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.

Cited by 28 Publications

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 NUDLPFVYTnWwY4Tpc44hSXO|YYm= Mm\iOVAuOTJ3MDDuUS=> M3TIb|I1KGh? MmXvSG1UVw>? NUfi[3JkcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFN4IHvpcoF{\SBqdHHy[4V1KG:oIH3UU3JEOSliYX7kJIl1eyCmb4fud5Rz\WGvIIThdodmfCCyaH;zdIhwNVN4wrC= M2L2U|I3OTd5MEWx
U87vIII  NVzJOW1QTnWwY4Tpc44hSXO|YYm= MYWwMlA1NTJwNTFOwG0> Mn24NlQhcA>? MnLqbY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh MWiyOlE{PDZzNx?=
U87vIII  MlnaSpVv[3Srb36gRZN{[Xl? M4PIO|IvPS93IN88US=> NXyxdlQ4OTJiaB?= M{DiOYlvcGmkaYTzJIdieCClbH;zbY5oKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mn\6NlYyOzR4MUe=
PC12  NFXZOFNHfW6ldHnvckBCe3OjeR?= NF65R5k1OMLibl2= NUDxe|JucW6mdXPld{BtgXOxc3;tZYwh[mmxZ3Xu[ZNqeyCjbnSgZYxt\X[rYYTl[EDPuS2VWV6gZYNkfW23bHH0bY9vyqB? MXWyOlAxOTZzNB?=
3T3-L1 NUSyZ2VwTnWwY4Tpc44hSXO|YYm= MoK3NVUh|ryP M1fCelQhcA>? NVzTNFV5e3WycILld5NmeyCneIDy[ZN{cW:wIH;mJJRp\SCHZ4KxJJBzd3SnaX9CpC=> M4nLfVI2QDF2Nk[y
Rh30 NHfPXmdHfW6ldHnvckBCe3OjeR?= MnPHNUDPxE1? MWCyJIg> NYG0XIM2cW6qaXLpeJMh[m:2aDDtWG9TSzFvbXXkbYF1\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGO2T|Eh[W6mIH3UU3JEOi2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NVj3SJY4OjV5NkK2NVk>
HT29 MmnUSpVv[3Srb36gRZN{[Xl? MmnXNUDPxE1? M3fPdFIhcA>? M3ywZolvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= MnLLNlU4PjJ4MUm=
Rh30 NX3yPFg1TnWwY4Tpc44hSXO|YYm= MnfTNUDPxE1? M3y3OVIhcA>? NWe5T3BOe3WycILld5NmeyC2aHWgZoF{[Wxib4KgTWdHNTFvc4TpcZVt[XSnZDDj[YxtKGGmaHXzbY9v M3PXd|I2PzZ{NkG5
HT29 MmPySpVv[3Srb36gRZN{[Xl? MU[xJO69VQ>? Mlz6NkBp NGDjWoJ{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> NUjCbZlKOjV5NkK2NVk>
U87 MmrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fK[FI2KG6P NVzWXnN{OjRiaB?= MYjpcoNz\WG|ZYOgSHVUWDFyIHvuc4Ns\WRvZH;3ckBqdmS3Y3XkJINmdGxiaX7obYJqfGmxbh?= M17McVI2PTZ6Nk[1
AGS MXjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4TEOlAuOTByMDDuUS=> M4D4fVI1NzR6IHi= NVjWU3VNTE2VTx?= M{OyeIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGT3e4YzPTB|NUm2NS=>
MKN45 MnjpR4VtdCCYaXHibYxqfHliQYPzZZk> MnTDNE0yODByIH7N MlXBNlQwPDhiaB?= NX3JcYJoTE2VTx?= NYT3Spht\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M4rBVFI2ODN3OU[x
MKN28 M{PGT2NmdGxiVnnhZoltcXS7IFHzd4F6 M4CwVFAuOTByMDDuUS=> MYiyOE81QCCq M1r1b2ROW09? MU\k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz Mn;ONlUxOzV7NkG=
KATO3 NHPn[YFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MojqNE0yODByIH7N MXiyOE81QCCq NF3TNVlFVVOR Mlny[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MkjONlUxOzV7NkG=
SGC7901 NFf2dItE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXKwMVExODBibl2= NIHI[JkzPC92ODDo MnTySG1UVw>? NF;abGVl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MojlNlUxOzV7NkG=
N87 NVfTdZh5S2WubDDWbYFjcWyrdImgRZN{[Xl? MknUNE0yODByIH7N NX3kXoFIOjRxNEigbC=> M2TGR2ROW09? Moj0[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NFrnfpQzPTB|NUm2NS=>
HMEC NEjxTGVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnHhNE0yODByIH7N MofGNlQwPDhiaB?= MV7EUXNQ NUDYSFdF\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MXKyOVA{PTl4MR?=
HUVEC NWLONWJYS2WubDDWbYFjcWyrdImgRZN{[Xl? M3XNSlAuOTByMDDuUS=> MXyyOE81QCCq NWC3W5hZTE2VTx?= M2SzbIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NIfPc5kzPTB|NUm2NS=>
MG63 NV;pOXNyTnWwY4Tpc44hSXO|YYm= MofZOVAuOTByMDDuUS=> NV7XPYJqOC53IHi= NVjJUoYz\G:|ZTDk[ZBmdmSnboTsfUApPTEkgKOxNFAxKG6PKTDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRYt1 MUKyOFg1ODF|NB?=
U2OS  NXfve|VFTnWwY4Tpc44hSXO|YYm= MkDLOVAuOTByMDDuUS=> M3;JXVAvPSCq MmHK[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 MV[yOFg1ODF|NB?=
Saos-2  NWfBSWpJTnWwY4Tpc44hSXO|YYm= NEHicmo2OC1zMECwJI5O NV3Vc5hiOC53IHi= MmfF[I9{\SCmZYDlcoRmdnSueTCoOVDjiJNzMECwJI5OMSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 NGnvU3AzPDh2MEGzOC=>
Saos-2 NUTI[GZZTnWwY4Tpc44hSXO|YYm= NX\TOVdIOTByIH7N M3vGUVAvPSCq M3zETJBz\X[nboTzJI9{fGWxc3HyZ49u[SClZXzsJI1q\3KjdHnvci=> MnfGNlQ5PDBzM{S=
MG63 NVi2WYVpSXCxcITvd4l{KEG|c3H5 NYXBZWZjOTByIH7N M3TkRVM3KGh? MWTwdo9ud3SnczDhdI9xfG:|aYO= MlHsNlQ5PDBzM{S=
U2OS  Ml31RZBweHSxc3nzJGF{e2G7 M4rGOFExOCCwTR?= MUmzOkBp MXjwdo9ud3SnczDhdI9xfG:|aYO= NIi0O|kzPDh2MEGzOC=>
Saos-2  NW\jeFhmSXCxcITvd4l{KEG|c3H5 NHG1fFAyODBibl2= MWSzOkBp NEHCUFFxem:vb4Tld{BieG:ydH;zbZM> NG\hdIIzPDh2MEGzOC=>
HT1376 NUPw[IVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTFwOEigxtEhOS5zIN88US=> NXrUZnJ3OjRyNUS4O|E>
T24 NXzTPFFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jpSmlEPTB;MT6zO{DDuSByLkSg{txO M1TNVVI1ODV2OEex
UM-UC-3 NFnpXFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH2TWM2OD1yLk[zJOKyOC5zIN88US=> M3TT[|I1ODV2OEex
DLD-1 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2HZTFAuOTByMDDuUS=> NWrvSoNuOjRiaB?= MWLpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MVKyN|k6OTF5OR?=
Caco2 NF;WfIFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2S2eVAuOTByMDDuUS=> M2rp[|I1KGh? NWjo[3ZncW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHLGNoczOzl7MUG3PS=>
HT29 NVGwN2NSS2WubDDWbYFjcWyrdImgRZN{[Xl? NHe2TncxNTFyMECgcm0> NHf2dWwzPCCq MofvbY5pcWKrdIOgeIhmKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlX4NlM6QTFzN{m=
H116 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4fUNlAuOTByMDDuUS=> MXOyOEBp MYPpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX2yN|k6OTF5OR?=
Hct-8 M1Xo[GNmdGxiVnnhZoltcXS7IFHzd4F6 NVjTVoJNOC1zMECwJI5O M1TndVI1KGh? M1O4ZYlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3nuR|I{QTlzMUe5
Colo320 Mo\nR4VtdCCYaXHibYxqfHliQYPzZZk> M{C4c|AuOTByMDDuUS=> NIjxSHUzPCCq M4jYPIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{jOR|I{QTlzMUe5
Sw948 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnnYNE0yODByIH7N MlTwNlQhcA>? NXLQcJF5cW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NEeyWJczOzl7MUG3PS=>
Colo205 MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3jRXVAuOTByMDDuUS=> Mo\ONlQhcA>? NVvhfFNTcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1\Mb|I{QTlzMUe5
Colo320 NEHBfldHfW6ldHnvckBCe3OjeR?= M321VlEh|ryP M{PYVlAuOjRiaB?= NYrvVVNt[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? M2jBNVI{QTlzMUe5
HT29 NI\kcpFHfW6ldHnvckBCe3OjeR?= MoLoNUDPxE1? NWjabIJUOC1{NDDo M2PHOYFjd2yrc3jld{B1cGViU{\TNlM2NzJ|NtMgZpV1KHCjcoTpZYxtgSC{ZXT1Z4V{KHSqZTC0SU1DWDGWM{[vOFU> MUKyN|k6OTF5OR?=
Sw948 MnPKSpVv[3Srb36gRZN{[Xl? M4TFb|Eh|ryP M{W4UVAuOjRiaB?= MlLuZYJwdGm|aHXzJJRp\SCVNmOyN|UwOjN4wrDieZQheGG{dHnhcIx6KHKnZIXj[ZMhfGinIETFMWJROVR|Nj:0OS=> NYntSm9QOjN7OUGxO|k>
DLD-1 MXHGeY5kfGmxbjDBd5NigQ>? MnvKNUDPxE1? M3nTeVAuOjRiaB?= MULhZo9tcXOqZYOgeIhmKFN4U{KzOU8zOzcEoHL1eEBx[XK2aXHscJkhemWmdXPld{B1cGViNFWtRnAyXDN4L{S1 M{W4NVI{QTlzMUe5
SW620 M2fO[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTdwODFOwG0> MXSyN|U1OjF5OB?=
SW480 NXfhc|VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fhemlEPTB;ND62JO69VQ>? Ml:zNlM2PDJzN{i=
SK-CO-1 MkDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTRizszN MVGyN|U1OjF5OB?=
LS-513 NIHzbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfWTWM2OD1|Lkmg{txO NYDNbHIyOjN3NEKxO|g>
SW1116 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwOESg{txO NUjWPIJROjN3NEKxO|g>
LS-174T NFTOUIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml22TWM2OD1yLki0JO69VQ>? NWnPepp1OjN3NEKxO|g>
HCT 116 MknES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTiRW56UUN3ME2wMlQyKM7:TR?= MV[yN|U1OjF5OB?=
HCT 15 MmXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTBwMzFOwG0> MYGyN|U1OjF5OB?=
COLO 205 Mlr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnQcIlQUUN3ME2wMlI1KM7:TR?= MYWyN|U1OjF5OB?=
HT-29 MkPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHZO2VKSzVyPUCuNlMh|ryP MWWyN|U1OjF5OB?=
COLO 201 NULhS|hqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrOO3VKSzVyPUCuNlMh|ryP MUmyN|U1OjF5OB?=
Caco-2 NFLqc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXETWM2OD1yLkKyJO69VQ>? NFrP[oczOzV2MkG3PC=>
SW48 M4\FXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHi1XYNKSzVyPUCuNFkh|ryP M4rQXFI{PTR{MUe4
DND-1 MlHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPBZ3ZYOC5{NT:wMlUwOSEQvF2= NXfN[IRxTE2VTx?= M3fpbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NIric20zOzR6Mke0PC=>
TMD8 M{DDV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\vZmVmOC5{NT:wMlUwOSEQvF2= MYDEUXNQ NGjqSIZqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M{nlblI{PDh{N{S4
Jurkat Mn7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnYeFYxNjJ3L{CuOU8yKM7:TR?= NVXYbIVHTE2VTx?= NEfYdm1qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NYH5bIJQOjN2OEK3OFg>
KOPT-K1 NYfjfWpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1foeVAvOjVxMD61M|Eh|ryP NYHLeZJGTE2VTx?= NUD1fIJHcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MWCyN|Q5Ojd2OB?=
TMD7 NFjjfIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDwcXgxNjJ3L{CuOU8yKM7:TR?= M4LIOmROW09? MXvpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MnzsNlM1QDJ5NEi=
THP-1 NEDKW4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\EZVAvOjVxMD61M|Eh|ryP M1SxWWROW09? MmfLbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NHfGN5QzOzR6Mke0PC=>
786-O MW\GeY5kfGmxbjDBd5NigQ>? NELIepoxNjFxMD61JO69VQ>? MX2yOEBp MYnEUXNQ MXnpcoNz\WG|ZYOgSU1k[WSqZYLpckBuWk6DIHzleoVteyCmb4PlJIRmeGWwZHXueIx6 NInyPXYzOzF2N{K1NS=>
786-O NETJRZlHfW6ldHnvckBCe3OjeR?= MnHPNE0xNjVizszN MnK3NlQhcA>? MlvsSG1UVw>? MUfy[ZN2dHS|IHnuJIEh\G:|ZTDk[ZBmdmSnboSgbY5kemWjc3WgbY4hTS2lYXTo[ZJqdiCycn;0[YlvKGW6cILld5Nqd28EoB?= NH2zTW0zOzF2N{K1NS=>
OCI-AML3 M4rKSGFxd3C2b4Ppd{BCe3OjeR?= MoOzNk42KM7:TR?= M33aWlczKGh? NYr2NW1YcW6mdXPld{BieG:ydH;zbZM> MnHpNlI5OjZ3NkW=
Jurkat NFLPbnFHfW6ldHnvckBCe3OjeR?= NILENGoyODBxMkCwM|QxOCCwTR?= NGjyT3kyQCCq NWW3bYhqcW6qaXLpeJMhdVSRUlOxMYRmeGWwZHXueEBUPiCVMkO1M|I{PiCyaH;zdIhwenmuYYTpc44> MXGyNlU3PjZyNB?=
p210 BCR-Abl NXS3e3JXTnWwY4Tpc44hSXO|YYm= NVe0bVFIOTByL{KwNE81ODBibl2= NWjjeI04OThiaB?= MXLpcohq[mm2czDtWG9TSzFvZHXw[Y5l\W62IGO2JHMzOzVxMkO2JJBpd3OyaH;yfYxifGmxbh?= NVnNdItvOjJ3Nk[2NFQ>
Jurkat NXPVW3c{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPyOFAxdk1? NIq3WZYzPC92ODDo M3fuUZN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= MnGwNlI2PjZ4MES=
p210 BCR-Abl MojHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrBOFAxdk1? MlzMNlQwPDhiaB?= M1XLepN6dmW{Z3n6[UB4cXSqIEG3MWFCTyC2bzDzeZBxemW|czDj[YxtKHC{b3zp[oVz[XSrb36= NYrlSGxqOjJ3Nk[2NFQ>
8226 MYPGeY5kfGmxbjDBd5NigQ>? MVuxNFAuOTByMDDuUS=> NYHwTHEzOzBibXnu M1\HemROW09? MW\hZ5RqfmG2ZYOgSXJMyqB? MVeyNlU2PjRyOR?=
MM1.S  MWPGeY5kfGmxbjDBd5NigQ>? NF\HfpUyODBvMUCwNEBvVQ>? MlTPN|AhdWmw NF\l[HZFVVOR MX3hZ5RqfmG2ZYOgSXJMyqB? M{mx[|IzPTV4NEC5
8226 NWX1V2xiTnWwY4Tpc44hSXO|YYm= MorXNE42KM7:TR?= NFnIOI0{OCCvaX6= NX73W41zTE2VTx?= MULpcoR2[2W|IHHjeIl3[XSrb36gc4YhWkGIIHHu[EBxcG:|cHjvdplt[XSrb36gc4YhVUWN NVq3TG1{OjJ3NU[0NFk>
MM1.S  MVLGeY5kfGmxbjDBd5NigQ>? NV6xUpVYOC53IN88US=> NUnZZZZtOzBibXnu MXrEUXNQ NIKzTlZqdmS3Y3XzJIFkfGm4YYTpc44hd2ZiUlHGJIFv\CCyaH;zdIhwenmuYYTpc44hd2ZiTVXL MX[yNlU2PjRyOR?=
MCF-7 M13DTmZ2dmO2aX;uJGF{e2G7 M4O4RVUxNzJyMD:1NFAhdk1? NX3MeZVVOzBibXnu M2HVWIRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MmjLNlI1PzZ6NUK=
T47D Mn7TSpVv[3Srb36gRZN{[Xl? NIToToU2OC9{MECvOVAxKG6P NHzjZXE{OCCvaX6= NWW2e|hS\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? MnTuNlI1PzZ6NUK=
MDA-MB-231 NHTuRYNHfW6ldHnvckBCe3OjeR?= NFPLbXA2OC9{MECvOVAxKG6P NHHldoU{OCCvaX6= M1nicoRwe2VvZHXw[Y5l\W62bImgLFUx6oDVNUCwxsBvVSlic4XwdJJme3OnczDwbI9{eGixconsZZRqd25ib3[gRYt1 MorlNlI1PzZ6NUK=
Bcap-37 MUfGeY5kfGmxbjDBd5NigQ>? MVS1NE8zODBxNUCwJI5O M1HVRlMxKG2rbh?= Monz[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MmXNNlI1PzZ6NUK=
MCF-7 NGroVm5CeG:ydH;zbZMhSXO|YYm= NYr0RZYzOjBywrDuUS=> MX[zOkBp NH3uWXBFVVOR NFXRPIxqdmS3Y3XzJIFxd3C2b4Ppdy=> Mn7LNlI1PzZ6NUK=
MDA-MB-231 NVnldFFUSXCxcITvd4l{KEG|c3H5 MkjqNlAxyqCwTR?= NIT3VZQ{PiCq NGjL[|BFVVOR M3XZZYlv\HWlZYOgZZBweHSxc3nz NHfyWHkzOjR5Nki1Ni=>
Bcap-37 M1G1d2Fxd3C2b4Ppd{BCe3OjeR?= MVeyNFDDqG6P MnfjN|YhcA>? Mmq3SG1UVw>? MX7pcoR2[2W|IHHwc5B1d3Orcx?= NImycIwzOjR5Nki1Ni=>
LS174T MUXGeY5kfGmxbjDBd5NigQ>? NEnMVWIyOC9zMECvNVAxOCCwTR?= M3TPSVYhcA>? M3TFUGROW09? M3jYZYlvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> M12wRlIzPDBzMkm0
DLD-1  NUDQNmh7TnWwY4Tpc44hSXO|YYm= Mnn2NVAwOTByL{GwNFAhdk1? MnrsOkBp MnPzSG1UVw>? M4[3ZYlvcGmkaYTzJI1VV1KFMTDhZ5Rqfmm2eTDifUB1cGViZHXwbI9{eGixconsZZRqd25ib3[gV|Yhemmkb4PvcYFtKHC{b4TlbY4> MYWyNlQxOTJ7NB?=
SW480 MVPGeY5kfGmxbjDBd5NigQ>? MlS3NVAwOTByL{GwNFAhdk1? M4fyNFYhcA>? MnfYSG1UVw>? MWHpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu M3Tx[VIzPDBzMkm0
SW-48 NInRNINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMTFOwG0> NWXmOIdIOjJ{N{CyOVc>
HCT-15 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOwcpFnUUN3ME2wMlMh|ryP Moe4NlIzPzB{NUe=
HCT 116 NWfaOZY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnx[5d4UUN3ME2wMlYh|ryP MoDENlIzPzB{NUe=
SW620-R NXjDeoN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFwMzFOwG0> MoH6NlIzPzB{NUe=
SK-CO-1 M4jNb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXoZ5FKSzVyPUKuNUDPxE1? MUiyNlI4ODJ3Nx?=
SW620 M4Didmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;xTWM2OD1zMTFOwG0> Mn3CNlIzPzB{NUe=
BaF3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\HTVUxRTFwNES5JO69VQ>? M3nlRVIzOjJ|NkS1
NIH 3T3 MVPGeY5kfGmxbjDBd5NigQ>? NXO5TJJ{OiEQvF2= NX7S[3FNOThiaB?= M1m1XolvcGmkaYTzJI1VV1KFMjDwbI9{eGixconsZZRqd25ib3[gRYt1KG:wIGPldlQ4OyCjbnSgcXRQWkNzIIDoc5NxcG:{eXzheIlwdiCxZjC0SU1DWDFib36gWIhzOzdxNE[= NHG1eXMzOTh5NkGzNC=>
HCT15 Ml3YSpVv[3Srb36gRZN{[Xl? NETnNoMxNjVxMjFOwG0> MmnqOEBp MXjwdoV3\W62czDTOmsyKHCqb4PwbI9zgWyjdHnvckBw\iC{aXLvd49u[WxicILveIVqdiCVNjDheEBU\XJ{NECvNlQ1KGGwZDDtWG9TSzJicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBifCCVZYK0O|M> MlXLNlE5PzZzM{C=
SW620  M17qemZ2dmO2aX;uJGF{e2G7 NHzpPYcxNjVxMjFOwG0> NGHUPFk1KGh? MnraZoxw[2u|IHHscEB1cHKnZTDtWG9TKG:3dID1eJM> Mm\5NlE5PzZzM{C=

... Click to View More Cell Line Experimental Data

In vivo Administration of PP242 is able to completely inhibit the phosphorylation of Akt at S473 and T308 in fat and liver of mice. PP242 only partially inhibits the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite able to fully inhibit the phosphorylation of 4EBP1 and S6. [2] Oral administration PP242 potently delays the leukemia onset in the mice model, and induces leukemia regression by inhibiting mTORC2 and mTORC1 activation that correlates with loss in cell size. [3] PP242 treatment potently inhibits the growth of 8226 cells in mice. [4]

Protocol

Kinase Assay:[1]
+ Expand

In vitro mTOR (FRAP1) kinase assay:

Recombinant mTOR is incubated with PP242 at 2-fold dilutions over a concentration range of 50-0.001 μM in an assay containing 50 mM HEPES, pH 7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Tween, 10 μM ATP (2.5 μCi of γ-32P-ATP), and 3 μg/mL BSA. Rat recombinant PHAS-1/4EBP1 (2 mg/mL) is used as a substrate. Reactions are terminated by spotting onto nitrocellulose, which is washed with 1 M NaCl/1% phosphoric acid (approximately 6 times, 5-10 minutes each). Sheets are dried and the transferred radioactivity quantitated by phosphorimaging. IC50 value is calculated by fitting the data to a sigmoidal dose-response curve using the Prism software package.
Cell Research:[2]
+ Expand
  • Cell lines: MEFs
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method: Cells are treated with increasing concentrations of PP242 for 72 hours in 96-well plates. After 72 hours of treatment, 10 μL of 440 μM resazurin sodium salt is added to each well, and after 18 hours, the florescence intensity in each well is measured using a top-reading florescent plate reader with excitation at 530 nm and emission at 590 nm.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: Syngeneic (Balbc/J) mice with mouse p190-transformed BM cells to initiate leukemia, and female NSG mice injected (i.v.) with SUP-B15ffLuc cells or human Ph+ leukemia
  • Formulation: Dissolved in PEG400 (Carbowax polyethylene glycol)
  • Dosages: ~60 mg/kg/day
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (197.83 mM)
Ethanol 18 mg/mL (58.37 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 308.34
Formula

C16H16N6O

CAS No. 1092351-67-1
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Do you have any suggestions about potential candidates for vehicles that we could use for in vivo studies?

  • Answer:

    S2218 in the recommended solvent (30% PEG400 + 0.5% Tween80 + 5% Propylene glycol) is a suspension, and this formulation is for oral gavage. For IV injection, this compound can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5mg/ml as a clear solution.

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

Related mTOR Products4

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