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 NUTaWHNzTnWwY4Tpc44hSXO|YYm= M1TicVUxNTF{NUCgcm0> MnvDNlQhcA>? NGDJT5NFVVOR M3vwZolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPiCtaX7hd4UhMHSjcnfleEBw\iCvVF;SR|EqKGGwZDDpeJMh\G:5boP0doVidSC2YYLn[ZQheGixc4Doc{1UPsLi MYeyOlE4PzB3MR?=
U87vIII  Mnu0SpVv[3Srb36gRZN{[Xl? M1[2TVAvODRvMj61JO69VQ>? NILvWngzPCCq MULpcohq[mm2czDtWG9TSzFiYX7kJI1VV1KFMjDhZ5Rqfmm2aXXzxsA> MnT5NlYyOzR4MUe=
U87vIII  NYLRVpBJTnWwY4Tpc44hSXO|YYm= NVTx[mlKOi53L{Wg{txO NEPsVXQyOiCq NELXNlNqdmirYnn0d{Bo[XBiY3zvd4lv\yCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NV;iXFlNOjZzM{S2NVc>
PC12  MWrGeY5kfGmxbjDBd5NigQ>? M4DLelQxyqCwTR?= MlfLbY5lfWOnczDsfZNwe2:vYXygZolw\2WwZYPpd{BidmRiYXzs[ZZq[XSnZDFOtU1UYU5iYXPjeY12dGG2aX;uxsA> MkDoNlYxODF4MUS=
3T3-L1 NIL1[4xHfW6ldHnvckBCe3OjeR?= NGfVV5QyPSEQvF2= NHXyU2k1KGh? M1rte5N2eHC{ZYPz[ZMh\XiycnXzd4lwdiCxZjD0bIUhTWe{MTDwdo91\WmwwrC= MVKyOVgyPDZ4Mh?=
Rh30 NFv4e|VHfW6ldHnvckBCe3OjeR?= M4q2e|Eh|ryP MXGyJIg> MXjpcohq[mm2czDic5RpKG2WT2LDNU1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhWz[NMTDhcoQhdVSRUlOyMY1m\GmjdHXkJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MXeyOVc3OjZzOR?=
HT29 NEiyd4tHfW6ldHnvckBCe3OjeR?= NV;nTHJsOSEQvF2= Mn7mNkBp M1;6VIlvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= NHTLRXgzPTd4Mk[xPS=>
Rh30 NYrrc2VQTnWwY4Tpc44hSXO|YYm= NE\OfZoyKM7:TR?= NXXyWFlLOiCq NIeyWVN{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> NI\ESXEzPTd4Mk[xPS=>
HT29 M2\pVWZ2dmO2aX;uJGF{e2G7 NFvK[W8yKM7:TR?= MVGyJIg> MoDZd5VxeHKnc4Pld{B1cGViYnHzZYwhd3JiSVfGMVEue3SrbYXsZZRm\CClZXzsJIFlcGW|aX;u M1XtfVI2PzZ{NkG5
U87 M3;tXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCyOUBvVQ>? MVmyOEBp NITRPGhqdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> MYiyOVU3QDZ4NR?=
AGS NW\NbWo5S2WubDDWbYFjcWyrdImgRZN{[Xl? MXSwMVExODBibl2= Mm\WNlQwPDhiaB?= M{Lze2ROW09? NUHmUIoy\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NWHMbpVYOjVyM{W5OlE>
MKN45 MlO0R4VtdCCYaXHibYxqfHliQYPzZZk> M1roblAuOTByMDDuUS=> NUnmNItCOjRxNEigbC=> M4HtZWROW09? NHnXd4Nl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NEnxdY8zPTB|NUm2NS=>
MKN28 M4HaW2NmdGxiVnnhZoltcXS7IFHzd4F6 M37pb|AuOTByMDDuUS=> M{PZW|I1NzR6IHi= NWTBVFBXTE2VTx?= NHTPR2Nl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MX2yOVA{PTl4MR?=
KATO3 MnHsR4VtdCCYaXHibYxqfHliQYPzZZk> MV6wMVExODBibl2= M{XqVlI1NzR6IHi= M1\5OmROW09? MnzI[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NWPDbYRYOjVyM{W5OlE>
SGC7901 M4nnWWNmdGxiVnnhZoltcXS7IFHzd4F6 M3rSO|AuOTByMDDuUS=> MW[yOE81QCCq MYLEUXNQ M{XOWYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXGyOVA{PTl4MR?=
N87 M{Xkc2NmdGxiVnnhZoltcXS7IFHzd4F6 MXSwMVExODBibl2= M4j0VVI1NzR6IHi= NGP2N|lFVVOR MkX4[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mn6yNlUxOzV7NkG=
HMEC NGPHfG9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFzWXHExNTFyMECgcm0> NXL4[nJjOjRxNEigbC=> NXfhUGc2TE2VTx?= M4HFdYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MWCyOVA{PTl4MR?=
HUVEC MnHCR4VtdCCYaXHibYxqfHliQYPzZZk> NIr0OI0xNTFyMECgcm0> M2C3ZVI1NzR6IHi= M3rPZWROW09? M1z5PIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MUOyOVA{PTl4MR?=
MG63 NUXFVHdSTnWwY4Tpc44hSXO|YYm= MmXPOVAuOTByMDDuUS=> MVKwMlUhcA>? MmXH[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M1fZU|I1QDRyMUO0
U2OS  NWS3ZXExTnWwY4Tpc44hSXO|YYm= M1fIZlUxNTFyMECgcm0> MXywMlUhcA>? Mojq[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M3;ESVI1QDRyMUO0
Saos-2  NGHkR4NHfW6ldHnvckBCe3OjeR?= MUO1NE0yODByIH7N MVuwMlUhcA>? MkLr[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NF\mV5MzPDh2MEGzOC=>
Saos-2 NVvKcW9wTnWwY4Tpc44hSXO|YYm= NUPGVYJVOTByIH7N NF7mNHMxNjViaB?= NIDjNWJxemW4ZX70d{Bwe3Snb4PhdoNwdWFiY3XscEBucWe{YYTpc44> MVSyOFg1ODF|NB?=
MG63 MWnBdI9xfG:|aYOgRZN{[Xl? MV:xNFAhdk1? NVzDcFhPOzZiaB?= MWPwdo9ud3SnczDhdI9xfG:|aYO= M3X1PFI1QDRyMUO0
U2OS  MlfZRZBweHSxc3nzJGF{e2G7 MXmxNFAhdk1? MlzKN|YhcA>? M{C5b5Bzd22xdHXzJIFxd3C2b4Ppdy=> NF3OVmEzPDh2MEGzOC=>
Saos-2  Mn3qRZBweHSxc3nzJGF{e2G7 MnjFNVAxKG6P NWr0elNNOzZiaB?= NUPj[XJ3eHKxbX;0[ZMh[XCxcITvd4l{ M1zzfFI1QDRyMUO0
HT1376 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLlbHJKSzVyPUGuPFghyrFiMT6xJO69VQ>? NFXpUVMzPDB3NEi3NS=>
T24 NXfxSo9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFwM{egxtEhOC52IN88US=> NFHoXmQzPDB3NEi3NS=>
UM-UC-3 M3jvNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNkOgxtExNjFizszN MX[yOFA2PDh5MR?=
DLD-1 MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlTBNE0yODByIH7N NVPRd4xGOjRiaB?= MW\pcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NHnL[IUzOzl7MUG3PS=>
Caco2 M{XCSWNmdGxiVnnhZoltcXS7IFHzd4F6 NXfFWGFOOC1zMECwJI5O NYfjXVZ3OjRiaB?= M3vENYlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWfaTmhtOjN7OUGxO|k>
HT29 MnTFR4VtdCCYaXHibYxqfHliQYPzZZk> M3zkVFAuOTByMDDuUS=> Ml3kNlQhcA>? NXv6Vog1cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYSyN|k6OTF5OR?=
H116 MUTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUnqRpd6OC1zMECwJI5O NYW5doZmOjRiaB?= M4nHZYlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUWyN|k6OTF5OR?=
Hct-8 MoPTR4VtdCCYaXHibYxqfHliQYPzZZk> MXOwMVExODBibl2= NFHEXHQzPCCq MkXwbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{fzTFI{QTlzMUe5
Colo320 NGHTbopE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVLCOpFvOC1zMECwJI5O MYCyOEBp NITzZoZqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1\nVVI{QTlzMUe5
Sw948 M4HHNGNmdGxiVnnhZoltcXS7IFHzd4F6 NV\WcWFDOC1zMECwJI5O MnzzNlQhcA>? MULpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NUnISmJjOjN7OUGxO|k>
Colo205 MoPvR4VtdCCYaXHibYxqfHliQYPzZZk> NVS2T4J7OC1zMECwJI5O NEH6T28zPCCq NV\uO5lOcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NU\ERmd4OjN7OUGxO|k>
Colo320 M3P2cGZ2dmO2aX;uJGF{e2G7 NH7NeY0yKM7:TR?= MonDNE0zPCCq NFHrfnli[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 NIeyNY4zOzl7MUG3PS=>
HT29 NVnVbFZPTnWwY4Tpc44hSXO|YYm= Mm\ONUDPxE1? NWTKUmZPOC1{NDDo NYj6TnVx[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MoPzNlM6QTFzN{m=
Sw948 M2XrXWZ2dmO2aX;uJGF{e2G7 NXHXeZpzOSEQvF2= Mlu0NE0zPCCq Mm\PZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> NIrPTpUzOzl7MUG3PS=>
DLD-1 Mm\tSpVv[3Srb36gRZN{[Xl? NXvnRWZFOSEQvF2= NIrSSZoxNTJ2IHi= M37ZboFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> M{O5eFI{QTlzMUe5
SW620 MmDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTYTWM2OD15Lkig{txO M1XlcFI{PTR{MUe4
SW480 M1r2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTRwNjFOwG0> MWCyN|U1OjF5OB?=
SK-CO-1 NV7q[2M1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILwVWVKSzVyPUSg{txO MWWyN|U1OjF5OB?=
LS-513 MlfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTISmtFUUN3ME2zMlkh|ryP NI\nSYQzOzV2MkG3PC=>
SW1116 NX;Rc|FWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvUN5RKSzVyPUCuPFQh|ryP NGjZdI4zOzV2MkG3PC=>
LS-174T NWPzSINpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzzPZhKSzVyPUCuPFQh|ryP NIL2Z3czOzV2MkG3PC=>
HCT 116 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvtfHhHUUN3ME2wMlQyKM7:TR?= MUOyN|U1OjF5OB?=
HCT 15 MmC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTWc5RKSzVyPUCuN{DPxE1? NYnUcId4OjN3NEKxO|g>
COLO 205 NGnBPXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfMTWM2OD1yLkK0JO69VQ>? NEe5eoYzOzV2MkG3PC=>
HT-29 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDzS4tKSzVyPUCuNlMh|ryP MWmyN|U1OjF5OB?=
COLO 201 NGLWOo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzSW5dKSzVyPUCuNlMh|ryP NEfUTGkzOzV2MkG3PC=>
Caco-2 Mmr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmGyTWM2OD1yLkKyJO69VQ>? MoPrNlM2PDJzN{i=
SW48 MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwMEmg{txO M1LHflI{PTR{MUe4
DND-1 M{PUWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnGNE4zPS9yLkWvNUDPxE1? MYHEUXNQ MlPybY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Mlz3NlM1QDJ5NEi=
TMD8 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvqTWsxNjJ3L{CuOU8yKM7:TR?= NGX6fXlFVVOR NGDGVWJqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NVnVXVRsOjN2OEK3OFg>
Jurkat NW\tU5RxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETGdGwxNjJ3L{CuOU8yKM7:TR?= M2\ZTWROW09? M{HWVIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MnHrNlM1QDJ5NEi=
KOPT-K1 NYjT[|RxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUWwMlI2NzBwNT:xJO69VQ>? NH3teFJFVVOR MlXjbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MnPDNlM1QDJ5NEi=
TMD7 MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfSNE4zPS9yLkWvNUDPxE1? M2rqRWROW09? MkfmbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M{fzZVI{PDh{N{S4
THP-1 MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVOxPFh5OC5{NT:wMlUwOSEQvF2= NILQd4dFVVOR NW\1ZmdncW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M16weVI{PDh{N{S4
786-O MWfGeY5kfGmxbjDBd5NigQ>? M33a[FAvOS9yLkWg{txO NILjW48zPCCq NXGwPG97TE2VTx?= Mn3QbY5kemWjc3XzJGUu[2GmaHXybY4hdVKQQTDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgQ>? NXHFVHg{OjNzNEeyOVE>
786-O M3zBb2Z2dmO2aX;uJGF{e2G7 MYqwMVAvPSEQvF2= NXLTSYJvOjRiaB?= NUThZ|Z2TE2VTx?= NVfxd3VUemW|dXz0d{BqdiCjIHTvd4Uh\GWyZX7k[Y51KGmwY4LlZZNmKGmwIFWtZ4FlcGW{aX6gdJJwfGWrbjDlfJBz\XO|aX;uxsA> M{CxWFI{OTR5MkWx
OCI-AML3 NFrRbnBCeG:ydH;zbZMhSXO|YYm= NX;xd41POi53IN88US=> M3vodlczKGh? MYLpcoR2[2W|IHHwc5B1d3Orcx?= MlizNlI5OjZ3NkW=
Jurkat MkDxSpVv[3Srb36gRZN{[Xl? NHy4fHAyODBxMkCwM|QxOCCwTR?= MV:xPEBp M1fHWYlvcGmkaYTzJI1VV1KFMT3k[ZBmdmSnboSgV|YhWzJ|NT:yN|YheGixc4Doc5J6dGG2aX;u NUnEWpZCOjJ3Nk[2NFQ>
p210 BCR-Abl M4nJe2Z2dmO2aX;uJGF{e2G7 MYOxNFAwOjByL{SwNEBvVQ>? MVKxPEBp M1uwdIlvcGmkaYTzJI1VV1KFMT3k[ZBmdmSnboSgV|YhWzJ|NT:yN|YheGixc4Doc5J6dGG2aX;u M2LGc|IzPTZ4NkC0
Jurkat Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33jUFQxOG6P MmP2NlQwPDhiaB?= NXPMSHcye3mwZYLnbZpmKHerdHigNVcuSUGJIITvJJN2eHC{ZYPzJINmdGxicILvcIln\XKjdHnvci=> M3jMelIzPTZ4NkC0
p210 BCR-Abl MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4X2VlQxOG6P MXKyOE81QCCq NFK3fmd{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u MYSyNlU3PjZyNB?=
8226 MmHSSpVv[3Srb36gRZN{[Xl? NHXnUo4yODBvMUCwNEBvVQ>? MnvxN|AhdWmw NFrCZldFVVOR MojaZYN1cX[jdHXzJGVTU8Li MXiyNlU2PjRyOR?=
MM1.S  M1jJ[mZ2dmO2aX;uJGF{e2G7 MnTRNVAxNTFyMECgcm0> M1O2OVMxKG2rbh?= M2\pU2ROW09? NXriXm9x[WO2aY\heIV{KEWUS9Mg NWrzcmMzOjJ3NU[0NFk>
8226 Mlu5SpVv[3Srb36gRZN{[Xl? M4S5dlAvPSEQvF2= NWryVZhTOzBibXnu M{OwVGROW09? M3rTdolv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= NUnkbFFPOjJ3NU[0NFk>
MM1.S  NYXhfGlXTnWwY4Tpc44hSXO|YYm= Mny5NE42KM7:TR?= Ml;ON|AhdWmw NHHqfYpFVVOR MXfpcoR2[2W|IHHjeIl3[XSrb36gc4YhWkGIIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhVUWN M3r2WlIzPTV4NEC5
MCF-7 M171OmZ2dmO2aX;uJGF{e2G7 NHW2TZU2OC9{MECvOVAxKG6P NUezVG52OzBibXnu MXTkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NHjPTmMzOjR5Nki1Ni=>
T47D MVvGeY5kfGmxbjDBd5NigQ>? NHTF[lM2OC9{MECvOVAxKG6P NUP5PWhPOzBibXnu MlS4[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> NVHvb5dyOjJ2N{[4OVI>
MDA-MB-231 NEW4UlZHfW6ldHnvckBCe3OjeR?= Mn7tOVAwOjByL{WwNEBvVQ>? Mnv3N|AhdWmw MUHkc5NmNWSncHXu[IVvfGy7IDi1NQKBmzVyMNMgcm0qKHO3cIDy[ZN{\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MoOwNlI1PzZ6NUK=
Bcap-37 MnnNSpVv[3Srb36gRZN{[Xl? NWjCbXlrPTBxMkCwM|UxOCCwTR?= NGi1Uo0{OCCvaX6= MmHU[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MVGyNlQ4Pjh3Mh?=
MCF-7 NFjtVm9CeG:ydH;zbZMhSXO|YYm= MX:yNFDDqG6P NUjxcnJmOzZiaB?= M{fyeGROW09? MmXabY5lfWOnczDhdI9xfG:|aYO= NInWU4YzOjR5Nki1Ni=>
MDA-MB-231 NFXifVBCeG:ydH;zbZMhSXO|YYm= MWSyNFDDqG6P MUSzOkBp M{nkVGROW09? NUHxbmtNcW6mdXPld{BieG:ydH;zbZM> NFP1coMzOjR5Nki1Ni=>
Bcap-37 MkHiRZBweHSxc3nzJGF{e2G7 NGXlS2szODEEoH7N NUHVWIZbOzZiaB?= NYjhbG5FTE2VTx?= NFXpbpRqdmS3Y3XzJIFxd3C2b4Ppdy=> M4\hZVIzPDd4OEWy
LS174T MlXPSpVv[3Srb36gRZN{[Xl? NWnLPZVqOTBxMUCwM|ExODBibl2= NYf4UJBUPiCq NIT5VnpFVVOR MYfpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu NXHMSGR4OjJ2MEGyPVQ>
DLD-1  MW\GeY5kfGmxbjDBd5NigQ>? Ml3ZNVAwOTByL{GwNFAhdk1? M2nve|YhcA>? MWHEUXNQ M1PpNIlvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> NH2xTWczOjRyMUK5OC=>
SW480 MUDGeY5kfGmxbjDBd5NigQ>? MmHvNVAwOTByL{GwNFAhdk1? NE\LVVA3KGh? NWTKZo82TE2VTx?= NFzVU25qdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv M3iwcFIzPDBzMkm0
SW-48 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPpTWM2OD1yLkGg{txO NWPmOGs1OjJ{N{CyOVc>
HCT-15 M1\6fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnyNlFmUUN3ME2wMlMh|ryP MX6yNlI4ODJ3Nx?=
HCT 116 NVjDR|RRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwNjFOwG0> NX75Z|VMOjJ{N{CyOVc>
SW620-R NHO2[4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTFwMzFOwG0> MVmyNlI4ODJ3Nx?=
SK-CO-1 NV3wOJNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGn4V|BKSzVyPUKuNUDPxE1? NEfmOo4zOjJ5MEK1Oy=>
SW620 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTFzIN88US=> M4TpfFIzOjdyMkW3
BaF3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\HTVUxRTFwNES5JO69VQ>? M{KyfFIzOjJ|NkS1
NIH 3T3 MUHGeY5kfGmxbjDBd5NigQ>? NVn4b5VXOiEQvF2= MoDLNVghcA>? M3e3[4lvcGmkaYTzJI1VV1KFMjDwbI9{eGixconsZZRqd25ib3[gRYt1KG:wIGPldlQ4OyCjbnSgcXRQWkNzIIDoc5NxcG:{eXzheIlwdiCxZjC0SU1DWDFib36gWIhzOzdxNE[= NGXLUYYzOTh5NkGzNC=>
HCT15 NV3lRoN2TnWwY4Tpc44hSXO|YYm= MnuyNE42NzJizszN Mn:zOEBp Mn;KdJJmfmWwdIOgV|ZMOSCyaH;zdIhwenmuYYTpc44hd2Zicnnic5NwdWGuIIDyc5RmcW5iU{[gZZQhW2W{MkSwM|I1PCCjbnSgcXRQWkN{IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qh[XRiU3XyOFc{ MoTiNlE5PzZzM{C=
SW620  M4XUUGZ2dmO2aX;uJGF{e2G7 NHvkUlYxNjVxMjFOwG0> M3;XdFQhcA>? MnH5Zoxw[2u|IHHscEB1cHKnZTDtWG9TKG:3dID1eJM> NWf6[VI4OjF6N{[xN|A>

... 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