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 MVXGeY5kfGmxbjDBd5NigQ>? Mk[xOVAuOTJ3MDDuUS=> NGm4fYozPCCq M3HEVWROW09? Ml\1bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHM3KGurbnHz[UApfGG{Z3X0JI9nKG2WT2LDNUkh[W6mIHn0d{Bld3ewc4Ty[YFuKHSjcnfleEBxcG:|cHjvMXM3yqB? M1f4eFI3OTd5MEWx
U87vIII  M{nRd2Z2dmO2aX;uJGF{e2G7 NGPMN3MxNjB2LUKuOUDPxE1? M1TYO|I1KGh? MnLobY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh NWLBfYlzOjZzM{S2NVc>
U87vIII  M{Wwb2Z2dmO2aX;uJGF{e2G7 NXXSVmt2Oi53L{Wg{txO M{L6[|EzKGh? MX7pcohq[mm2czDnZZAh[2yxc3nu[{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1\iV|I3OTN2NkG3
PC12  NYnSWHFmTnWwY4Tpc44hSXO|YYm= NH\2SXE1OMLibl2= NFfXbZNqdmS3Y3XzJIx6e2:|b33hcEBjcW:pZX7ld4l{KGGwZDDhcIxmfmmjdHXkJO6yNVO\TjDhZ4N2dXWuYYTpc47DqA>? MonaNlYxODF4MUS=
3T3-L1 M17BdWZ2dmO2aX;uJGF{e2G7 M2LaNVE2KM7:TR?= MlHlOEBp NUW0fJdYe3WycILld5NmeyCneIDy[ZN{cW:wIH;mJJRp\SCHZ4KxJJBzd3SnaX9CpC=> M2DjOFI2QDF2Nk[y
Rh30 MmDYSpVv[3Srb36gRZN{[Xl? M3rEXVEh|ryP MmrINkBp MnrnbY5pcWKrdIOgZo91cCCvVF;SR|EudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKFN4S{GgZY5lKG2WT2LDNk1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhSWu2 NXr2WGJVOjV5NkK2NVk>
HT29 MUHGeY5kfGmxbjDBd5NigQ>? MlXFNUDPxE1? MlewNkBp NUfz[ZdtcW6qaXLpeJMh[m:2aDDtWG9TSzFvbXXkbYF1\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGO2T|Eh[W6mIH3UU3JEOi2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NH;MNYgzPTd4Mk[xPS=>
Rh30 NX\re25iTnWwY4Tpc44hSXO|YYm= MojxNUDPxE1? MXmyJIg> NEXJS2F{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> NUHkb5g6OjV5NkK2NVk>
HT29 M{PzU2Z2dmO2aX;uJGF{e2G7 MX2xJO69VQ>? NVvrSoZyOiCq M4S4WZN2eHC{ZYPz[ZMhfGinIHLhd4FtKG:{IFnHSk0yNXO2aX31cIF1\WRiY3XscEBi\Ginc3nvci=> NE\nb|QzPTd4Mk[xPS=>
U87 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoriNlUhdk1? NF\2cJYzPCCq NHSxR45qdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> MlfBNlU2Pjh4NkW=
AGS MVrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUKwMVExODBibl2= MmT3NlQwPDhiaB?= M2fIc2ROW09? MXfk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NUS2[GlqOjVyM{W5OlE>
MKN45 M{XDeGNmdGxiVnnhZoltcXS7IFHzd4F6 M3\5[lAuOTByMDDuUS=> NFjJdY8zPC92ODDo Mnv3SG1UVw>? M{P5VoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MkLkNlUxOzV7NkG=
MKN28 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnzxNE0yODByIH7N Ml\QNlQwPDhiaB?= MXzEUXNQ M4rzboRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MkXBNlUxOzV7NkG=
KATO3 NXzIRmhES2WubDDWbYFjcWyrdImgRZN{[Xl? NF3BXYoxNTFyMECgcm0> M1LQWlI1NzR6IHi= MX3EUXNQ MV\k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M13UUFI2ODN3OU[x
SGC7901 MmLIR4VtdCCYaXHibYxqfHliQYPzZZk> NFPwZXgxNTFyMECgcm0> MoDmNlQwPDhiaB?= M4r4TGROW09? NVzKZZJr\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NFrRW4szPTB|NUm2NS=>
N87 NGLRSXNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mmi3NE0yODByIH7N MUCyOE81QCCq MXjEUXNQ MWTk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MnfSNlUxOzV7NkG=
HMEC MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mk\MNE0yODByIH7N MnXDNlQwPDhiaB?= MmDUSG1UVw>? NXK2[29H\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= Mo\XNlUxOzV7NkG=
HUVEC NEXCNnhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVWwMVExODBibl2= M3zNSVI1NzR6IHi= NEfJendFVVOR NH35bWVl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M1;rOVI2ODN3OU[x
MG63 MkTJSpVv[3Srb36gRZN{[Xl? MVq1NE0yODByIH7N MVSwMlUhcA>? MkHh[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 MnP4NlQ5PDBzM{S=
U2OS  MmjqSpVv[3Srb36gRZN{[Xl? NF7Ie5c2OC1zMECwJI5O NXjDXIhtOC53IHi= NIjN[3Zld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NVzrWY5{OjR6NECxN|Q>
Saos-2  MomySpVv[3Srb36gRZN{[Xl? Mlf5OVAuOTByMDDuUS=> NVPCPYF1OC53IHi= NH7WTmFld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NYKzT281OjR6NECxN|Q>
Saos-2 NG\KZmRHfW6ldHnvckBCe3OjeR?= MWKxNFAhdk1? NIrTd40xNjViaB?= NVX0ZXBjeHKndnXueJMhd3O2ZX;zZZJkd22jIHPlcIwhdWmpcnH0bY9v NXmxfVQ2OjR6NECxN|Q>
MG63 MknKRZBweHSxc3nzJGF{e2G7 NFTGPG4yODBibl2= NF;rTHU{PiCq NH\y[HNxem:vb4Tld{BieG:ydH;zbZM> M4XUXlI1QDRyMUO0
U2OS  NGHXbJRCeG:ydH;zbZMhSXO|YYm= NF\mdYUyODBibl2= MkHrN|YhcA>? NEPuWWpxem:vb4Tld{BieG:ydH;zbZM> MXKyOFg1ODF|NB?=
Saos-2  MXTBdI9xfG:|aYOgRZN{[Xl? NHnTfFUyODBibl2= M4judFM3KGh? MYPwdo9ud3SnczDhdI9xfG:|aYO= MXqyOFg1ODF|NB?=
HT1376 MkDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfpSJJrUUN3ME2xMlg5KMLzIEGuNUDPxE1? MljXNlQxPTR6N{G=
T24 M3HSNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXxTWM2OD1zLkO3JOKyKDBwNDFOwG0> NWLhZoo{OjRyNUS4O|E>
UM-UC-3 NYixN3BIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLmTWM2OD1yLk[zJOKyOC5zIN88US=> NWXYSJFbOjRyNUS4O|E>
DLD-1 NHfXUWFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIfUN4IxNTFyMECgcm0> MYOyOEBp M1uwZolvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M4qxNlI{QTlzMUe5
Caco2 M{Xjc2NmdGxiVnnhZoltcXS7IFHzd4F6 M4fic|AuOTByMDDuUS=> MWeyOEBp MX\pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NHjab3QzOzl7MUG3PS=>
HT29 NGnlWZlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVXlUIVxOC1zMECwJI5O M4fsUVI1KGh? MWrpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MYGyN|k6OTF5OR?=
H116 NUDLeY5MS2WubDDWbYFjcWyrdImgRZN{[Xl? MWWwMVExODBibl2= M4W0dFI1KGh? Mn;tbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnixNlM6QTFzN{m=
Hct-8 NITCTXhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWWwTXRZOC1zMECwJI5O M1W5XlI1KGh? NHPlSY5qdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVGyN|k6OTF5OR?=
Colo320 Mn6yR4VtdCCYaXHibYxqfHliQYPzZZk> NU\5SXB1OC1zMECwJI5O NIi2V2ozPCCq M2\LZYlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1\jR|I{QTlzMUe5
Sw948 NYXufHQ6S2WubDDWbYFjcWyrdImgRZN{[Xl? NIjHOXUxNTFyMECgcm0> M2nUZlI1KGh? MlvtbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MljiNlM6QTFzN{m=
Colo205 NFi5TWJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3XCSVAuOTByMDDuUS=> NYjZcWhHOjRiaB?= MoXZbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXSyN|k6OTF5OR?=
Colo320 NHuzZ5RHfW6ldHnvckBCe3OjeR?= NXPXOGZLOSEQvF2= MkLlNE0zPCCq NH\ySnBi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 M3HRZ|I{QTlzMUe5
HT29 MVfGeY5kfGmxbjDBd5NigQ>? NHrNRWUyKM7:TR?= MVqwMVI1KGh? MlPwZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> MUKyN|k6OTF5OR?=
Sw948 MVPGeY5kfGmxbjDBd5NigQ>? MX:xJO69VQ>? NXLlVnR1OC1{NDDo M4rXc4Fjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> MojONlM6QTFzN{m=
DLD-1 MX7GeY5kfGmxbjDBd5NigQ>? M3zJRVEh|ryP M2jnWFAuOjRiaB?= M1:1W4Fjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> NWnRPVlxOjN7OUGxO|k>
SW620 M2PDUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTdwODFOwG0> MoflNlM2PDJzN{i=
SW480 NYTWTmJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojjTWM2OD12Lk[g{txO Ml;xNlM2PDJzN{i=
SK-CO-1 MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEW1UHJKSzVyPUSg{txO M4f0XFI{PTR{MUe4
LS-513 MonMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLabZl{UUN3ME2zMlkh|ryP MlfjNlM2PDJzN{i=
SW1116 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHaZoRKSzVyPUCuPFQh|ryP MnPMNlM2PDJzN{i=
LS-174T MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3e3e2lEPTB;MD64OEDPxE1? Mn;XNlM2PDJzN{i=
HCT 116 NH7VRZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK3WWtKSzVyPUCuOFEh|ryP Mkj1NlM2PDJzN{i=
HCT 15 NFqx[XRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnuzTWM2OD1yLkOg{txO NIC3PHQzOzV2MkG3PC=>
COLO 205 M2DKdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHPTWM2OD1yLkK0JO69VQ>? NF;ufHUzOzV2MkG3PC=>
HT-29 M33Gbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwMkOg{txO M{XDTlI{PTR{MUe4
COLO 201 NXTCSZZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TrbGlEPTB;MD6yN{DPxE1? Mn;pNlM2PDJzN{i=
Caco-2 NHrM[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXXTWM2OD1yLkKyJO69VQ>? MlvONlM2PDJzN{i=
SW48 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO5TWM2OD1yLkC5JO69VQ>? NYTIT45ROjN3NEKxO|g>
DND-1 NVfqfXZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\aNE4zPS9yLkWvNUDPxE1? Ml;tSG1UVw>? NFnxUYhqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MkH1NlM1QDJ5NEi=
TMD8 NEK1c41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnqwNE4zPS9yLkWvNUDPxE1? MV;EUXNQ NVvhNnpCcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NF\QRlIzOzR6Mke0PC=>
Jurkat MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVOweYZxOC5{NT:wMlUwOSEQvF2= M2X0ZWROW09? Moe4bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MknuNlM1QDJ5NEi=
KOPT-K1 NIe1VnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\ONE4zPS9yLkWvNUDPxE1? MXPEUXNQ M3XXNIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NYraPI5LOjN2OEK3OFg>
TMD7 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLJZlkxNjJ3L{CuOU8yKM7:TR?= NV\0flVYTE2VTx?= MlfvbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M1nXOFI{PDh{N{S4
THP-1 M3jwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7LNE4zPS9yLkWvNUDPxE1? M3XCfGROW09? MUnpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M4jxXVI{PDh{N{S4
786-O NXL0Z|E{TnWwY4Tpc44hSXO|YYm= NUPwSpp[OC5zL{CuOUDPxE1? NG\4[W8zPCCq NEHaZlNFVVOR Mn;GbY5kemWjc3XzJGUu[2GmaHXybY4hdVKQQTDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgQ>? NV7kN4ZiOjNzNEeyOVE>
786-O MnTCSpVv[3Srb36gRZN{[Xl? NX3ZOFRwOC1yLkWg{txO NVziVHpZOjRiaB?= Ml[1SG1UVw>? NEn0cZRz\XO3bITzJIlvKGFiZH;z[UBl\XCnbnTlcpQhcW6lcnXhd4UhcW5iRT3jZYRp\XKrbjDwdo91\WmwIHX4dJJme3Orb39CpC=> NHG0ZnczOzF2N{K1NS=>
OCI-AML3 M37jPWFxd3C2b4Ppd{BCe3OjeR?= NFzyXHozNjVizszN MWm3NkBp NYDHZ4RtcW6mdXPld{BieG:ydH;zbZM> MWOyNlgzPjV4NR?=
Jurkat M1zidmZ2dmO2aX;uJGF{e2G7 NInhRpUyODBxMkCwM|QxOCCwTR?= MknVNVghcA>? NI[2[lZqdmirYnn0d{BuXE:UQ{Gt[IVx\W6mZX70JHM3KFN{M{WvNlM3KHCqb4PwbI9zgWyjdHnvci=> Mk\HNlI2PjZ4MES=
p210 BCR-Abl NG\Jfo9HfW6ldHnvckBCe3OjeR?= NETMWIkyODBxMkCwM|QxOCCwTR?= MlzPNVghcA>? MkHmbY5pcWKrdIOgcXRQWkNzLXTldIVv\GWwdDDTOkBUOjN3L{KzOkBxcG:|cHjvdplt[XSrb36= M2j3VVIzPTZ4NkC0
Jurkat NHuzTotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[0NFBvVQ>? MmfiNlQwPDhiaB?= NXfENlU{e3mwZYLnbZpmKHerdHigNVcuSUGJIITvJJN2eHC{ZYPzJINmdGxicILvcIln\XKjdHnvci=> M4LWZVIzPTZ4NkC0
p210 BCR-Abl NEDvbmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLhTIRMPDBybl2= M{Ljd|I1NzR6IHi= MlLHd5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= Mn\UNlI2PjZ4MES=
8226 NYfT[XdOTnWwY4Tpc44hSXO|YYm= MUWxNFAuOTByMDDuUS=> MYezNEBucW5? NILJWXdFVVOR M4\weoFkfGm4YYTld{BGWkwEoB?= MmD1NlI2PTZ2MEm=
MM1.S  MY\GeY5kfGmxbjDBd5NigQ>? NEXGO2YyODBvMUCwNEBvVQ>? M4DGOVMxKG2rbh?= NWPTV3JqTE2VTx?= NY\JWFYy[WO2aY\heIV{KEWUS9Mg MlW1NlI2PTZ2MEm=
8226 MofiSpVv[3Srb36gRZN{[Xl? Ml25NE42KM7:TR?= MX6zNEBucW5? MV3EUXNQ NFiwVY9qdmS3Y3XzJIFkfGm4YYTpc44hd2ZiUlHGJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiTVXL NGLjTpYzOjV3NkSwPS=>
MM1.S  NIHrWlBHfW6ldHnvckBCe3OjeR?= NH;tcIwxNjVizszN Mk\3N|AhdWmw NG[zTHFFVVOR NV3nNJpvcW6mdXPld{Bi[3SrdnH0bY9vKG:oIGLBSkBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIF3FTy=> Mon0NlI2PTZ2MEm=
MCF-7 M2fNfmZ2dmO2aX;uJGF{e2G7 NVu0bFJIPTBxMkCwM|UxOCCwTR?= NX\z[ZZJOzBibXnu NYK5bZpQ\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MX6yNlQ4Pjh3Mh?=
T47D NU\l[II2TnWwY4Tpc44hSXO|YYm= MlL3OVAwOjByL{WwNEBvVQ>? NXvxWJI5OzBibXnu M{j1RoRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MVGyNlQ4Pjh3Mh?=
MDA-MB-231 NVHI[YJQTnWwY4Tpc44hSXO|YYm= NFrXeXc2OC9{MECvOVAxKG6P MVuzNEBucW5? Mme3[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MkDVNlI1PzZ6NUK=
Bcap-37 MV;GeY5kfGmxbjDBd5NigQ>? MmjaOVAwOjByL{WwNEBvVQ>? M3mzb|MxKG2rbh?= Mk\K[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> M{LobFIzPDd4OEWy
MCF-7 M4i4NWFxd3C2b4Ppd{BCe3OjeR?= MViyNFDDqG6P NUPI[4p{OzZiaB?= M4nhSGROW09? MnjUbY5lfWOnczDhdI9xfG:|aYO= NG\BcZUzOjR5Nki1Ni=>
MDA-MB-231 MV;BdI9xfG:|aYOgRZN{[Xl? M3\aNVIxOMLibl2= MlHHN|YhcA>? MYnEUXNQ MXXpcoR2[2W|IHHwc5B1d3Orcx?= NUPZcG81OjJ2N{[4OVI>
Bcap-37 NEHDNJNCeG:ydH;zbZMhSXO|YYm= MWWyNFDDqG6P NILPdGU{PiCq M3K2WmROW09? NUfoUlFZcW6mdXPld{BieG:ydH;zbZM> Mk\wNlI1PzZ6NUK=
LS174T NUGzRWt7TnWwY4Tpc44hSXO|YYm= MXmxNE8yODBxMUCwNEBvVQ>? M4j3VlYhcA>? MWnEUXNQ NIH0RYZqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv NWLxVZJIOjJ2MEGyPVQ>
DLD-1  MVfGeY5kfGmxbjDBd5NigQ>? NYPMSnE1OTBxMUCwM|ExODBibl2= MnWwOkBp M{HEPGROW09? NF\uV3FqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv NWPXO5pDOjJ2MEGyPVQ>
SW480 MUfGeY5kfGmxbjDBd5NigQ>? Mle2NVAwOTByL{GwNFAhdk1? MXS2JIg> MXLEUXNQ MoLobY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> NWX0PZk{OjJ2MEGyPVQ>
SW-48 M4niV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\kTWM2OD1yLkGg{txO M3TVPFIzOjdyMkW3
HCT-15 NUnvWpFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLsfGxKSzVyPUCuN{DPxE1? NGPzUYgzOjJ5MEK1Oy=>
HCT 116 M2fu[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PyemlEPTB;MD62JO69VQ>? NVr0cYFpOjJ{N{CyOVc>
SW620-R NF;oZmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H6emlEPTB;MT6zJO69VQ>? Mo[5NlIzPzB{NUe=
SK-CO-1 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTJwMTFOwG0> MViyNlI4ODJ3Nx?=
SW620 NFjqc3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXOSWVFUUN3ME2xNUDPxE1? NX\FdnY{OjJ{N{CyOVc>
BaF3 NX[xb2l2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnO0S2k2OD1zLkS0PUDPxE1? MYGyNlIzOzZ2NR?=
NIH 3T3 NYi4PVJTTnWwY4Tpc44hSXO|YYm= NFPjZpQzKM7:TR?= M4\YU|E5KGh? MUXpcohq[mm2czDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBwdiCVZYK0O|Mh[W6mIH3UU3JEOSCyaH;zdIhwenmuYYTpc44hd2ZiNFWtRnAyKG:wIGTodlM4NzR4 NG\6XZYzOTh5NkGzNC=>
HCT15 M4TYT2Z2dmO2aX;uJGF{e2G7 MXewMlUwOiEQvF2= M4nPbVQhcA>? NWHRco5seHKndnXueJMhWz[NMTDwbI9{eGixconsZZRqd25ib3[gdoljd3OxbXHsJJBzd3SnaX6gV|Yh[XRiU3XyNlQxNzJ2NDDhcoQhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3RiYYSgV4VzPDd| NGnEd5gzOTh5NkGzNC=>
SW620  M3fWZ2Z2dmO2aX;uJGF{e2G7 NWTzeWExOC53L{Kg{txO MXe0JIg> M{HnTYJtd2OtczDhcIwhfGi{ZXWgcXRQWiCxdYTweZR{ MlTHNlE5PzZzM{C=

... 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(Data is from Selleck tests instead of citations):
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
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.

  • * 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.

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