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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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 MoD3SpVv[3Srb36gRZN{[Xl? MUK1NE0yOjVyIH7N MmTGNlQhcA>? NUPxO2h1TE2VTx?= NGXFVFhqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZia3nuZZNmKCi2YYLn[ZQhd2ZibWTPVmMyMSCjbnSgbZR{KGSxd37zeJJm[W1idHHy[4V1KHCqb4PwbI8uWzcEoB?= NXmzPVhiOjZzN{ewOVE>
U87vIII  NFrFNYlHfW6ldHnvckBCe3OjeR?= MlzZNE4xPC1{LkWg{txO MmfiNlQhcA>? MkflbY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh NWnxTZB1OjZzM{S2NVc>
U87vIII  NIDtWGdHfW6ldHnvckBCe3OjeR?= MWmyMlUwPSEQvF2= NIDpWnMyOiCq M1f5WYlvcGmkaYTzJIdieCClbH;zbY5oKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGfyOZMzPjF|NE[xOy=>
PC12  MmjuSpVv[3Srb36gRZN{[Xl? MV[0NOKhdk1? MmqybY5lfWOnczDsfZNwe2:vYXygZolw\2WwZYPpd{BidmRiYXzs[ZZq[XSnZDFOtU1UYU5iYXPjeY12dGG2aX;uxsA> M4S4clI3ODBzNkG0
3T3-L1 MkLPSpVv[3Srb36gRZN{[Xl? NWniXYd3OTVizszN NH;jWWU1KGh? M2LGV5N2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhTWe{MTDwdo91\WmwwrC= MXWyOVgyPDZ4Mh?=
Rh30 M2G5WWZ2dmO2aX;uJGF{e2G7 MVKxJO69VQ>? MXmyJIg> MVfpcohq[mm2czDic5RpKG2WT2LDNU1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhWz[NMTDhcoQhdVSRUlOyMY1m\GmjdHXkJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MYCyOVc3OjZzOR?=
HT29 M2jYPWZ2dmO2aX;uJGF{e2G7 NHfu[VgyKM7:TR?= Mkj0NkBp M4PqfYlvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= NE\5O3czPTd4Mk[xPS=>
Rh30 NEfrUIhHfW6ldHnvckBCe3OjeR?= MXyxJO69VQ>? MXOyJIg> NIraeHN{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> NXX0elhiOjV5NkK2NVk>
HT29 NUnWdnc1TnWwY4Tpc44hSXO|YYm= NELjW4wyKM7:TR?= MXeyJIg> Ml21d5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u MYGyOVc3OjZzOR?=
U87 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojXNlUhdk1? MVWyOEBp NF25OXFqdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> MWCyOVU3QDZ4NR?=
AGS NWHQO|BjS2WubDDWbYFjcWyrdImgRZN{[Xl? Mk\HNE0yODByIH7N MmPwNlQwPDhiaB?= NXzCPXZ3TE2VTx?= MX3k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NUC0SW5pOjVyM{W5OlE>
MKN45 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MonHNE0yODByIH7N NWfOdG9bOjRxNEigbC=> NFPJfnhFVVOR M{TkXoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1HM[FI2ODN3OU[x
MKN28 M13VdmNmdGxiVnnhZoltcXS7IFHzd4F6 NGrGcGExNTFyMECgcm0> NWqxd5hOOjRxNEigbC=> MoLKSG1UVw>? NXzVNIVy\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MWGyOVA{PTl4MR?=
KATO3 NFzWSGZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYSwXVhTOC1zMECwJI5O MXqyOE81QCCq NYLOO5RXTE2VTx?= NXrNRpY6\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NFr3NZIzPTB|NUm2NS=>
SGC7901 MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGixS2UxNTFyMECgcm0> MVGyOE81QCCq M33oc2ROW09? MWTk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MnXaNlUxOzV7NkG=
N87 M3PtdmNmdGxiVnnhZoltcXS7IFHzd4F6 MnniNE0yODByIH7N MnPRNlQwPDhiaB?= Mn76SG1UVw>? NEi5epBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MnzsNlUxOzV7NkG=
HMEC NYjofGhCS2WubDDWbYFjcWyrdImgRZN{[Xl? M3XuclAuOTByMDDuUS=> NF6wSlMzPC92ODDo NELzN2ZFVVOR NUjvWGE1\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MlmzNlUxOzV7NkG=
HUVEC MUTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NInTPXAxNTFyMECgcm0> M2Tlc|I1NzR6IHi= MmDYSG1UVw>? MkTq[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NXHtToZ1OjVyM{W5OlE>
MG63 MmnvSpVv[3Srb36gRZN{[Xl? MoC0OVAuOTByMDDuUS=> NUjSXlY6OC53IHi= M4Py[YRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NVjwbHBKOjR6NECxN|Q>
U2OS  NFP5b5lHfW6ldHnvckBCe3OjeR?= NFnWfXU2OC1zMECwJI5O NIXySGkxNjViaB?= NU\uPWlT\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 MnS1NlQ5PDBzM{S=
Saos-2  M4LyPGZ2dmO2aX;uJGF{e2G7 MkXUOVAuOTByMDDuUS=> NWH1V4NuOC53IHi= Mn;J[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M1nad|I1QDRyMUO0
Saos-2 NYDzOZpPTnWwY4Tpc44hSXO|YYm= NIjDdngyODBibl2= M2TRWFAvPSCq NY[2XnlPeHKndnXueJMhd3O2ZX;zZZJkd22jIHPlcIwhdWmpcnH0bY9v M1PpSVI1QDRyMUO0
MG63 MorkRZBweHSxc3nzJGF{e2G7 Mlf0NVAxKG6P NYXY[XZbOzZiaB?= NF;CdVJxem:vb4Tld{BieG:ydH;zbZM> MXqyOFg1ODF|NB?=
U2OS  MUnBdI9xfG:|aYOgRZN{[Xl? NUnqTlVsOTByIH7N NIqxepk{PiCq MYrwdo9ud3SnczDhdI9xfG:|aYO= MlXaNlQ5PDBzM{S=
Saos-2  Mmj4RZBweHSxc3nzJGF{e2G7 NH3wNnUyODBibl2= MmTsN|YhcA>? NUjuN|N3eHKxbX;0[ZMh[XCxcITvd4l{ MojKNlQ5PDBzM{S=
HT1376 MoGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPpTWM2OD1zLki4JOKyKDFwMTFOwG0> MWKyOFA2PDh5MR?=
T24 NWjiV3JCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXeySZRpUUN3ME2xMlM4KMLzIECuOEDPxE1? MVmyOFA2PDh5MR?=
UM-UC-3 NVW4TpNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDCTWM2OD1yLk[zJOKyOC5zIN88US=> NYThfXZuOjRyNUS4O|E>
DLD-1 M{LRcWNmdGxiVnnhZoltcXS7IFHzd4F6 NH[1eGExNTFyMECgcm0> NHTzXoIzPCCq M2rPOIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUnyRm94OjN7OUGxO|k>
Caco2 NX;vZnRyS2WubDDWbYFjcWyrdImgRZN{[Xl? M{TxeVAuOTByMDDuUS=> NETQV|EzPCCq M{XJR4lvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXWyN|k6OTF5OR?=
HT29 NWDyWog5S2WubDDWbYFjcWyrdImgRZN{[Xl? MVOwMVExODBibl2= MnnpNlQhcA>? NYLQXGZOcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{niOFI{QTlzMUe5
H116 NV3JSY52S2WubDDWbYFjcWyrdImgRZN{[Xl? MYOwMVExODBibl2= MlzkNlQhcA>? NV\KPI13cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1fGOFI{QTlzMUe5
Hct-8 MnLRR4VtdCCYaXHibYxqfHliQYPzZZk> NVf5XotNOC1zMECwJI5O NHXSXFMzPCCq MVvpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1e0ZVI{QTlzMUe5
Colo320 MkC5R4VtdCCYaXHibYxqfHliQYPzZZk> MnP2NE0yODByIH7N MY[yOEBp MnTobY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NH7PR2wzOzl7MUG3PS=>
Sw948 M4\jN2NmdGxiVnnhZoltcXS7IFHzd4F6 M1vpdFAuOTByMDDuUS=> NGK1cHkzPCCq MVjpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlHNNlM6QTFzN{m=
Colo205 MoTZR4VtdCCYaXHibYxqfHliQYPzZZk> Mli2NE0yODByIH7N MlXxNlQhcA>? NX34UFZ1cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1vId|I{QTlzMUe5
Colo320 MXvGeY5kfGmxbjDBd5NigQ>? MkXzNUDPxE1? MV6wMVI1KGh? NV;peGZt[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? M3HGdVI{QTlzMUe5
HT29 NVHkRXJkTnWwY4Tpc44hSXO|YYm= MXOxJO69VQ>? NIT1VmYxNTJ2IHi= MnzkZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> MmD6NlM6QTFzN{m=
Sw948 MmXpSpVv[3Srb36gRZN{[Xl? M3fXcVEh|ryP Ml\wNE0zPCCq MmfzZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> M1jZNVI{QTlzMUe5
DLD-1 NE\GOIJHfW6ldHnvckBCe3OjeR?= MkTuNUDPxE1? MlnUNE0zPCCq MoDDZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> NH;ydFgzOzl7MUG3PS=>
SW620 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn62TWM2OD15Lkig{txO MnK3NlM2PDJzN{i=
SW480 M3\PVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmGzTWM2OD12Lk[g{txO MUeyN|U1OjF5OB?=
SK-CO-1 NFm0W21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj4TWM2OD12IN88US=> M3nIOVI{PTR{MUe4
LS-513 Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r4NGlEPTB;Mz65JO69VQ>? MnLkNlM2PDJzN{i=
SW1116 NHLnZVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXSy[W9kUUN3ME2wMlg1KM7:TR?= M1jMd|I{PTR{MUe4
LS-174T NW\3PZluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwOESg{txO M1fNVlI{PTR{MUe4
HCT 116 M1T1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnWbI93UUN3ME2wMlQyKM7:TR?= M1exblI{PTR{MUe4
HCT 15 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7QTWM2OD1yLkOg{txO Mn3xNlM2PDJzN{i=
COLO 205 M1zoNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwMkSg{txO NY\QU4lUOjN3NEKxO|g>
HT-29 NILBR4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTBwMkOg{txO NEnqcZQzOzV2MkG3PC=>
COLO 201 NHe2S4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwMkOg{txO NUCwPHpWOjN3NEKxO|g>
Caco-2 NYXYSlI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfOeXlKSzVyPUCuNlIh|ryP MX6yN|U1OjF5OB?=
SW48 M{flZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITJV5RKSzVyPUCuNFkh|ryP NYnWSpJMOjN3NEKxO|g>
DND-1 NEH0eVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDoNE4zPS9yLkWvNUDPxE1? NXTBRpZXTE2VTx?= M4HwfIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NHvFdZEzOzR6Mke0PC=>
TMD8 NVLTUplPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jQVVAvOjVxMD61M|Eh|ryP MmT6SG1UVw>? NIjVXopqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MV:yN|Q5Ojd2OB?=
Jurkat MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXZZmkxNjJ3L{CuOU8yKM7:TR?= MnvGSG1UVw>? M{LVVIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NWKzd3FGOjN2OEK3OFg>
KOPT-K1 M4n0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHLco1nOC5{NT:wMlUwOSEQvF2= NYDMUGhFTE2VTx?= M1jUV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MmXLNlM1QDJ5NEi=
TMD7 NX\6O45xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zI[VAvOjVxMD61M|Eh|ryP M4HMOGROW09? M2O4NolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MX:yN|Q5Ojd2OB?=
THP-1 NVf0XlFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjZPI1VOC5{NT:wMlUwOSEQvF2= MVfEUXNQ NXuy[Hk5cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MnezNlM1QDJ5NEi=
786-O NWTnfXh5TnWwY4Tpc44hSXO|YYm= NXnDWnF1OC5zL{CuOUDPxE1? MUOyOEBp NX;pVowzTE2VTx?= Mn;SbY5kemWjc3XzJGUu[2GmaHXybY4hdVKQQTDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgQ>? MV:yN|E1PzJ3MR?=
786-O MXjGeY5kfGmxbjDBd5NigQ>? M3;zUlAuOC53IN88US=> NYLIdm1sOjRiaB?= MY\EUXNQ NFXOTHFz\XO3bITzJIlvKGFiZH;z[UBl\XCnbnTlcpQhcW6lcnXhd4UhcW5iRT3jZYRp\XKrbjDwdo91\WmwIHX4dJJme3Orb39CpC=> MnTGNlMyPDd{NUG=
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Jurkat NIPUbVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoezOFAxdk1? MojlNlQwPDhiaB?= M1jaR5N6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= MUOyNlU3PjZyNB?=
p210 BCR-Abl MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILaRms1ODCwTR?= NF\3b2YzPC92ODDo M{TJcpN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= NFO4clUzOjV4Nk[wOC=>
8226 MWjGeY5kfGmxbjDBd5NigQ>? NEDvfWkyODBvMUCwNEBvVQ>? M3zONVMxKG2rbh?= NUHwZYFGTE2VTx?= NIDYVG1i[3SrdnH0[ZMhTVKNwrC= MW[yNlU2PjRyOR?=
MM1.S  MkfESpVv[3Srb36gRZN{[Xl? Mk\ENVAxNTFyMECgcm0> NWSyfVZ7OzBibXnu NGX4PYNFVVOR Mof4ZYN1cX[jdHXzJGVTU8Li MYqyNlU2PjRyOR?=
8226 Ml;KSpVv[3Srb36gRZN{[Xl? NF;xTm0xNjVizszN NE\qbZY{OCCvaX6= MYHEUXNQ NVfCcnducW6mdXPld{Bi[3SrdnH0bY9vKG:oIGLBSkBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIF3FTy=> NGH0fWMzOjV3NkSwPS=>
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MCF-7 NX\6[ZlJTnWwY4Tpc44hSXO|YYm= M{\SXVUxNzJyMD:1NFAhdk1? NWTYeYVCOzBibXnu M1:2S4Rwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 NEC2c3czOjR5Nki1Ni=>
T47D M1qzeGZ2dmO2aX;uJGF{e2G7 M{PnNFUxNzJyMD:1NFAhdk1? NH;pc4k{OCCvaX6= MV;kc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MlHRNlI1PzZ6NUK=
MDA-MB-231 NX:zWXBkTnWwY4Tpc44hSXO|YYm= NULCUVB3PTBxMkCwM|UxOCCwTR?= MmLsN|AhdWmw M1[ySoRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 M{XHXFIzPDd4OEWy
Bcap-37 NILBSG9HfW6ldHnvckBCe3OjeR?= M332T|UxNzJyMD:1NFAhdk1? MoHPN|AhdWmw M2[xPYRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 NYO4fpgxOjJ2N{[4OVI>
MCF-7 MYXBdI9xfG:|aYOgRZN{[Xl? M{G0OVIxOMLibl2= MWGzOkBp MlLCSG1UVw>? NG\sVZRqdmS3Y3XzJIFxd3C2b4Ppdy=> Mo[5NlI1PzZ6NUK=
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Bcap-37 MXzBdI9xfG:|aYOgRZN{[Xl? M1jye|IxOMLibl2= MkH3N|YhcA>? NFLKfWhFVVOR MkfJbY5lfWOnczDhdI9xfG:|aYO= MnrQNlI1PzZ6NUK=
LS174T NH3FfnhHfW6ldHnvckBCe3OjeR?= MWSxNE8yODBxMUCwNEBvVQ>? MnnmOkBp MUTEUXNQ NXLDZnpQcW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? NEntWo0zOjRyMUK5OC=>
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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