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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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 NXjBc4xLTnWwY4Tpc44hSXO|YYm= M3G2VVUxNTF{NUCgcm0> MVOyOEBp MXTEUXNQ M17TfYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPiCtaX7hd4UhMHSjcnfleEBw\iCvVF;SR|EqKGGwZDDpeJMh\G:5boP0doVidSC2YYLn[ZQheGixc4Doc{1UPsLi NV7abHVSOjZzN{ewOVE>
U87vIII  M2\NWWZ2dmO2aX;uJGF{e2G7 NWi0fokzOC5yND2yMlUh|ryP MlPrNlQhcA>? M2TUVYlvcGmkaYTzJI1VV1KFMTDhcoQhdVSRUlOyJIFkfGm4aYTp[ZPDqA>? MkLWNlYyOzR4MUe=
U87vIII  M1XDWWZ2dmO2aX;uJGF{e2G7 NHjvU2czNjVxNTFOwG0> MW[xNkBp NXn5OWtYcW6qaXLpeJMh\2GyIHPsc5NqdmdiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1G3dFI3OTN2NkG3
PC12  MmnKSpVv[3Srb36gRZN{[Xl? MWG0NOKhdk1? NV35fVJ[cW6mdXPld{BtgXOxc3;tZYwh[mmxZ3Xu[ZNqeyCjbnSgZYxt\X[rYYTl[EDPuS2VWV6gZYNkfW23bHH0bY9vyqB? MVSyOlAxOTZzNB?=
3T3-L1 M{ixPGZ2dmO2aX;uJGF{e2G7 MnLPNVUh|ryP M2DzeFQhcA>? M4TOdZN2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhTWe{MTDwdo91\WmwwrC= MorJNlU5OTR4NkK=
Rh30 M{HYUmZ2dmO2aX;uJGF{e2G7 NXnNPXM1OSEQvF2= MVqyJIg> NGnreVBqdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= Mo\oNlU4PjJ4MUm=
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Rh30 MljpSpVv[3Srb36gRZN{[Xl? NV;ZOJNkOSEQvF2= MUSyJIg> M3[0bJN2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> MoTENlU4PjJ4MUm=
HT29 NFvEVHlHfW6ldHnvckBCe3OjeR?= MX[xJO69VQ>? NYjk[WltOiCq NI\sdZF{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> MnrZNlU4PjJ4MUm=
U87 M4L1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUiyOUBvVQ>? NW[5cFJHOjRiaB?= NEDhOlZqdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> Mn6xNlU2Pjh4NkW=
AGS MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NW\pPGprOC1zMECwJI5O MVmyOE81QCCq MkT2SG1UVw>? MU\k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M3X1fFI2ODN3OU[x
MKN45 M3e4W2NmdGxiVnnhZoltcXS7IFHzd4F6 NEP2bFAxNTFyMECgcm0> NVHpbGFGOjRxNEigbC=> NUPUNpg4TE2VTx?= NXH1RZVE\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NVz2[ZU{OjVyM{W5OlE>
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KATO3 Mor1R4VtdCCYaXHibYxqfHliQYPzZZk> MWWwMVExODBibl2= MV2yOE81QCCq MX\EUXNQ NFjrXpBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NWO0VXZFOjVyM{W5OlE>
SGC7901 MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWXDXFlvOC1zMECwJI5O NIXFe4szPC92ODDo Ml70SG1UVw>? NUDpRYxz\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MXKyOVA{PTl4MR?=
N87 M4nrR2NmdGxiVnnhZoltcXS7IFHzd4F6 MnXHNE0yODByIH7N MVOyOE81QCCq MXLEUXNQ NXXTfVhV\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MXKyOVA{PTl4MR?=
HMEC MWjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkOzNE0yODByIH7N M4\VflI1NzR6IHi= NUHjeYhXTE2VTx?= NE\4SpBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ Mkn1NlUxOzV7NkG=
HUVEC M2fVPWNmdGxiVnnhZoltcXS7IFHzd4F6 NX7vWlNlOC1zMECwJI5O MkXrNlQwPDhiaB?= MUPEUXNQ NFjYe|Fl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M4DjcFI2ODN3OU[x
MG63 NX2zW5pxTnWwY4Tpc44hSXO|YYm= NH[5c4c2OC1zMECwJI5O NX;JN2pKOC53IHi= NF3J[otld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NF\iTZIzPDh2MEGzOC=>
U2OS  MVjGeY5kfGmxbjDBd5NigQ>? MVe1NE0yODByIH7N M3vGfFAvPSCq MVrkc5NmKGSncHXu[IVvfGy7IDi1NQKBmzFyMECgcm0qKGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= M4PLT|I1QDRyMUO0
Saos-2  NFHSUpJHfW6ldHnvckBCe3OjeR?= M4\a[|UxNTFyMECgcm0> M3;tNVAvPSCq MlHP[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NFjFNmMzPDh2MEGzOC=>
Saos-2 NF;aW41HfW6ldHnvckBCe3OjeR?= M3\sblExOCCwTR?= MlTwNE42KGh? NWfycGJReHKndnXueJMhd3O2ZX;zZZJkd22jIHPlcIwhdWmpcnH0bY9v MUKyOFg1ODF|NB?=
MG63 MW\BdI9xfG:|aYOgRZN{[Xl? M{jTcFExOCCwTR?= NFK4U|k{PiCq M3\UNJBzd22xdHXzJIFxd3C2b4Ppdy=> MVSyOFg1ODF|NB?=
U2OS  MoDhRZBweHSxc3nzJGF{e2G7 Mmf3NVAxKG6P M{PX[FM3KGh? NVKxTnQyeHKxbX;0[ZMh[XCxcITvd4l{ NVvHWY5FOjR6NECxN|Q>
Saos-2  M{TFTGFxd3C2b4Ppd{BCe3OjeR?= M3\keVExOCCwTR?= NYXrTlZZOzZiaB?= NIDON5Zxem:vb4Tld{BieG:ydH;zbZM> NF7jOXUzPDh2MEGzOC=>
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UM-UC-3 NWnX[|lDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\GR3pUUUN3ME2wMlY{KMLzMD6xJO69VQ>? MV6yOFA2PDh5MR?=
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HT29 NYLLbI5zS2WubDDWbYFjcWyrdImgRZN{[Xl? NVrORW5oOC1zMECwJI5O M2LiO|I1KGh? MmDTbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmDxNlM6QTFzN{m=
H116 NInrNJFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3e0U|AuOTByMDDuUS=> NHOzfo8zPCCq NF:4eYxqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUCyN|k6OTF5OR?=
Hct-8 NV7q[JVCS2WubDDWbYFjcWyrdImgRZN{[Xl? NHP5N3UxNTFyMECgcm0> MnPkNlQhcA>? M3HEXolvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUGyN|k6OTF5OR?=
Colo320 NYTXTXhtS2WubDDWbYFjcWyrdImgRZN{[Xl? NWPScJduOC1zMECwJI5O NV\NV3BlOjRiaB?= MkjEbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVq3b4s{OjN7OUGxO|k>
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Colo205 M2S5R2NmdGxiVnnhZoltcXS7IFHzd4F6 NUfZb3B5OC1zMECwJI5O NGfzbnczPCCq NFXwNotqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXuyN|k6OTF5OR?=
Colo320 M2O2[mZ2dmO2aX;uJGF{e2G7 NEPMTZcyKM7:TR?= MYiwMVI1KGh? NFjhd4Ri[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 M3\XclI{QTlzMUe5
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SW620 NWXlU|VNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTdwODFOwG0> MUOyN|U1OjF5OB?=
SW480 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{W3TGlEPTB;ND62JO69VQ>? MX6yN|U1OjF5OB?=
SK-CO-1 NGfob2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TFSGlEPTB;NDFOwG0> MnLiNlM2PDJzN{i=
LS-513 NV3jd2luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPoTWM2OD1|Lkmg{txO MXyyN|U1OjF5OB?=
SW1116 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLNTWM2OD1yLki0JO69VQ>? MVOyN|U1OjF5OB?=
LS-174T M2DFOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfkUmNKSzVyPUCuPFQh|ryP MnjYNlM2PDJzN{i=
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HT-29 NYD1Vmo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwMkOg{txO MWeyN|U1OjF5OB?=
COLO 201 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTaTWM2OD1yLkKzJO69VQ>? MWGyN|U1OjF5OB?=
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SW48 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwMEmg{txO MkXuNlM2PDJzN{i=
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TMD8 Mlj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVywMlI2NzBwNT:xJO69VQ>? NV;HR4hYTE2VTx?= MlHibY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXyyN|Q5Ojd2OB?=
Jurkat M{LOWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TiOVAvOjVxMD61M|Eh|ryP NGS4b2tFVVOR NIXIbXlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MorONlM1QDJ5NEi=
KOPT-K1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzJNE4zPS9yLkWvNUDPxE1? MkHESG1UVw>? M13TOolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M1fSV|I{PDh{N{S4
TMD7 Ml21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV34fnlZOC5{NT:wMlUwOSEQvF2= NXXsRWo{TE2VTx?= NYfvbItPcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M3HsVVI{PDh{N{S4
THP-1 M3P6VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NID0WngxNjJ3L{CuOU8yKM7:TR?= MU\EUXNQ M4LCb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MljuNlM1QDJ5NEi=
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786-O MXHGeY5kfGmxbjDBd5NigQ>? NVTZXI9IOC1yLkWg{txO MVSyOEBp NE\RdHhFVVOR MoHFdoV{fWy2czDpckBiKGSxc3Wg[IVx\W6mZX70JIlv[3KnYYPlJIlvKEVvY3HkbIVzcW5icILveIVqdiCneIDy[ZN{cW:wwrC= MYqyN|E1PzJ3MR?=
OCI-AML3 MVnBdI9xfG:|aYOgRZN{[Xl? Ml:yNk42KM7:TR?= MVi3NkBp NILuVWxqdmS3Y3XzJIFxd3C2b4Ppdy=> NH\5O2UzOjh{NkW2OS=>
Jurkat MUHGeY5kfGmxbjDBd5NigQ>? M{PSSlExOC9{MECvOFAxKG6P M13PTFE5KGh? MkS3bY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= MofZNlI2PjZ4MES=
p210 BCR-Abl NUizS2xrTnWwY4Tpc44hSXO|YYm= MoTNNVAxNzJyMD:0NFAhdk1? NV\GeJpmOThiaB?= Ml3KbY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= MYmyNlU3PjZyNB?=
Jurkat Mn3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUK0NFBvVQ>? MV:yOE81QCCq MkDtd5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= M1qyc|IzPTZ4NkC0
p210 BCR-Abl M3rpR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmX4OFAxdk1? MU[yOE81QCCq MULzfY5memerenWge4l1cCBzNz3BRWchfG9ic4XwdJJme3NiY3XscEBxem:uaX\ldoF1cW:w MWSyNlU3PjZyNB?=
8226 NYnJVoVJTnWwY4Tpc44hSXO|YYm= MWmxNFAuOTByMDDuUS=> NFTuWmY{OCCvaX6= NXnU[IlRTE2VTx?= NH\WUG9i[3SrdnH0[ZMhTVKNwrC= NUTQZWxSOjJ3NU[0NFk>
MM1.S  MkjhSpVv[3Srb36gRZN{[Xl? MmnzNVAxNTFyMECgcm0> Ml7LN|AhdWmw NEnESolFVVOR M{\2WoFkfGm4YYTld{BGWkwEoB?= NH;0[ZQzOjV3NkSwPS=>
8226 MlnUSpVv[3Srb36gRZN{[Xl? MonaNE42KM7:TR?= MVyzNEBucW5? MXXEUXNQ NWKzOnFKcW6mdXPld{Bi[3SrdnH0bY9vKG:oIGLBSkBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIF3FTy=> NFLE[pQzOjV3NkSwPS=>
MM1.S  NWP6dYRrTnWwY4Tpc44hSXO|YYm= Mlv6NE42KM7:TR?= MWWzNEBucW5? MVrEUXNQ MYrpcoR2[2W|IHHjeIl3[XSrb36gc4YhWkGIIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhVUWN MnfvNlI2PTZ2MEm=
MCF-7 Mn[ySpVv[3Srb36gRZN{[Xl? NWKwU4RlPTBxMkCwM|UxOCCwTR?= MnO3N|AhdWmw MoXo[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> Mnm3NlI1PzZ6NUK=
T47D NYrmPVhvTnWwY4Tpc44hSXO|YYm= M1ruNlUxNzJyMD:1NFAhdk1? M4XublMxKG2rbh?= MkT5[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NHnVbVUzOjR5Nki1Ni=>
MDA-MB-231 MY\GeY5kfGmxbjDBd5NigQ>? NHT4bHo2OC9{MECvOVAxKG6P MmTVN|AhdWmw M1z0e4Rwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 M3;sblIzPDd4OEWy
Bcap-37 MY\GeY5kfGmxbjDBd5NigQ>? Mly1OVAwOjByL{WwNEBvVQ>? MknQN|AhdWmw MmLn[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NIHGeFkzOjR5Nki1Ni=>
MCF-7 MlPMRZBweHSxc3nzJGF{e2G7 MlH1NlAxyqCwTR?= NYGwR4EzOzZiaB?= NEmycm1FVVOR M2nSfYlv\HWlZYOgZZBweHSxc3nz Mln6NlI1PzZ6NUK=
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LS174T NIDw[JFHfW6ldHnvckBCe3OjeR?= NGX0PVMyOC9zMECvNVAxOCCwTR?= MV62JIg> NITofWdFVVOR Mn:wbY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> NYXnWVkxOjJ2MEGyPVQ>
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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 individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
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