d5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u MmjMNlU4PjJ4MUm=
HT29 M2LvRWZ2dmO2aX;uJGF{e2G7 M4T5T|Eh|ryP M2f6WVIhcA>? M17KPJN2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> M2XFU|I2PzZ{NkG5
U87 NVXNZmpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XWTlI2KG6P MYmyOEBp MkGwbY5kemWjc3XzJGRWW1BzMDDrco9kc2WmLXTve44hcW6mdXPl[EBk\WyuIHnubIljcXSrb36= MUiyOVU3QDZ4NR?=
AGS NUni[JdES2WubDDWbYFjcWyrdImgRZN{[Xl? Mme1NE0yODByIH7N M{n1bFI1NzR6IHi= Mo\RSG1UVw>? MXjk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz Moi5NlUxOzV7NkG=
MKN45 MkDrR4VtdCCYaXHibYxqfHliQYPzZZk> MYWwMVExODBibl2= M1\kVlI1NzR6IHi= NWTzRXRxTE2VTx?= NIS4dGFl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M4TyVFI2ODN3OU[x
MKN28 M{nzfmNmdGxiVnnhZoltcXS7IFHzd4F6 MlXqNE0yODByIH7N NFHQUmszPC92ODDo NGTEXG1FVVOR MnP0[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M3HxXVI2ODN3OU[x
KATO3 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkXBNE0yODByIH7N MmPPNlQwPDhiaB?= NWjtVplNTE2VTx?= NUXHc3dG\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NITEUoUzPTB|NUm2NS=>
SGC7901 NHTTSoFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXOwMVExODBibl2= MXiyOE81QCCq NH24W2ZFVVOR NXLjbW9K\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MYGyOVA{PTl4MR?=
N87 MmXaR4VtdCCYaXHibYxqfHliQYPzZZk> MV[wMVExODBibl2= MXSyOE81QCCq NXm3THJLTE2VTx?= NFTRWJZl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NUjQfGlNOjVyM{W5OlE>
HMEC MkXsR4VtdCCYaXHibYxqfHliQYPzZZk> NFqxRokxNTFyMECgcm0> MUCyOE81QCCq MoTNSG1UVw>? Mlnk[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NX7ielQ1OjVyM{W5OlE>
HUVEC NWKxbHZ6S2WubDDWbYFjcWyrdImgRZN{[Xl? Mm\WNE0yODByIH7N MUKyOE81QCCq NHPEWGJFVVOR NYrheVFk\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MmWzNlUxOzV7NkG=
MG63 M1KzOmZ2dmO2aX;uJGF{e2G7 M2fWUVUxNTFyMECgcm0> MkXoNE42KGh? NEXKT5Zld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NXrKUWtNOjR6NECxN|Q>
U2OS  NGDaTm5HfW6ldHnvckBCe3OjeR?= MXS1NE0yODByIH7N NIW3dI0xNjViaB?= NUHCOYFt\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 NWe1e4Z2OjR6NECxN|Q>
Saos-2  NYPtWYd2TnWwY4Tpc44hSXO|YYm= NEe4UI42OC1zMECwJI5O NX;JTlJQOC53IHi= NIPTfmVld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MXeyOFg1ODF|NB?=
Saos-2 MlzVSpVv[3Srb36gRZN{[Xl? MYKxNFAhdk1? MkjYNE42KGh? MnzhdJJmfmWwdIOgc5N1\W:|YYLjc41iKGOnbHygcYloemG2aX;u NUXpOFZUOjR6NECxN|Q>
MG63 MYjBdI9xfG:|aYOgRZN{[Xl? NWSzbWJuOTByIH7N NWDsbFlVOzZiaB?= MmjrdJJwdW:2ZYOgZZBweHSxc3nz MlzqNlQ5PDBzM{S=
U2OS  Mlj2RZBweHSxc3nzJGF{e2G7 MlG0NVAxKG6P M3rXZVM3KGh? MkHydJJwdW:2ZYOgZZBweHSxc3nz MlzENlQ5PDBzM{S=
Saos-2  Mmf2RZBweHSxc3nzJGF{e2G7 Ml\yNVAxKG6P MWizOkBp M3nBUZBzd22xdHXzJIFxd3C2b4Ppdy=> MlywNlQ5PDBzM{S=
HT1376 Mnu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzZTWM2OD1zLki4JOKyKDFwMTFOwG0> MV:yOFA2PDh5MR?=
T24 M1rUPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfzTWM2OD1zLkO3JOKyKDBwNDFOwG0> M4rZNlI1ODV2OEex
UM-UC-3 NEDRS21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLSWJZ4UUN3ME2wMlY{KMLzMD6xJO69VQ>? NFTwOpkzPDB3NEi3NS=>
DLD-1 MnnXR4VtdCCYaXHibYxqfHliQYPzZZk> MWewMVExODBibl2= NWT3NJFwOjRiaB?= MX\pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2nRflI{QTlzMUe5
Caco2 MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NInBdZYxNTFyMECgcm0> M17helI1KGh? MofkbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MU[yN|k6OTF5OR?=
HT29 NHq0SVJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEO5bocxNTFyMECgcm0> MmfVNlQhcA>? M3fsRolvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2jUd|I{QTlzMUe5
H116 MmK5R4VtdCCYaXHibYxqfHliQYPzZZk> M3TWXFAuOTByMDDuUS=> NVnZXZVHOjRiaB?= NHjGWlBqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3PoeVI{QTlzMUe5
Hct-8 MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVGwMVExODBibl2= NFPRbIYzPCCq MWHpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NITZZXMzOzl7MUG3PS=>
Colo320 NWXjVXdJS2WubDDWbYFjcWyrdImgRZN{[Xl? MXewMVExODBibl2= M2CwcVI1KGh? NYrZbW85cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MoSwNlM6QTFzN{m=
Sw948 NGO0NHBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{KxZ|AuOTByMDDuUS=> NU\wS4pLOjRiaB?= MXvpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX2yN|k6OTF5OR?=
Colo205 MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkTTNE0yODByIH7N NXHOOVBDOjRiaB?= NV7QcGN3cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NULjVYpvOjN7OUGxO|k>
Colo320 Moi5SpVv[3Srb36gRZN{[Xl? MoLnNUDPxE1? MmPQNE0zPCCq NF;pUYFi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 MnnxNlM6QTFzN{m=
HT29 M33zeWZ2dmO2aX;uJGF{e2G7 MUKxJO69VQ>? NXfnNnJJOC1{NDDo NWjQR25T[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MXmyN|k6OTF5OR?=
Sw948 MUHGeY5kfGmxbjDBd5NigQ>? M4DwbVEh|ryP MYKwMVI1KGh? NIqy[Wpi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 MojYNlM6QTFzN{m=
DLD-1 Mo\QSpVv[3Srb36gRZN{[Xl? MY[xJO69VQ>? MUiwMVI1KGh? MoD3ZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> M13oZ|I{QTlzMUe5
SW620 M3LEdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnH2TWM2OD15Lkig{txO NWDYZmp1OjN3NEKxO|g>
SW480 NECxenVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zocGlEPTB;ND62JO69VQ>? MV[yN|U1OjF5OB?=
SK-CO-1 NWrw[Y5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTRizszN M{m2N|I{PTR{MUe4
LS-513 NUjNbFA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfoTWM2OD1|Lkmg{txO NH\Zb28zOzV2MkG3PC=>
SW1116 M{\VRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkT3TWM2OD1yLki0JO69VQ>? M2D6TlI{PTR{MUe4
LS-174T M1;qUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{eyTWlEPTB;MD64OEDPxE1? M{TObVI{PTR{MUe4
HCT 116 NH24RoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3hV41KSzVyPUCuOFEh|ryP NWHyPWttOjN3NEKxO|g>
HCT 15 M4jiZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHq1fIZKSzVyPUCuN{DPxE1? MkWzNlM2PDJzN{i=
COLO 205 NYLocJNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkj6TWM2OD1yLkK0JO69VQ>? NWfKVINqOjN3NEKxO|g>
HT-29 NUfBNGlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPxTWM2OD1yLkKzJO69VQ>? NUmxbG5TOjN3NEKxO|g>
COLO 201 M4rnVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rIWWlEPTB;MD6yN{DPxE1? Mkj2NlM2PDJzN{i=
Caco-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHXTWM2OD1yLkKyJO69VQ>? MVmyN|U1OjF5OB?=
SW48 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PvV2lEPTB;MD6wPUDPxE1? NGTMbJczOzV2MkG3PC=>
DND-1 Mkf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MViwMlI2NzBwNT:xJO69VQ>? MkXrSG1UVw>? MnnZbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MYCyN|Q5Ojd2OB?=
TMD8 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTzWVNDOC5{NT:wMlUwOSEQvF2= NYraT2dYTE2VTx?= MYjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M{X3eFI{PDh{N{S4
Jurkat NUXPdZlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO5ZooxNjJ3L{CuOU8yKM7:TR?= NIXiZm1FVVOR MoDqbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MkTHNlM1QDJ5NEi=
KOPT-K1 NYXTOZN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC5XoxHOC5{NT:wMlUwOSEQvF2= Mn6wSG1UVw>? NWjrXnBPcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mm\xNlM1QDJ5NEi=
TMD7 NHTZWIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGS4VHQxNjJ3L{CuOU8yKM7:TR?= NGHjOJhFVVOR NWrsVVIzcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NV6zdGhXOjN2OEK3OFg>
THP-1 MmfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\oNIUxNjJ3L{CuOU8yKM7:TR?= MVfEUXNQ MlLsbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NFfrOWEzOzR6Mke0PC=>
786-O NXLVWIRVTnWwY4Tpc44hSXO|YYm= Mk\RNE4yNzBwNTFOwG0> M2S2PVI1KGh? MUfEUXNQ MY\pcoNz\WG|ZYOgSU1k[WSqZYLpckBuWk6DIHzleoVteyCmb4PlJIRmeGWwZHXueIx6 Mkf3NlMyPDd{NUG=
786-O MWjGeY5kfGmxbjDBd5NigQ>? MmnWNE0xNjVizszN M{nL[VI1KGh? M{TWc2ROW09? M1HrdZJme3WudIOgbY4h[SCmb4PlJIRmeGWwZHXueEBqdmO{ZXHz[UBqdiCHLXPh[IhmemmwIIDyc5RmcW5iZYjwdoV{e2mxbtMg M2fBc|I{OTR5MkWx
OCI-AML3 MVrBdI9xfG:|aYOgRZN{[Xl? MlPxNk42KM7:TR?= NID2OmQ4OiCq MoTsbY5lfWOnczDhdI9xfG:|aYO= MWCyNlgzPjV4NR?=
Jurkat MU\GeY5kfGmxbjDBd5NigQ>? MoixNVAxNzJyMD:0NFAhdk1? M3fJcVE5KGh? NFzNNYVqdmirYnn0d{BuXE:UQ{Gt[IVx\W6mZX70JHM3KFN{M{WvNlM3KHCqb4PwbI9zgWyjdHnvci=> MnfNNlI2PjZ4MES=
p210 BCR-Abl M323NmZ2dmO2aX;uJGF{e2G7 Mkj6NVAxNzJyMD:0NFAhdk1? M{j6fVE5KGh? NV:2N5d{cW6qaXLpeJMhdVSRUlOxMYRmeGWwZHXueEBUPiCVMkO1M|I{PiCyaH;zdIhwenmuYYTpc44> M4LhbVIzPTZ4NkC0
Jurkat NUTqW49vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTHOFAxdk1? M3HaV|I1NzR6IHi= M3fNRZN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= Ml;HNlI2PjZ4MES=
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8226 NHO2enRHfW6ldHnvckBCe3OjeR?= Ml:1NVAxNTFyMECgcm0> NV3odmhrOzBibXnu M3[3cmROW09? M2i4[YFkfGm4YYTld{BGWkwEoB?= MWSyNlU2PjRyOR?=
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MM1.S  M3XzOmZ2dmO2aX;uJGF{e2G7 NHPmNVkxNjVizszN NV3DU|E1OzBibXnu M{HDfmROW09? MYnpcoR2[2W|IHHjeIl3[XSrb36gc4YhWkGIIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhVUWN MYCyNlU2PjRyOR?=
MCF-7 NEPBWZNHfW6ldHnvckBCe3OjeR?= NGPX[GI2OC9{MECvOVAxKG6P MmrSN|AhdWmw NWHhVpRs\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MkXzNlI1PzZ6NUK=
T47D NIDIWWxHfW6ldHnvckBCe3OjeR?= MYq1NE8zODBxNUCwJI5O M4T6RlMxKG2rbh?= NWjrUIRW\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? NWnDblhLOjJ2N{[4OVI>
MDA-MB-231 MVHGeY5kfGmxbjDBd5NigQ>? Ml\COVAwOjByL{WwNEBvVQ>? M1HJ[|MxKG2rbh?= MoTT[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NF7xdIQzOjR5Nki1Ni=>
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MCF-7 NEXue4JCeG:ydH;zbZMhSXO|YYm= M1uzbVIxOMLibl2= MVSzOkBp M{TDc2ROW09? M{WzSolv\HWlZYOgZZBweHSxc3nz NUfpZWlLOjJ2N{[4OVI>
MDA-MB-231 Mk\nRZBweHSxc3nzJGF{e2G7 M2\BXFIxOMLibl2= NHnwfYU{PiCq MkLaSG1UVw>? M3[5RYlv\HWlZYOgZZBweHSxc3nz NYnrUmptOjJ2N{[4OVI>
Bcap-37 MmXXRZBweHSxc3nzJGF{e2G7 NWLXW45jOjBywrDuUS=> MVezOkBp MU\EUXNQ M4TRSYlv\HWlZYOgZZBweHSxc3nz NXn0blU1OjJ2N{[4OVI>
LS174T MmTHSpVv[3Srb36gRZN{[Xl? NUDsZm5xOTBxMUCwM|ExODBibl2= M1yye|YhcA>? MXLEUXNQ NGLFVWhqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv MYOyNlQxOTJ7NB?=
DLD-1  NFvuSndHfW6ldHnvckBCe3OjeR?= MVyxNE8yODBxMUCwNEBvVQ>? NXjVOZo2PiCq MWDEUXNQ NVTuUZY4cW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? NHzhdYgzOjRyMUK5OC=>
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SW620 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT4TVFKSzVyPUGxJO69VQ>? NV70dGREOjJ{N{CyOVc>
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NIH 3T3 NWXtPVg1TnWwY4Tpc44hSXO|YYm= NIDQV2czKM7:TR?= Mn31NVghcA>? NXXJUpNkcW6qaXLpeJMhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3Rib36gV4VzPDd|IHHu[EBuXE:UQ{GgdIhwe3Cqb4L5cIF1cW:wIH;mJFRGNUKSMTDvckBVcHJ|Nz:0Oi=> MkGyNlE5PzZzM{C=
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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]
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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]
+ 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