Torkinib (PP242)

Catalog No.S2218

Torkinib (PP242) Chemical Structure

Molecular Weight(MW): 308.34

Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.

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In DMSO USD 91 In stock
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8 Customer Reviews

  • MTORC1 regulates the subcellular distribution of TFEB. Immunofluorescence confocal microscopy showing nuclear localization of recombinant TFEB-Flag in ARPE-19 cells incubated with MTORC1 inhibitors (PP242, LY294002, Wortmannin).

    Autophagy 2012 8(6), 903-14. Torkinib (PP242) purchased from Selleck.

    Pharmacological PP242 induces transport of TFEB to the nucleus. HeLa cells stably expressing TFEB (CF7) were incubated with the indicated kinase inhibitors and the electrophoretic mobility of TFEB was monitored by immunoblotting.

    Autophagy 2012 8(6), 903-14. Torkinib (PP242) purchased from Selleck.

  • AKT protein kinase activity controls protein synthesis by regulating the multistep process of mRNA translation at multiple stages from ribosome biogenesis to translation initiation and elongation. PC3-LN4 cells were treated with GSK690693 (5 uM) alone, or in combination with PP242 (2 uM) or AZD8055 (1 uM) for 24 h, and immunoblotting performed.

    Cancer Res 2013 73(11), 3402-11. Torkinib (PP242) purchased from Selleck.

    Synergistic effect of BMS-777607 with mTOR inhibitors in reduction of CSCs+24/44/ESA viability. CSCs+24/44/ESA at 5,000 cells per well with stem cell culture media in triplicate in an ultra-low adhesion plate were treated with 5 umol/L BMS-777607, 1 umol/L AZD8055, 1 umol/L RAD001, and 1 umol/L PP242 alone, or in their different combinations. Cells were cultured for 72 hours. Percentages of polyploid cells were determined by counting 300 cells from two different regions. Results shown here were from one of two experiments with similar results.

    Mol Cancer Ther 2014 13(1), 37-48. Torkinib (PP242) purchased from Selleck.

  • (A) MEF and PC3-LN4 cells were treated with GNE-652 or LGB321 in a dose dependent manner and PP242 (1 µmol/L) for 16 hr

    Oncotarget, 2016, 7(15):20152-65. Torkinib (PP242) purchased from Selleck.

    HeLa cells were treated with MK2206 (1 uM), rapamycin (Rapa; 100 nM), PP242 (1 uM), BEZ235 (0.5 uM), U0126 (U0; 15 uM), BI-D1870 (BI; 10 uM), GNE-652 (1 uM), AZD1208 (3 uM), and the indicated inhibitor combinations for 3 h. Cell lysates were analyzed by immunoblot assays using indicated antibodies.

    Mol Cell Biol 2014 34(13), 2517-32. Torkinib (PP242) purchased from Selleck.

  • Torkinib (PP242) purchased from Selleck.

    A549 cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of  PP242 for 24 hours.

     

     

    Dr. Zhang of Tianjin Medical University. Torkinib (PP242) purchased from Selleck.

Purity & Quality Control

Choose Selective mTOR Inhibitors

Biological Activity

Description Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.
Features One of the first selective inhibitors that targets ATP domain of mTOR.
Targets
mTOR [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
DNA-PK [1]
(Cell-free assay)
PDGFR [1]
(Cell-free assay)
8 nM 0.10 μM 0.41 μM 0.41 μM
In vitro

PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively. PP242 displays some inhibitory activity against Ret, PKCα, PKCβ, and JAK2, while exhibits remarkable selectivity against 215 other protein kinases. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2. In BT549 cells, PP242 treatment (0.04-10 μM) inhibits the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner. [1] PP242 potently inhibits PKCα with IC50 of 49 nM. Low concentrations of PP242 inhibit the phosphorylation of Akt S473 and higher concentrations partially inhibit Akt T308-P in addition to S473-P. As PP242 is a more effective mTORC1 inhibitor than rapamycin, PP242 inhibits the proliferation of primary MEFs, and the phosphorylation of 4EBP1 at T36/45 and S65, more potently than rapamycin. PP242 but not rapamycin potently inhibits cap-dependent translation, by causing a higher level of binding between 4EBP1 and eIF4E than rapamycin. [2] PP242 potently inhibits the proliferation of p190-transformed murine BM, SUP-B15, and K562 cells with GI50 of 12 nM, 90 nM, and 85 nM, respectively. PP242 also inhibits the growth of solid tumor cell lines such as SKOV3, PC3, 786-O, and U87 with GI50 of 0.49 μM, 0.19 μM, 2.13 μM, and 1.57 μM, respectively. [3] PP242 is also more effective than rapamycin in achieving cytoreduction and apoptosis in multiple myeloma (MM) cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-p21 MX7GeY5kfGmxbjDBd5NigQ>? NILvXJo2OC1zMkWwJI5O M1jaelI1KGh? Ml7NSG1UVw>? MnfNbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHM3KGurbnHz[UApfGG{Z3X0JI9nKG2WT2LDNUkh[W6mIHn0d{Bld3ewc4Ty[YFuKHSjcnfleEBxcG:|cHjvMXM3yqB? M4rlV|I3OTd5MEWx
U87vIII  M2m0WWZ2dmO2aX;uJGF{e2G7 MWKwMlA1NTJwNTFOwG0> M1\jRVI1KGh? MYPpcohq[mm2czDtWG9TSzFiYX7kJI1VV1KFMjDhZ5Rqfmm2aXXzxsA> M4TkS|I3OTN2NkG3
U87vIII  M3TCSGZ2dmO2aX;uJGF{e2G7 MmfFNk42NzVizszN NEHTPYoyOiCq NUXufWpWcW6qaXLpeJMh\2GyIHPsc5NqdmdiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGDSengzPjF|NE[xOy=>
PC12  MV;GeY5kfGmxbjDBd5NigQ>? NFXNe2U1OMLibl2= MnjFbY5lfWOnczDsfZNwe2:vYXygZolw\2WwZYPpd{BidmRiYXzs[ZZq[XSnZDFOtU1UYU5iYXPjeY12dGG2aX;uxsA> M3zWXFI3ODBzNkG0
3T3-L1 NWDtdJhVTnWwY4Tpc44hSXO|YYm= MV2xOUDPxE1? MVq0JIg> MWHzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZidHjlJGVoejFicILveIVqdsLi NXzvcHg4OjV6MUS2OlI>
Rh30 MVfGeY5kfGmxbjDBd5NigQ>? MUWxJO69VQ>? MXOyJIg> MlXKbY5pcWKrdIOgZo91cCCvVF;SR|EudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKFN4S{GgZY5lKG2WT2LDNk1u\WSrYYTl[EBxcG:|cHjvdplt[XSrb36gc4YhSWu2 NX3rfmo3OjV5NkK2NVk>
HT29 MYTGeY5kfGmxbjDBd5NigQ>? MWWxJO69VQ>? M3TkT|IhcA>? NFLNVVdqdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= NHWxNnYzPTd4Mk[xPS=>
Rh30 NGi0bnJHfW6ldHnvckBCe3OjeR?= M13DT|Eh|ryP M2LtNFIhcA>? NYTM[Fhse3WycILld5NmeyC2aHWgZoF{[Wxib4KgTWdHNTFvc4TpcZVt[XSnZDDj[YxtKGGmaHXzbY9v NH[5ZoszPTd4Mk[xPS=>
HT29 NGLB[5hHfW6ldHnvckBCe3OjeR?= Mo[zNUDPxE1? MX6yJIg> MW\zeZBxemW|c3XzJJRp\SCkYYPhcEBweiCLR1[tNU1{fGmvdXzheIVlKGOnbHygZYRp\XOrb36= M3W4flI2PzZ{NkG5
U87 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSyOUBvVQ>? NVT1SWpEOjRiaB?= NETOO25qdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> MYmyOVU3QDZ4NR?=
AGS NIjH[ZBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXuwMVExODBibl2= M{TFTFI1NzR6IHi= NXnyWY9QTE2VTx?= NXvhOotC\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NXLSZnBqOjVyM{W5OlE>
MKN45 NVrNbXlvS2WubDDWbYFjcWyrdImgRZN{[Xl? MXiwMVExODBibl2= M13Ie|I1NzR6IHi= M{TCPWROW09? MlXq[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mkn2NlUxOzV7NkG=
MKN28 M1TwNGNmdGxiVnnhZoltcXS7IFHzd4F6 MWewMVExODBibl2= NUTrVWdsOjRxNEigbC=> MWnEUXNQ M2DJb4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MX[yOVA{PTl4MR?=
KATO3 M4CyWGNmdGxiVnnhZoltcXS7IFHzd4F6 MWWwMVExODBibl2= NYXM[ZdmOjRxNEigbC=> NYHOVlBnTE2VTx?= NI\2NZZl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MWiyOVA{PTl4MR?=
SGC7901 NG[xTnhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFO0VVExNTFyMECgcm0> MnrKNlQwPDhiaB?= NF[3PVRFVVOR NVz4cI9X\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= Ml7VNlUxOzV7NkG=
N87 Mk\oR4VtdCCYaXHibYxqfHliQYPzZZk> M{PaTFAuOTByMDDuUS=> MV6yOE81QCCq MkOwSG1UVw>? MW\k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NFKxd|AzPTB|NUm2NS=>
HMEC NWWwbVFYS2WubDDWbYFjcWyrdImgRZN{[Xl? MXmwMVExODBibl2= NVn1cGhlOjRxNEigbC=> MXrEUXNQ MlTC[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NUTpfFh{OjVyM{W5OlE>
HUVEC M3LOWGNmdGxiVnnhZoltcXS7IFHzd4F6 MojYNE0yODByIH7N M4ftUlI1NzR6IHi= MWrEUXNQ NVnSbIdY\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NYHrbIs3OjVyM{W5OlE>
MG63 M1HIZWZ2dmO2aX;uJGF{e2G7 NYfMboNFPTBvMUCwNEBvVQ>? NXzwSnJHOC53IHi= MWDkc5NmKGSncHXu[IVvfGy7IDi1NQKBmzFyMECgcm0qKGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= NUHsV|Z3OjR6NECxN|Q>
U2OS  MnexSpVv[3Srb36gRZN{[Xl? M{DH[FUxNTFyMECgcm0> M3\wbFAvPSCq M{jW[4Rwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NWXZWFVnOjR6NECxN|Q>
Saos-2  MmfUSpVv[3Srb36gRZN{[Xl? MV[1NE0yODByIH7N MkHYNE42KGh? NVXZS5pC\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 NVfIXVRrOjR6NECxN|Q>
Saos-2 NVX6VXkxTnWwY4Tpc44hSXO|YYm= MnX5NVAxKG6P M4TjW|AvPSCq MkP1dJJmfmWwdIOgc5N1\W:|YYLjc41iKGOnbHygcYloemG2aX;u MkGzNlQ5PDBzM{S=
MG63 NGTtcWFCeG:ydH;zbZMhSXO|YYm= M13sS|ExOCCwTR?= MmDDN|YhcA>? Ml\UdJJwdW:2ZYOgZZBweHSxc3nz MXKyOFg1ODF|NB?=
U2OS  M123WmFxd3C2b4Ppd{BCe3OjeR?= M17rUVExOCCwTR?= MofYN|YhcA>? MWLwdo9ud3SnczDhdI9xfG:|aYO= NVjGdWl7OjR6NECxN|Q>
Saos-2  MVvBdI9xfG:|aYOgRZN{[Xl? NGXNfIsyODBibl2= NVjZeXhUOzZiaB?= M1LRfpBzd22xdHXzJIFxd3C2b4Ppdy=> MmiyNlQ5PDBzM{S=
HT1376 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHrWpNKSzVyPUGuPFghyrFiMT6xJO69VQ>? M4PtfVI1ODV2OEex
T24 NW[xOHluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XmUWlEPTB;MT6zO{DDuSByLkSg{txO NGDN[ZkzPDB3NEi3NS=>
UM-UC-3 MkTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHD[HJyUUN3ME2wMlY{KMLzMD6xJO69VQ>? NGP6dlgzPDB3NEi3NS=>
DLD-1 M{Tu[GNmdGxiVnnhZoltcXS7IFHzd4F6 NVXhdnZPOC1zMECwJI5O NID5WHczPCCq NUK5RpRrcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWOyN|k6OTF5OR?=
Caco2 MoGwR4VtdCCYaXHibYxqfHliQYPzZZk> MXOwMVExODBibl2= MWWyOEBp NV76SZVscW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIjtbVczOzl7MUG3PS=>
HT29 NHjHdJZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1z2NlAuOTByMDDuUS=> M2jBe|I1KGh? NFjYWoxqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVrL[|dJOjN7OUGxO|k>
H116 M2CwU2NmdGxiVnnhZoltcXS7IFHzd4F6 NXftU45vOC1zMECwJI5O MlvkNlQhcA>? MVPpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NV3KUHdrOjN7OUGxO|k>
Hct-8 NEnXe|NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnPmNE0yODByIH7N NYOwVpdSOjRiaB?= MVHpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MoLpNlM6QTFzN{m=
Colo320 MkDCR4VtdCCYaXHibYxqfHliQYPzZZk> Ml3SNE0yODByIH7N MYGyOEBp M1rkZYlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnzBNlM6QTFzN{m=
Sw948 MoTxR4VtdCCYaXHibYxqfHliQYPzZZk> NV3Xc|F{OC1zMECwJI5O M1n1XFI1KGh? MoLpbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkHYNlM6QTFzN{m=
Colo205 NVTOTI06S2WubDDWbYFjcWyrdImgRZN{[Xl? MmnTNE0yODByIH7N MlnVNlQhcA>? NWrEfmczcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVKyN|k6OTF5OR?=
Colo320 NEfFTWNHfW6ldHnvckBCe3OjeR?= M{T1TFEh|ryP NEPybpIxNTJ2IHi= NUHoc5JG[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MoC3NlM6QTFzN{m=
HT29 NULBSIp2TnWwY4Tpc44hSXO|YYm= NWnBTJlbOSEQvF2= NIT1UoExNTJ2IHi= M36wZYFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> NFjDSpIzOzl7MUG3PS=>
Sw948 M1W5OWZ2dmO2aX;uJGF{e2G7 NEf2NpYyKM7:TR?= NVHxPJJ7OC1{NDDo NH\6V4Ri[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 MYCyN|k6OTF5OR?=
DLD-1 NI\xToNHfW6ldHnvckBCe3OjeR?= MoPUNUDPxE1? M1HS[lAuOjRiaB?= NITSOVVi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 M{jJOVI{QTlzMUe5
SW620 NHSxZ2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTdwODFOwG0> NITYOmczOzV2MkG3PC=>
SW480 NHPPT|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrqTWM2OD12Lk[g{txO NYXiZ3B5OjN3NEKxO|g>
SK-CO-1 Ml61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF21elVKSzVyPUSg{txO NVH3SpVCOjN3NEKxO|g>
LS-513 NIXUdWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTaXJV7UUN3ME2zMlkh|ryP NHr0SIEzOzV2MkG3PC=>
SW1116 MlP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjWTWM2OD1yLki0JO69VQ>? NYfETZZROjN3NEKxO|g>
LS-174T MlvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfYWFlKSzVyPUCuPFQh|ryP NEHEeo8zOzV2MkG3PC=>
HCT 116 MnnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVf2SXZbUUN3ME2wMlQyKM7:TR?= M1TS[VI{PTR{MUe4
HCT 15 NIjGfZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DGRWlEPTB;MD6zJO69VQ>? MnKyNlM2PDJzN{i=
COLO 205 M2XxRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrSTWM2OD1yLkK0JO69VQ>? NEO5S4wzOzV2MkG3PC=>
HT-29 M2D6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfMPZB2UUN3ME2wMlI{KM7:TR?= MlTwNlM2PDJzN{i=
COLO 201 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\JblJKSzVyPUCuNlMh|ryP NUm1T4EzOjN3NEKxO|g>
Caco-2 MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMkKg{txO MoX3NlM2PDJzN{i=
SW48 MmLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLlTWM2OD1yLkC5JO69VQ>? NI\EZpUzOzV2MkG3PC=>
DND-1 Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvtW2FSOC5{NT:wMlUwOSEQvF2= NGTPSYdFVVOR NYrEOlNUcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MoPmNlM1QDJ5NEi=
TMD8 NGH0VmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TEXlAvOjVxMD61M|Eh|ryP MXnEUXNQ Ml;IbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M3u1VlI{PDh{N{S4
Jurkat M1j2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXwblkxNjJ3L{CuOU8yKM7:TR?= NYXkN5JWTE2VTx?= MX\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NIS2NYszOzR6Mke0PC=>
KOPT-K1 NGLpPFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojWNE4zPS9yLkWvNUDPxE1? MlLXSG1UVw>? MWDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWTWSlhxOjN2OEK3OFg>
TMD7 NYjpXY51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXWwMlI2NzBwNT:xJO69VQ>? NEfxTIdFVVOR NEXETlZqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NEe0c3ozOzR6Mke0PC=>
THP-1 NIjRNVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljLNE4zPS9yLkWvNUDPxE1? M{nhVmROW09? NHTSbWVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MWqyN|Q5Ojd2OB?=
786-O M1S5TmZ2dmO2aX;uJGF{e2G7 M2TOOlAvOS9yLkWg{txO NWDWc3FROjRiaB?= NE\vb4RFVVOR NXGyVo9VcW6lcnXhd4V{KEVvY3HkbIVzcW5ibWLORUBt\X[nbIOg[I9{\SCmZYDlcoRmdnSueR?= M33re|I{OTR5MkWx
786-O MmK2SpVv[3Srb36gRZN{[Xl? M33qSFAuOC53IN88US=> MmX5NlQhcA>? MmK4SG1UVw>? NYXNWZlDemW|dXz0d{BqdiCjIHTvd4Uh\GWyZX7k[Y51KGmwY4LlZZNmKGmwIFWtZ4FlcGW{aX6gdJJwfGWrbjDlfJBz\XO|aX;uxsA> NYHoRXR7OjNzNEeyOVE>
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p210 BCR-Abl M3jK[WZ2dmO2aX;uJGF{e2G7 M4m2WVExOC9{MECvOFAxKG6P NWr3OnBMOThiaB?= MYjpcohq[mm2czDtWG9TSzFvZHXw[Y5l\W62IGO2JHMzOzVxMkO2JJBpd3OyaH;yfYxifGmxbh?= M1TvSFIzPTZ4NkC0
Jurkat M{fMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml61OFAxdk1? Mo\PNlQwPDhiaB?= NGD6R2N{gW6ncnfpfoUhf2m2aDCxO{1CSUdidH:gd5VxeHKnc4OgZ4VtdCCycn;sbYZmemG2aX;u M{fo[VIzPTZ4NkC0
p210 BCR-Abl NEXGeFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXu0NFBvVQ>? NGLLOoQzPC92ODDo MnHGd5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= MXSyNlU3PjZyNB?=
8226 MljNSpVv[3Srb36gRZN{[Xl? NEfuRZYyODBvMUCwNEBvVQ>? NXTzWHZPOzBibXnu NH[0NJlFVVOR M3jVO4FkfGm4YYTld{BGWkwEoB?= M{CxO|IzPTV4NEC5
MM1.S  M2TEb2Z2dmO2aX;uJGF{e2G7 NXzoZlRoOTByLUGwNFAhdk1? NY\wd|k1OzBibXnu MYrEUXNQ M1XkSYFkfGm4YYTld{BGWkwEoB?= NYjHeZd{OjJ3NU[0NFk>
8226 NWLOcnloTnWwY4Tpc44hSXO|YYm= NUfGdm1bOC53IN88US=> NEDHbpc{OCCvaX6= NVXGOIE{TE2VTx?= MV;pcoR2[2W|IHHjeIl3[XSrb36gc4YhWkGIIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhVUWN NVfjW252OjJ3NU[0NFk>
MM1.S  NXHyR3Q3TnWwY4Tpc44hSXO|YYm= MYOwMlUh|ryP MmS2N|AhdWmw NHv5S3pFVVOR NUXhVWVzcW6mdXPld{Bi[3SrdnH0bY9vKG:oIGLBSkBidmRicHjvd5Bpd3K7bHH0bY9vKG:oIF3FTy=> M1SyeVIzPTV4NEC5
MCF-7 NFn3bpFHfW6ldHnvckBCe3OjeR?= NUDrSXFyPTBxMkCwM|UxOCCwTR?= NYTRcYU5OzBibXnu NGrHc29ld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? NWfIXJVkOjJ2N{[4OVI>
T47D NIT6SHhHfW6ldHnvckBCe3OjeR?= NYDBb29ZPTBxMkCwM|UxOCCwTR?= Ml20N|AhdWmw M3mwXIRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 NIH5NlkzOjR5Nki1Ni=>
MDA-MB-231 MVHGeY5kfGmxbjDBd5NigQ>? MVG1NE8zODBxNUCwJI5O M4ewXFMxKG2rbh?= M4i4PIRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MY[yNlQ4Pjh3Mh?=
Bcap-37 NEfnS2lHfW6ldHnvckBCe3OjeR?= M2HPZ|UxNzJyMD:1NFAhdk1? NXvjc2ZKOzBibXnu NHLRblJld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? M3HaZ|IzPDd4OEWy
MCF-7 NYL5OIlESXCxcITvd4l{KEG|c3H5 MWeyNFDDqG6P MmfpN|YhcA>? MXvEUXNQ MVXpcoR2[2W|IHHwc5B1d3Orcx?= NUHpe|ZXOjJ2N{[4OVI>
MDA-MB-231 MnHLRZBweHSxc3nzJGF{e2G7 NGXSV|IzODEEoH7N M2jTZlM3KGh? M{D2S2ROW09? NELYOGdqdmS3Y3XzJIFxd3C2b4Ppdy=> M2n3bFIzPDd4OEWy
Bcap-37 MU\BdI9xfG:|aYOgRZN{[Xl? M{PpflIxOMLibl2= NVnLNm1iOzZiaB?= NEXNfHFFVVOR MkWwbY5lfWOnczDhdI9xfG:|aYO= M2P6OFIzPDd4OEWy
LS174T M4TSfWZ2dmO2aX;uJGF{e2G7 M1W3OlExNzFyMD:xNFAxKG6P NFrhe5g3KGh? NIjvbXlFVVOR NUXwVI5xcW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? MmHDNlI1ODF{OUS=
DLD-1  MVPGeY5kfGmxbjDBd5NigQ>? MWKxNE8yODBxMUCwNEBvVQ>? NHi5U2g3KGh? MUXEUXNQ NWSyNVVicW6qaXLpeJMhdVSRUlOxJIFkfGm4aYT5JIJ6KHSqZTDk[ZBpd3OyaH;yfYxifGmxbjDv[kBUPiC{aXLvd49u[WxicILveIVqdg>? M33RUlIzPDBzMkm0
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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 to the product individually and in order:
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
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

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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