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 MnfLSpVv[3Srb36gRZN{[Xl? MVu1NE0yOjVyIH7N MnrxNlQhcA>? M1jJOGROW09? MULpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Yhc2mwYYPlJEh1[XKpZYSgc4YhdVSRUlOxLUBidmRiaYTzJIRwf26|dILlZY0hfGG{Z3X0JJBpd3OyaH:tV|bDqA>? MojSNlYyPzdyNUG=
U87vIII  NXLYUGJtTnWwY4Tpc44hSXO|YYm= Ml\5NE4xPC1{LkWg{txO M1nYZlI1KGh? MXfpcohq[mm2czDtWG9TSzFiYX7kJI1VV1KFMjDhZ5Rqfmm2aXXzxsA> Ml7KNlYyOzR4MUe=
U87vIII  NYHVNVJlTnWwY4Tpc44hSXO|YYm= MknQNk42NzVizszN M1XuPVEzKGh? M17RZ4lvcGmkaYTzJIdieCClbH;zbY5oKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoXDNlYyOzR4MUe=
PC12  NHXxNopHfW6ldHnvckBCe3OjeR?= NVr0OndSPDEEoH7N Mm\ZbY5lfWOnczDsfZNwe2:vYXygZolw\2WwZYPpd{BidmRiYXzs[ZZq[XSnZDFOtU1UYU5iYXPjeY12dGG2aX;uxsA> MXKyOlAxOTZzNB?=
3T3-L1 MYnGeY5kfGmxbjDBd5NigQ>? MV2xOUDPxE1? NFexSHo1KGh? NI\jTFB{fXCycnXzd4V{KGW6cILld5Nqd25ib3[geIhmKEWpckGgdJJwfGWrbtMg MV:yOVgyPDZ4Mh?=
Rh30 NGPwcWVHfW6ldHnvckBCe3OjeR?= NF7US44yKM7:TR?= NEfPc4MzKGh? MlqwbY5pcWKrdIOgZo91cCCvVF;SR|EudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKFN4S{GgZY5lKG2WT2LDNk1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhSWu2 NF3XcY0zPTd4Mk[xPS=>
HT29 MkO3SpVv[3Srb36gRZN{[Xl? NUC1[Xc3OSEQvF2= MkK5NkBp M17sOIlvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= Mk\VNlU4PjJ4MUm=
Rh30 MnfHSpVv[3Srb36gRZN{[Xl? NVTLZ|lLOSEQvF2= MVGyJIg> MWjzeZBxemW|c3XzJJRp\SCkYYPhcEBweiCLR1[tNU1{fGmvdXzheIVlKGOnbHygZYRp\XOrb36= MWiyOVc3OjZzOR?=
HT29 NVn4emxFTnWwY4Tpc44hSXO|YYm= MVyxJO69VQ>? NYPTWJFqOiCq MVHzeZBxemW|c3XzJJRp\SCkYYPhcEBweiCLR1[tNU1{fGmvdXzheIVlKGOnbHygZYRp\XOrb36= NHrqc5EzPTd4Mk[xPS=>
U87 NXrs[|lkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4m2PFI2KG6P NX3sWm5QOjRiaB?= MlvpbY5kemWjc3XzJGRWW1BzMDDrco9kc2WmLXTve44hcW6mdXPl[EBk\WyuIHnubIljcXSrb36= MlT1NlU2Pjh4NkW=
AGS NVPHZm1vS2WubDDWbYFjcWyrdImgRZN{[Xl? M4rRdFAuOTByMDDuUS=> M{n5SVI1NzR6IHi= NULJZ4FpTE2VTx?= NWD6c4V5\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MoDxNlUxOzV7NkG=
MKN45 NH7x[mxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYGzXFY1OC1zMECwJI5O M3L0UFI1NzR6IHi= Mlr3SG1UVw>? NGG5fJBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MkfCNlUxOzV7NkG=
MKN28 Ml36R4VtdCCYaXHibYxqfHliQYPzZZk> MWKwMVExODBibl2= MV6yOE81QCCq NH\Jc3pFVVOR MnH1[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MnXzNlUxOzV7NkG=
KATO3 NFHMc3JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M173e|AuOTByMDDuUS=> MV[yOE81QCCq MY\EUXNQ M1LlWIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M4rM[FI2ODN3OU[x
SGC7901 M4jjUGNmdGxiVnnhZoltcXS7IFHzd4F6 NV;5[ndHOC1zMECwJI5O Mny1NlQwPDhiaB?= NH7ZOopFVVOR MVHk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M3T0R|I2ODN3OU[x
N87 MmXBR4VtdCCYaXHibYxqfHliQYPzZZk> M{e2NlAuOTByMDDuUS=> M2LpVVI1NzR6IHi= MYfEUXNQ NWLQW|hW\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NEfifYkzPTB|NUm2NS=>
HMEC MlzQR4VtdCCYaXHibYxqfHliQYPzZZk> NFjCWpUxNTFyMECgcm0> M4PHOFI1NzR6IHi= NVnBOI1UTE2VTx?= MnLl[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NGjweWQzPTB|NUm2NS=>
HUVEC MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVe3RVU5OC1zMECwJI5O NGO1c5kzPC92ODDo MoXXSG1UVw>? NEe2NI1l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MXWyOVA{PTl4MR?=
MG63 M3Xh[2Z2dmO2aX;uJGF{e2G7 MkL1OVAuOTByMDDuUS=> M3;0elAvPSCq NXeycW44\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 NX;ufGZOOjR6NECxN|Q>
U2OS  NUHxS5pZTnWwY4Tpc44hSXO|YYm= NX60eZE4PTBvMUCwNEBvVQ>? M{DCPFAvPSCq NV7ERXM4\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 MVKyOFg1ODF|NB?=
Saos-2  NGTjVWRHfW6ldHnvckBCe3OjeR?= NX\i[pdnPTBvMUCwNEBvVQ>? MYmwMlUhcA>? MV;kc5NmKGSncHXu[IVvfGy7IDi1NQKBmzFyMECgcm0qKGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= NEi1SZMzPDh2MEGzOC=>
Saos-2 NVX3cFZ6TnWwY4Tpc44hSXO|YYm= MXuxNFAhdk1? MVmwMlUhcA>? MYDwdoV3\W62czDvd5Rmd3OjcnPvcYEh[2WubDDtbYdz[XSrb36= M{PPRVI1QDRyMUO0
MG63 NX7ROYttSXCxcITvd4l{KEG|c3H5 M4L1S|ExOCCwTR?= MoDzN|YhcA>? M3PKUJBzd22xdHXzJIFxd3C2b4Ppdy=> NFzIR28zPDh2MEGzOC=>
U2OS  M1vLeWFxd3C2b4Ppd{BCe3OjeR?= NES3NHcyODBibl2= NEXjTWg{PiCq NWnTRmpSeHKxbX;0[ZMh[XCxcITvd4l{ Mn7VNlQ5PDBzM{S=
Saos-2  MojhRZBweHSxc3nzJGF{e2G7 NVrvTFZxOTByIH7N MmC0N|YhcA>? NILHRVdxem:vb4Tld{BieG:ydH;zbZM> M2[wWFI1QDRyMUO0
HT1376 NG\Bd3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDNPXFKSzVyPUGuPFghyrFiMT6xJO69VQ>? M2XaVVI1ODV2OEex
T24 NFn2PXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17DPWlEPTB;MT6zO{DDuSByLkSg{txO M13mPVI1ODV2OEex
UM-UC-3 NVXSXpBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnX6TWM2OD1yLk[zJOKyOC5zIN88US=> M{Lsd|I1ODV2OEex
DLD-1 NGHPRYJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1zYSlAuOTByMDDuUS=> NHW3V5kzPCCq NWfHZ2I4cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{\H[FI{QTlzMUe5
Caco2 Mn;NR4VtdCCYaXHibYxqfHliQYPzZZk> MnXRNE0yODByIH7N MVqyOEBp MkTUbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUSyN|k6OTF5OR?=
HT29 MYTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2rzT|AuOTByMDDuUS=> M3;XdFI1KGh? NWjlOWI{cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnvMNlM6QTFzN{m=
H116 NEXKWGxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3jIfVAuOTByMDDuUS=> MoTENlQhcA>? M{PENIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MX:yN|k6OTF5OR?=
Hct-8 NVLS[XR[S2WubDDWbYFjcWyrdImgRZN{[Xl? M3zROlAuOTByMDDuUS=> NYL4NXozOjRiaB?= NWjkeoI{cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NX3DNFZHOjN7OUGxO|k>
Colo320 M2W1b2NmdGxiVnnhZoltcXS7IFHzd4F6 MWmwMVExODBibl2= NWryXFRJOjRiaB?= NFLS[npqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MV[yN|k6OTF5OR?=
Sw948 M4GyVmNmdGxiVnnhZoltcXS7IFHzd4F6 MonpNE0yODByIH7N MlPONlQhcA>? M3fQc4lvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYKyN|k6OTF5OR?=
Colo205 NYXLPFhQS2WubDDWbYFjcWyrdImgRZN{[Xl? MV:wMVExODBibl2= NWXNXJQ5OjRiaB?= NIfIdlFqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUPSNGNmOjN7OUGxO|k>
Colo320 MUTGeY5kfGmxbjDBd5NigQ>? MnPVNUDPxE1? NV3IR4lSOC1{NDDo NI\6Smti[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 NV;pOJBZOjN7OUGxO|k>
HT29 M{XzfWZ2dmO2aX;uJGF{e2G7 NWPkcGRbOSEQvF2= MViwMVI1KGh? NV[xWm81[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? Mo\SNlM6QTFzN{m=
Sw948 MXjGeY5kfGmxbjDBd5NigQ>? NUP1fnRqOSEQvF2= MYGwMVI1KGh? Mn35ZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> M1LpSVI{QTlzMUe5
DLD-1 MlXtSpVv[3Srb36gRZN{[Xl? NF\p[5AyKM7:TR?= M4LTVFAuOjRiaB?= M2nqSIFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> NWG2OYVMOjN7OUGxO|k>
SW620 NF;QcoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfMd2NKSzVyPUeuPEDPxE1? MXSyN|U1OjF5OB?=
SW480 NEDFWXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\yTWM2OD12Lk[g{txO NF;4TnIzOzV2MkG3PC=>
SK-CO-1 NFr3fmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTRizszN Mmi2NlM2PDJzN{i=
LS-513 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmxV|FKSzVyPUOuPUDPxE1? NVfzcpMyOjN3NEKxO|g>
SW1116 Mn76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LuNGlEPTB;MD64OEDPxE1? MYeyN|U1OjF5OB?=
LS-174T NYHz[WNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfuOopKSzVyPUCuPFQh|ryP MWeyN|U1OjF5OB?=
HCT 116 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXBTWM2OD1yLkSxJO69VQ>? M1vzXVI{PTR{MUe4
HCT 15 NXPGZ2I6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHuPY5KSzVyPUCuN{DPxE1? NX25VVAzOjN3NEKxO|g>
COLO 205 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwMkSg{txO MUWyN|U1OjF5OB?=
HT-29 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTBwMkOg{txO MojTNlM2PDJzN{i=
COLO 201 NWi5XGFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH2XnlKSzVyPUCuNlMh|ryP M2joelI{PTR{MUe4
Caco-2 NWrQOG0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P0VmlEPTB;MD6yNkDPxE1? M2O4WlI{PTR{MUe4
SW48 NUK3OllLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[zOWlEPTB;MD6wPUDPxE1? NVK0fVZSOjN3NEKxO|g>
DND-1 NXvhXJc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:wMlI2NzBwNT:xJO69VQ>? MnXWSG1UVw>? MWLpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M4XX[VI{PDh{N{S4
TMD8 NHW3OGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfl[lgxNjJ3L{CuOU8yKM7:TR?= M{XVR2ROW09? MWTpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 Mn7WNlM1QDJ5NEi=
Jurkat M2\Yd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13IOlAvOjVxMD61M|Eh|ryP M{D3VmROW09? NYjrNIRucW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NF3NT44zOzR6Mke0PC=>
KOPT-K1 M1LMSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnX5NE4zPS9yLkWvNUDPxE1? M3rtZWROW09? MnS1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Mlf3NlM1QDJ5NEi=
TMD7 MmHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vVflAvOjVxMD61M|Eh|ryP NWHkNZZYTE2VTx?= NWS0[Hh5cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NV\jVGlYOjN2OEK3OFg>
THP-1 MoTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUL6N4pIOC5{NT:wMlUwOSEQvF2= NVTFXHlGTE2VTx?= NWfOfIRZcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MorPNlM1QDJ5NEi=
786-O MXzGeY5kfGmxbjDBd5NigQ>? NFfGeGkxNjFxMD61JO69VQ>? MnX0NlQhcA>? NFW2dJBFVVOR NIrNXYRqdmO{ZXHz[ZMhTS2lYXTo[ZJqdiCvUl7BJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7 NUT2RpdUOjNzNEeyOVE>
786-O NG[wW25HfW6ldHnvckBCe3OjeR?= M{HZTlAuOC53IN88US=> MVuyOEBp NH3IbVdFVVOR MV7y[ZN2dHS|IHnuJIEh\G:|ZTDk[ZBmdmSnboSgbY5kemWjc3WgbY4hTS2lYXTo[ZJqdiCycn;0[YlvKGW6cILld5Nqd28EoB?= M1XHPFI{OTR5MkWx
OCI-AML3 M{DkdGFxd3C2b4Ppd{BCe3OjeR?= NGrBOmMzNjVizszN MnnoO|IhcA>? Mly2bY5lfWOnczDhdI9xfG:|aYO= NYHaVYpROjJ6Mk[1OlU>
Jurkat MnG1SpVv[3Srb36gRZN{[Xl? NYjEU25vOTByL{KwNE81ODBibl2= NWH1eZBiOThiaB?= NGr0dGhqdmirYnn0d{BuXE:UQ{Gt[IVx\W6mZX70JHM3KFN{M{WvNlM3KHCqb4PwbI9zgWyjdHnvci=> MYGyNlU3PjZyNB?=
p210 BCR-Abl MV;GeY5kfGmxbjDBd5NigQ>? NFnt[lIyODBxMkCwM|QxOCCwTR?= M{jPPFE5KGh? NUHyRmlZcW6qaXLpeJMhdVSRUlOxMYRmeGWwZHXueEBUPiCVMkO1M|I{PiCyaH;zdIhwenmuYYTpc44> M1fTe|IzPTZ4NkC0
Jurkat NVTPdJBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrPdWpjPDBybl2= M4nxc|I1NzR6IHi= NGThTFZ{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u MYmyNlU3PjZyNB?=
p210 BCR-Abl MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWK0NFBvVQ>? M4XQd|I1NzR6IHi= MYTzfY5memerenWge4l1cCBzNz3BRWchfG9ic4XwdJJme3NiY3XscEBxem:uaX\ldoF1cW:w MUSyNlU3PjZyNB?=
8226 NELMdopHfW6ldHnvckBCe3OjeR?= NVPleotrOTByLUGwNFAhdk1? MYCzNEBucW5? NWjNVYdtTE2VTx?= NVLWNm1S[WO2aY\heIV{KEWUS9Mg M2H5[FIzPTV4NEC5
MM1.S  MYDGeY5kfGmxbjDBd5NigQ>? NGruN5UyODBvMUCwNEBvVQ>? MWWzNEBucW5? NY\NU2JXTE2VTx?= MWDhZ5RqfmG2ZYOgSXJMyqB? NH\vVXYzOjV3NkSwPS=>
8226 MlnESpVv[3Srb36gRZN{[Xl? NXTNd5FnOC53IN88US=> NHrDNXY{OCCvaX6= M2rSfGROW09? M1zjV4lv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= NWrtdWRxOjJ3NU[0NFk>
MM1.S  NELWUXNHfW6ldHnvckBCe3OjeR?= NELvSlkxNjVizszN NIHIeIc{OCCvaX6= M17GUWROW09? NG\kUFhqdmS3Y3XzJIFkfGm4YYTpc44hd2ZiUlHGJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiTVXL MWKyNlU2PjRyOR?=
MCF-7 NUfFNoo2TnWwY4Tpc44hSXO|YYm= M4Cwb|UxNzJyMD:1NFAhdk1? NY\xUYZ6OzBibXnu MV\kc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MWWyNlQ4Pjh3Mh?=
T47D MYLGeY5kfGmxbjDBd5NigQ>? M2PzO|UxNzJyMD:1NFAhdk1? MWOzNEBucW5? NEewdWtld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? MofJNlI1PzZ6NUK=
MDA-MB-231 MVvGeY5kfGmxbjDBd5NigQ>? MUi1NE8zODBxNUCwJI5O NWL2SlNFOzBibXnu NWT4UWJE\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MkTNNlI1PzZ6NUK=
Bcap-37 MnXSSpVv[3Srb36gRZN{[Xl? M4nFW|UxNzJyMD:1NFAhdk1? NITTVWc{OCCvaX6= NYjncXdK\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? NHXBXmgzOjR5Nki1Ni=>
MCF-7 MlnxRZBweHSxc3nzJGF{e2G7 MorNNlAxyqCwTR?= M4\ZOFM3KGh? NGTUPJRFVVOR Ml;FbY5lfWOnczDhdI9xfG:|aYO= NVnQVGpkOjJ2N{[4OVI>
MDA-MB-231 M4P5e2Fxd3C2b4Ppd{BCe3OjeR?= M3j2TlIxOMLibl2= M2\j[|M3KGh? NYnpXFJrTE2VTx?= M3vGT4lv\HWlZYOgZZBweHSxc3nz NWX1PHNXOjJ2N{[4OVI>
Bcap-37 MoXhRZBweHSxc3nzJGF{e2G7 M4HiRVIxOMLibl2= NGLyfI4{PiCq NIr2O|hFVVOR NUfsc4J1cW6mdXPld{BieG:ydH;zbZM> MmrxNlI1PzZ6NUK=
LS174T MnHmSpVv[3Srb36gRZN{[Xl? MW[xNE8yODBxMUCwNEBvVQ>? NXPCSVM5PiCq NX7qSIJrTE2VTx?= MoLLbY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> NYfOSnRlOjJ2MEGyPVQ>
DLD-1  NV32XGtrTnWwY4Tpc44hSXO|YYm= MXqxNE8yODBxMUCwNEBvVQ>? MoTIOkBp MYXEUXNQ MnHibY5pcWKrdIOgcXRQWkNzIHHjeIl3cXS7IHL5JJRp\SCmZYDoc5NxcG:{eXzheIlwdiCxZjDTOkBzcWKxc3;tZYwheHKxdHXpci=> Mk\wNlI1ODF{OUS=
SW480 NIHQSXhHfW6ldHnvckBCe3OjeR?= MYOxNE8yODBxMUCwNEBvVQ>? M4KyWFYhcA>? NFTEcmxFVVOR NFrN[mVqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv M4rEN|IzPDBzMkm0
SW-48 NInhUXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi1XJlKSzVyPUCuNUDPxE1? MoDsNlIzPzB{NUe=
HCT-15 NF3sNnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnn1TWM2OD1yLkOg{txO MUmyNlI4ODJ3Nx?=
HCT 116 Ml;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r0N2lEPTB;MD62JO69VQ>? MVeyNlI4ODJ3Nx?=
SW620-R MkDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XwNWlEPTB;MT6zJO69VQ>? M33iVFIzOjdyMkW3
SK-CO-1 MkSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\QPHZlUUN3ME2yMlEh|ryP MVuyNlI4ODJ3Nx?=
SW620 M4LuV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPtXWxtUUN3ME2xNUDPxE1? NVXuRWVYOjJ{N{CyOVc>
BaF3 NHjxUolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\0WmdKPTB;MT60OFkh|ryP NGHwcXozOjJ{M{[0OS=>
NIH 3T3 NVjCbIFZTnWwY4Tpc44hSXO|YYm= MYmyJO69VQ>? M{XTXFE5KGh? NXLmS|BCcW6qaXLpeJMhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3Rib36gV4VzPDd|IHHu[EBuXE:UQ{GgdIhwe3Cqb4L5cIF1cW:wIH;mJFRGNUKSMTDvckBVcHJ|Nz:0Oi=> MmTDNlE5PzZzM{C=
HCT15 MUPGeY5kfGmxbjDBd5NigQ>? NEPDPWMxNjVxMjFOwG0> Mlv0OEBp NXficZY4eHKndnXueJMhWz[NMTDwbI9{eGixconsZZRqd25ib3[gdoljd3OxbXHsJJBzd3SnaX6gV|Yh[XRiU3XyNlQxNzJ2NDDhcoQhdVSRUlOyJJBpd3OyaH;yfYxifGmxbjDv[kBCc3RiYYSgV4VzPDd| NHnTW3gzOTh5NkGzNC=>
SW620  NViwNXJITnWwY4Tpc44hSXO|YYm= MonPNE42NzJizszN MV60JIg> NVT6Vmht[myxY3vzJIFtdCC2aILl[UBuXE:UIH;1eJB2fHN? MV2yNVg4PjF|MB?=

... 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