Torkinib (PP242)

For research use only. Not for use in humans.

目录号:S2218

Torkinib (PP242) Chemical Structure

CAS No. 1092351-67-1

Torkinib (PP242) 是一种选择性的mTOR抑制剂,在无细胞试验中IC50为8 nM;靶向作用于mTOR复合体,作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ选择性分别高10倍多和100倍。Torkinib (PP242) 可诱导线粒体自噬和凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 749.83 现货
RMB 570.16 现货
RMB 3037.18 现货
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客户使用Selleck生产的Torkinib (PP242)发表文献68篇:

产品安全说明书

mTOR抑制剂选择性比较

生物活性

产品描述 Torkinib (PP242) 是一种选择性的mTOR抑制剂,在无细胞试验中IC50为8 nM;靶向作用于mTOR复合体,作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ选择性分别高10倍多和100倍。Torkinib (PP242) 可诱导线粒体自噬和凋亡。
特性 第一批以mTOR的ATP域为靶点的选择性抑制剂之一。
靶点
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
体外研究

PP242作用于mTOR比作用于其他PI3K家族激酶,比如p110α,p110β,p110γ,p110δ,和DNA-PK(IC50分别为1.96 μM,2.2 μM,1.27 μM,0.102 μM,和0.408 μM),表现出更有效的选择性。PP242对Ret,PKCα,PKCβ,和JAK2表现出一定的抑制活性,而对215种其他蛋白激酶具有显著的选择性。不同于rapamycin,PP242同时抑制mTORC1和 mTORC2。在BT549细胞中,PP242治疗(0.04-10 μM)以剂量依赖的方式抑制Akt,mTOR底物p70S6K,和其下游靶点S6的磷酸化。[1] PP242有效抑制PKCα,IC50 为49 nM。低浓度PP242抑制Akt S473磷酸化,较高浓度部分抑制除S473-P 外的Akt T308-P。PP242作为比rapamycin更有效的mTORC1抑制剂,能够抑制原代MEFs细胞的增殖,以及4EBP1在T36/45和S65上的磷酸化,比rapamycin更有效。通过比rapamycin引起更高水平的4EBP1 和eIF4E结合,PP242有效抑制cap依赖性翻译,而 rapamycin无此作用。[2] PP242有效抑制p190转化的小鼠BM,SUP-B15,和K562细胞增殖,GI50分别为12 nM,90 nM,和85 nM。PP242也会抑制固体肿瘤细胞系,如SKOV3,PC3,786-O,和U87的生长,GI50 分别为0.49 μM,0.19 μM,2.13 μM,和1.57 μM。[3] PP242能够比rapamycin更有效地使多发性骨髓瘤(MM)细胞减少和凋亡。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-p21 M{nKfGZ2dmO2aX;uJGF{e2G7 M3TZ[FUxNTF{NUCgcm0> NGjFUW4zPCCq NEPGd5FFVVOR MV;pcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gV|Yhc2mwYYPlJEh1[XKpZYSgc4YhdVSRUlOxLUBidmRiaYTzJIRwf26|dILlZY0hfGG{Z3X0JJBpd3OyaH:tV|bDqA>? NV\6[HQ1OjZzN{ewOVE>
U87vIII  M4DPd2Z2dmO2aX;uJGF{e2G7 M4nkTVAvODRvMj61JO69VQ>? MnX2NlQhcA>? MnvIbY5pcWKrdIOgcXRQWkNzIHHu[EBuXE:UQ{KgZYN1cX[rdHnld:Kh M2ewclI3OTN2NkG3
U87vIII  MWPGeY5kfGmxbjDBd5NigQ>? M1[xZVIvPS93IN88US=> NWfONY5XOTJiaB?= MmHJbY5pcWKrdIOg[4FxKGOub4PpcochcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NIq5enUzPjF|NE[xOy=>
PC12  NYfWdnZGTnWwY4Tpc44hSXO|YYm= M3PmRlQxyqCwTR?= MVvpcoR2[2W|IHz5d49{d22jbDDibY9o\W6nc3nzJIFv\CCjbHzleolifGWmIN8xMXN[ViCjY3P1cZVt[XSrb39CpC=> Mnn2NlYxODF4MUS=
3T3-L1 M1jobmZ2dmO2aX;uJGF{e2G7 NUXYNZQxOTVizszN MVW0JIg> Moexd5VxeHKnc4Pld{BmgHC{ZYPzbY9vKG:oIITo[UBG\3JzIIDyc5RmcW8EoB?= M{fXTVI2QDF2Nk[y
Rh30 MlfFSpVv[3Srb36gRZN{[Xl? MlTYNUDPxE1? NHO5fnkzKGh? M2HxVolvcGmkaYTzJIJwfGhibWTPVmMyNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCVNluxJIFv\CCvVF;SR|IudWWmaXH0[YQheGixc4Doc5J6dGG2aX;uJI9nKEGtdB?= NGLybI8zPTd4Mk[xPS=>
HT29 M2PYSWZ2dmO2aX;uJGF{e2G7 NETUNIEyKM7:TR?= MVSyJIg> NHjnW5NqdmirYnn0d{Bjd3SqIH3UU3JEOS2vZXTpZZRm\CCyaH;zdIhwenmuYYTpc44hd2ZiU{\LNUBidmRibWTPVmMzNW2nZHnheIVlKHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= M2ThZVI2PzZ{NkG5
Rh30 MoTVSpVv[3Srb36gRZN{[Xl? M1WxZ|Eh|ryP NUO2PJZ5OiCq NY\nU4dHe3WycILld5NmeyC2aHWgZoF{[Wxib4KgTWdHNTFvc4TpcZVt[XSnZDDj[YxtKGGmaHXzbY9v NGjj[XQzPTd4Mk[xPS=>
HT29 MXPGeY5kfGmxbjDBd5NigQ>? NWm1NVFYOSEQvF2= M3PwXVIhcA>? NInYPHF{fXCycnXzd4V{KHSqZTDiZZNidCCxcjDJS2YuOS2|dHnteYxifGWmIHPlcIwh[WSqZYPpc44> MVmyOVc3OjZzOR?=
U87 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Dx[FI2KG6P NUjLcGo3OjRiaB?= NHfiVm1qdmO{ZXHz[ZMhTFWVUEGwJItvd2OtZXSt[I94diCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> NIXVZnIzPTV4OE[2OS=>
AGS NUPJfldXS2WubDDWbYFjcWyrdImgRZN{[Xl? MXKwMVExODBibl2= MkHDNlQwPDhiaB?= NVzlUlhJTE2VTx?= NEjuboNl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MmfvNlUxOzV7NkG=
MKN45 Mn\LR4VtdCCYaXHibYxqfHliQYPzZZk> MXOwMVExODBibl2= NVXucFM3OjRxNEigbC=> MV3EUXNQ NHy1OYRl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MmPRNlUxOzV7NkG=
MKN28 NGXRbFRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYPncWVZOC1zMECwJI5O NE\ZUHozPC92ODDo Mm\sSG1UVw>? MkfS[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MWWyOVA{PTl4MR?=
KATO3 MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGjzSVgxNTFyMECgcm0> MkLTNlQwPDhiaB?= NVfxTYp6TE2VTx?= NFPHdXRl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MYqyOVA{PTl4MR?=
SGC7901 MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NIrORm4xNTFyMECgcm0> NVvOZ3c2OjRxNEigbC=> NUPIVpFWTE2VTx?= MWrk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M4DnTFI2ODN3OU[x
N87 NIXrfYxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFnGVoUxNTFyMECgcm0> Mn35NlQwPDhiaB?= MWTEUXNQ NITyNopl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MnvzNlUxOzV7NkG=
HMEC Mle0R4VtdCCYaXHibYxqfHliQYPzZZk> MUiwMVExODBibl2= NYjEdY5YOjRxNEigbC=> NGGwTXNFVVOR M3G1boRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGTXV3ozPTB|NUm2NS=>
HUVEC Mo\aR4VtdCCYaXHibYxqfHliQYPzZZk> M2OwfFAuOTByMDDuUS=> M2LhPFI1NzR6IHi= Mn7aSG1UVw>? MoTE[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NXLLU25sOjVyM{W5OlE>
MG63 MnfTSpVv[3Srb36gRZN{[Xl? M3jGfFUxNTFyMECgcm0> NX[zcldYOC53IHi= M1\kS4Rwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M37he|I1QDRyMUO0
U2OS  NF75NpRHfW6ldHnvckBCe3OjeR?= MmHpOVAuOTByMDDuUS=> NF;We2QxNjViaB?= NEXwN4dld3OnIHTldIVv\GWwdHz5JEg2OOLCk{GwNFAhdk1rIHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MnK1NlQ5PDBzM{S=
Saos-2  MVLGeY5kfGmxbjDBd5NigQ>? NVXkR49EPTBvMUCwNEBvVQ>? M3zJRlAvPSCq M3ftSYRwe2ViZHXw[Y5l\W62bImgLFUx6oDVMUCwNEBvVSliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> MUeyOFg1ODF|NB?=
Saos-2 NYHwZ493TnWwY4Tpc44hSXO|YYm= MX2xNFAhdk1? MXuwMlUhcA>? MXHwdoV3\W62czDvd5Rmd3OjcnPvcYEh[2WubDDtbYdz[XSrb36= NHfmSnIzPDh2MEGzOC=>
MG63 MkfXRZBweHSxc3nzJGF{e2G7 NYG2cZQ3OTByIH7N MYSzOkBp NGTIO3Fxem:vb4Tld{BieG:ydH;zbZM> MWeyOFg1ODF|NB?=
U2OS  MnL3RZBweHSxc3nzJGF{e2G7 MnX0NVAxKG6P M2PPOVM3KGh? MlnKdJJwdW:2ZYOgZZBweHSxc3nz MU[yOFg1ODF|NB?=
Saos-2  M1Ti[WFxd3C2b4Ppd{BCe3OjeR?= NEPEXY0yODBibl2= NG\lOoc{PiCq Mnq3dJJwdW:2ZYOgZZBweHSxc3nz MkPMNlQ5PDBzM{S=
HT1376 NXq0WXptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:1OWtYUUN3ME2xMlg5KMLzIEGuNUDPxE1? NUTHeHQxOjRyNUS4O|E>
T24 MoG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTFwM{egxtEhOC52IN88US=> M{LCS|I1ODV2OEex
UM-UC-3 MkPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwNkOgxtExNjFizszN NX7rc5dDOjRyNUS4O|E>
DLD-1 M3vaNWNmdGxiVnnhZoltcXS7IFHzd4F6 M4LBcFAuOTByMDDuUS=> MXiyOEBp NH\UVIdqdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUWyN|k6OTF5OR?=
Caco2 MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEj3dlgxNTFyMECgcm0> NF6w[5YzPCCq NXfTZ4szcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MV[yN|k6OTF5OR?=
HT29 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1X0OFAuOTByMDDuUS=> M1;pOVI1KGh? M1PYeIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MoSyNlM6QTFzN{m=
H116 M1nOOWNmdGxiVnnhZoltcXS7IFHzd4F6 M{n5V|AuOTByMDDuUS=> MljKNlQhcA>? M4HsWIlvcGmkaYTzJJRp\SCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWHCb4ZrOjN7OUGxO|k>
Hct-8 NHv4O|JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWrNO5oxOC1zMECwJI5O NXOwfGxVOjRiaB?= NF7qfI1qdmirYnn0d{B1cGViZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX\sNIV3OjN7OUGxO|k>
Colo320 MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUSwMVExODBibl2= NYrPO2kyOjRiaB?= NVrNWnZvcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2DNbFI{QTlzMUe5
Sw948 MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlvpNE0yODByIH7N MoDKNlQhcA>? NW\LfoprcW6qaXLpeJMhfGinIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVnPWXNtOjN7OUGxO|k>
Colo205 M3TrZWNmdGxiVnnhZoltcXS7IFHzd4F6 NW\DR|NFOC1zMECwJI5O MojSNlQhcA>? MXHpcohq[mm2czD0bIUh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MVKyN|k6OTF5OR?=
Colo320 MlHnSpVv[3Srb36gRZN{[Xl? NFG4OmQyKM7:TR?= NHmyO3ExNTJ2IHi= NV\odFhM[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? MonONlM6QTFzN{m=
HT29 MlXSSpVv[3Srb36gRZN{[Xl? NVrkcmg6OSEQvF2= NF3ITIYxNTJ2IHi= NFnKenVi[m:uaYPo[ZMhfGinIGO2V|I{PS9{M{dCpIJ2fCCyYYL0bYFtdHlicnXkeYNmeyC2aHWgOGUuSlBzVEO2M|Q2 NVfPfI5JOjN7OUGxO|k>
Sw948 M3fuUWZ2dmO2aX;uJGF{e2G7 NXL1THhsOSEQvF2= NIXqb3cxNTJ2IHi= NXjWb3J[[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? NYGxcG1EOjN7OUGxO|k>
DLD-1 NHnKfIVHfW6ldHnvckBCe3OjeR?= M2XXRVEh|ryP MnfaNE0zPCCq NWXC[JJn[WKxbHnzbIV{KHSqZTDTOnMzOzVxMkO2xsBjfXRicHHyeIlidGy7IILl[JVk\XNidHjlJFRGNUKSMWSzOk81PQ>? M1vub|I{QTlzMUe5
SW620 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3FTFJKSzVyPUeuPEDPxE1? NHXhZY8zOzV2MkG3PC=>
SW480 NH7LWnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnMXY5CUUN3ME20MlYh|ryP NUD2bZM4OjN3NEKxO|g>
SK-CO-1 NV7LeIFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS2cnh4UUN3ME20JO69VQ>? NVnINnIxOjN3NEKxO|g>
LS-513 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjiXWZxUUN3ME2zMlkh|ryP M4ewS|I{PTR{MUe4
SW1116 NUHpS|BOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTBwOESg{txO MYWyN|U1OjF5OB?=
LS-174T NFvIZ2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmq3TWM2OD1yLki0JO69VQ>? NHXZTWEzOzV2MkG3PC=>
HCT 116 NV;ZWWZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXOTWM2OD1yLkSxJO69VQ>? NHSyTJozOzV2MkG3PC=>
HCT 15 MnvFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwMzFOwG0> NUTCVnVZOjN3NEKxO|g>
COLO 205 NXj4UY1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrLS3J3UUN3ME2wMlI1KM7:TR?= NF60UWMzOzV2MkG3PC=>
HT-29 MmfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zJZmlEPTB;MD6yN{DPxE1? M{m0PVI{PTR{MUe4
COLO 201 NUDBeGpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHrcYdKSzVyPUCuNlMh|ryP NGm0O4QzOzV2MkG3PC=>
Caco-2 NU\ObpVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHsUVNKSzVyPUCuNlIh|ryP MW[yN|U1OjF5OB?=
SW48 NELBV4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDjTWM2OD1yLkC5JO69VQ>? NXvwUIt1OjN3NEKxO|g>
DND-1 NWj0WoVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn2yNE4zPS9yLkWvNUDPxE1? M4XPemROW09? MUjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M3LDSlI{PDh{N{S4
TMD8 NE\IO|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3f5S|AvOjVxMD61M|Eh|ryP NGfZNpZFVVOR NXLmSHdMcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NWmxTYljOjN2OEK3OFg>
Jurkat NGjBWIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVThZpF4OC5{NT:wMlUwOSEQvF2= MkK3SG1UVw>? NVvES45jcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M4rnWlI{PDh{N{S4
KOPT-K1 M1jYU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XPN|AvOjVxMD61M|Eh|ryP MmjNSG1UVw>? MmXqbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXuyN|Q5Ojd2OB?=
TMD7 MkOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[wMlI2NzBwNT:xJO69VQ>? MWDEUXNQ MWHpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmWyNlM1QDJ5NEi=
THP-1 M3PhTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV25W|JUOC5{NT:wMlUwOSEQvF2= NEHGTVdFVVOR MljRbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MXuyN|Q5Ojd2OB?=
786-O MX3GeY5kfGmxbjDBd5NigQ>? NILUd2wxNjFxMD61JO69VQ>? NIX4UWIzPCCq NWPU[HNzTE2VTx?= MWnpcoNz\WG|ZYOgSU1k[WSqZYLpckBuWk6DIHzleoVteyCmb4PlJIRmeGWwZHXueIx6 NXLNbo5QOjNzNEeyOVE>
786-O M2XkXGZ2dmO2aX;uJGF{e2G7 NHLlTpgxNTBwNTFOwG0> MW[yOEBp NYDMOVFGTE2VTx?= MWjy[ZN2dHS|IHnuJIEh\G:|ZTDk[ZBmdmSnboSgbY5kemWjc3WgbY4hTS2lYXTo[ZJqdiCycn;0[YlvKGW6cILld5Nqd28EoB?= MoPMNlMyPDd{NUG=
OCI-AML3 MYDBdI9xfG:|aYOgRZN{[Xl? MYWyMlUh|ryP NVfQXmlzPzJiaB?= NUTWWJFkcW6mdXPld{BieG:ydH;zbZM> MVSyNlgzPjV4NR?=
Jurkat MlLwSpVv[3Srb36gRZN{[Xl? MmTwNVAxNzJyMD:0NFAhdk1? MVixPEBp MXvpcohq[mm2czDtWG9TSzFvZHXw[Y5l\W62IGO2JHMzOzVxMkO2JJBpd3OyaH;yfYxifGmxbh?= NEP3WGEzOjV4Nk[wOC=>
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Jurkat Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHIOFAxdk1? NInINpkzPC92ODDo Mn;ad5lv\XKpaYrlJJdqfGhiMUetRWFIKHSxIIP1dJBz\XO|IHPlcIwheHKxbHnm[ZJifGmxbh?= NUe2WYw5OjJ3Nk[2NFQ>
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MM1.S  M3jETGZ2dmO2aX;uJGF{e2G7 M2LqXFExOC1zMECwJI5O M3fVe|MxKG2rbh?= M2nHTmROW09? MVzhZ5RqfmG2ZYOgSXJMyqB? MkjRNlI2PTZ2MEm=
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MM1.S  MnXYSpVv[3Srb36gRZN{[Xl? NEjXcZoxNjVizszN MXGzNEBucW5? MkjqSG1UVw>? M1np[olv\HWlZYOgZYN1cX[jdHnvckBw\iCUQV[gZY5lKHCqb4PwbI9zgWyjdHnvckBw\iCPRVu= M4OwUlIzPTV4NEC5
MCF-7 MUXGeY5kfGmxbjDBd5NigQ>? MUm1NE8zODBxNUCwJI5O NGn2W3A{OCCvaX6= NGDqUIlld3OnLXTldIVv\GWwdHz5JEg2OOLCk{WwNOKhdk1rIIP1dJBz\XO|ZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfA>? M1HTUVIzPDd4OEWy
T47D MV\GeY5kfGmxbjDBd5NigQ>? MX[1NE8zODBxNUCwJI5O NF\STJo{OCCvaX6= NYnZZWZp\G:|ZT3k[ZBmdmSnboTsfUApPTEkgKO1NFDDqG6PKTDzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBCc3R? Ml61NlI1PzZ6NUK=
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Bcap-37 MYLGeY5kfGmxbjDBd5NigQ>? MWW1NE8zODBxNUCwJI5O MofjN|AhdWmw Mmq3[I9{\S2mZYDlcoRmdnSueTCoOVDjiJN3MEFCpI5OMSC|dYDwdoV{e2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> M3voOVIzPDd4OEWy
MCF-7 M2SySGFxd3C2b4Ppd{BCe3OjeR?= MnXMNlAxyqCwTR?= M33nR|M3KGh? MkHJSG1UVw>? NVTvOGtHcW6mdXPld{BieG:ydH;zbZM> MVOyNlQ4Pjh3Mh?=
MDA-MB-231 NGr2TnNCeG:ydH;zbZMhSXO|YYm= NEDZWJAzODEEoH7N NEPCdnc{PiCq NW\XdmFETE2VTx?= M2Xpd4lv\HWlZYOgZZBweHSxc3nz M2DEUlIzPDd4OEWy
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LS174T MVXGeY5kfGmxbjDBd5NigQ>? Mn3qNVAwOTByL{GwNFAhdk1? MmHQOkBp MlXVSG1UVw>? NHr5NmRqdmirYnn0d{BuXE:UQ{GgZYN1cX[rdImgZpkhfGinIHTldIhwe3Cqb4L5cIF1cW:wIH;mJHM3KHKrYn;zc41idCCycn;0[Ylv NFu3fogzOjRyMUK5OC=>
DLD-1  M3ryU2Z2dmO2aX;uJGF{e2G7 MXmxNE8yODBxMUCwNEBvVQ>? NUHPWoo2PiCq MXvEUXNQ MXPpcohq[mm2czDtWG9TSzFiYXP0bZZqfHliYomgeIhmKGSncHjvd5Bpd3K7bHH0bY9vKG:oIGO2JJJq[m:|b33hcEBxem:2ZXnu Mlr2NlI1ODF{OUS=
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HCT-15 NIPCb|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Lie2lEPTB;MD6zJO69VQ>? M3PwXVIzOjdyMkW3
HCT 116 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYqydIJiUUN3ME2wMlYh|ryP MnfYNlIzPzB{NUe=
SW620-R NFrJbHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTFwMzFOwG0> MXKyNlI4ODJ3Nx?=
SK-CO-1 M3rzTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn1OGl[UUN3ME2yMlEh|ryP MoHrNlIzPzB{NUe=
SW620 M3PmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFzIN88US=> NEL5NW8zOjJ5MEK1Oy=>
BaF3 NUDMPItET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvuS2k2OD1zLkS0PUDPxE1? Mk\NNlIzOjN4NEW=
NIH 3T3 M2jkbmZ2dmO2aX;uJGF{e2G7 M2O0UFIh|ryP M1nKWFE5KGh? NH\l[HNqdmirYnn0d{BuXE:UQ{KgdIhwe3Cqb4L5cIF1cW:wIH;mJGFsfCCxbjDT[ZI1PzNiYX7kJI1VV1KFMTDwbI9{eGixconsZZRqd25ib3[gOGUuSlBzIH;uJHRpejN5L{S2 M2i1PVIyQDd4MUOw
HCT15 Mnn2SpVv[3Srb36gRZN{[Xl? MmO2NE42NzJizszN MoH6OEBp MmH3dJJmfmWwdIOgV|ZMOSCyaH;zdIhwenmuYYTpc44hd2Zicnnic5NwdWGuIIDyc5RmcW5iU{[gZZQhW2W{MkSwM|I1PCCjbnSgcXRQWkN{IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qh[XRiU3XyOFc{ MkDaNlE5PzZzM{C=
SW620  Ml\NSpVv[3Srb36gRZN{[Xl? MoLMNE42NzJizszN NXL4UGozPCCq MWjicI9kc3NiYXzsJJRpemWnIH3UU3Ihd3W2cIX0dy=> M2rOfVIyQDd4MUOw

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-mTOR / mTOR / p-AKT / AKT / p-S6 / S6 / p-4E-BP1 / 4E-BP-1 ; 

PubMed: 23991179     


Each of the cell lines as indicated to the top of the panel were untreated or treated with PP242 (1 μM) for the indicated hours and then examined by western blotting using antibodies against the phosphorylated (p-) and unphosphorylated proteins as indicated to the left of the panel.

23991179
Growth inhibition assay
Cell viability ; 

PubMed: 23991179     


The colorectal carcinoma cell lines as indicated were treated with PP242 in the indicated concentrations and then subjected to cell viability assay. The experiment was repeated three times and the data presented as mean ± SD (standard deviation).

23991179
体内研究 在小鼠脂肪和肝脏中,PP242给药能够完全抑制Akt在S473和T308的磷酸化。PP242仅部分抑制骨骼肌中Akt磷酸化,并且对T308磷酸化的抑制比对S473更有效,尽管其能够完全抑制4EBP1和S6的磷酸化。[2] PP242口服给药有效延缓白血病在小鼠模型中的发病,并通过抑制与细胞大小损失相关的mTORC2和mTORC1活化,诱导白血病消退。[3] PP242治疗有效抑制小鼠体内8226细胞的生长。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

体外mTOR (FRAP1)激酶试验:

重组mTOR与50-0.001 μM浓度范围内连续2倍稀释的PP242在试验缓冲液中进行培养,缓冲液包含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),和3 μg/mL BSA。大鼠重组PHAS-1/4EBP1 (2 mg/mL)用作底物。通过在1 M NaCl/1%磷酸(大约6次,每次5-10分钟)洗涤过的硝酸纤维素上点样终止反应。将板片干燥,转移的放射性通过磷光成像定量。IC50值使用Prism软件包将数据拟合到S形剂量反应曲线进行计算。
细胞实验:[2]
- 合并
  • Cell lines: MEFs
  • Concentrations: 在DMSO中溶解,终浓度为~10 μM
  • Incubation Time: 72小时
  • Method: 细胞用逐渐增加浓度的PP242在96孔板中处理72小时。处理72小时后,将10 μL 440 μM刃天青钠盐加入到每孔中,18小时后,每孔中的荧光强度使用顶端读取的荧光板阅读器在530 nm激发波长和590 nm发射波长下测量。
    (Only for Reference)
动物实验:[3]
- 合并
  • Animal Models: 负荷小鼠p190转染的会引发白血病的BM细胞的同源(Balbc/J)小鼠,和静脉注射SUP-B15ffLuc细胞或人Ph+白血病细胞的雌性小鼠
  • Dosages: ~60 mg/kg/day
  • Administration: 口服强饲
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 61 mg/mL (197.83 mM)
Ethanol 18 mg/mL (58.37 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 308.34
化学式

C16H16N6O

CAS号 1092351-67-1
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

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

  • 回答:

    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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID