PI-103

PI-103は、強力な、細胞透過性、ATP競争的クラスI PI3K阻害剤で、DNA-PK、 p110α、 mTORC1、 PI3-KC2β、 p110δ、 mTORC2、 p110β、p110γ に作用すると、IC50 がそれぞれ 2 nM、 8 nM、 20 nM、26 nM、 48 nM、 83 nM、 88 nM 、150 nMになる。

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USD 168 あり
USD 185 あり
USD 340 あり
USD 466 あり

PI-103 化学構造
分子量: 348.36

高品質保証

カスタマーフィードバック(4)

Quality Control & MSDS

製品説明

  • Compare PI3K Inhibitors
    PI3K製品生物活性の比較
  • 研究分野
  • PI-103のメカニズム

製品の説明

生物活性

製品説明 PI-103は、強力な、細胞透過性、ATP競争的クラスI PI3K阻害剤で、DNA-PK、 p110α、 mTORC1、 PI3-KC2β、 p110δ、 mTORC2、 p110β、p110γ に作用すると、IC50 がそれぞれ 2 nM、 8 nM、 20 nM、26 nM、 48 nM、 83 nM、 88 nM 、150 nMになる。
ターゲット p110α p110β p110δ p110γ mTOR DNA-PK
IC50 2 nM 3 nM 3 nM 15 nM 30 nM 23 nM [3]
In vitro試験 PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. [1] PI-103 inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. [2] In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. PI-103 inhibits p110α >200-fold more potently than p110β. PI-103 also potently blocks production of PI(3,4)P2 and PIP3 in adipocytes and PIP3 in myotubes. [2] PI-103 inhibits phosphorylation of Akt with an IC95 100-fold lower than that for LY294002. Strikingly, PI-103 completely protects animals from insulin-stimulated decline in blood glucose. PI-103 has additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SK-N-BE NF34OVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHS2NpcxNThizszN MXmyOE81QC95MjDo NWP0Uog5cW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> NUXhVFFwOjZ{MkS2PFE>
SH-SY5Y Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrTNE05KM7:TR?= MXWyOE81QC95MjDo NH3nVFdqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To MY[yOlIzPDZ6MR?=
SH-SY5Y  MoXERZBweHSxc3nzJGF{e2G7 MonKNUDPxE1? NYOyTpZJOC53LUK0JIg> M1jESpNmdnOrdHn6[ZMhdmW3cn;icIF{fG:vYTDj[YxteyC2bzDkc5hwenWkaXPpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> M2jmflI3OjJ2Nkix
G 35 SC M1f1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3H3U|AvODVvMkCg{txO M{HMXFI1Nzd{IHi= NXjKU4VnTE2VTx?= MXjpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 Mo\jNlYyOjF{NUG=
G 38 SC Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nxZ|AvODVvMkCg{txO MYSyOE84OiCq Ml\ISG1UVw>? MnPZbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M4LuVFI3OTJzMkWx
G 40 SC NVXhb2FWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXwNE4xPS1{MDFOwG0> Moe5NlQwPzJiaB?= MW\EUXNQ NEjLO21qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MXqyOlEzOTJ3MR?=
G 35 DC MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrmOFYxNjB3LUKwJO69VQ>? MnX3NlQwPzJiaB?= MWXEUXNQ MlP1bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MnnFNlYyOjF{NUG=
G 38 DC NEfEOGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjuPG5lOC5yNT2yNEDPxE1? MWmyOE84OiCq NGLWXmlFVVOR MofEbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NIfZVm0zPjF{MUK1NS=>
G 40 DC MoHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PvUFAvODVvMkCg{txO NUfVNJcyOjRxN{KgbC=> MX\EUXNQ NFf1UnpqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NVK4ZZV1OjZzMkGyOVE>
RD MUHBdI9xfG:|aYOgRZN{[Xl? M2ToTFEwOS53L{Kg{txO NGjtRoc4OiCq M2X6dIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy MWqyOVc1QTN5OB?=
TE381.T NIfTeIpCeG:ydH;zbZMhSXO|YYm= NUSxTXc4OS9zLkWvNkDPxE1? MVW3NkBp MnnPbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> MXKyOVc1QTN5OB?=
RMS13 M{jocGFxd3C2b4Ppd{BCe3OjeR?= Mn;oNU8yNjVxMjFOwG0> NH3Zepg4OiCq NYf0WFIzcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NFvZN|kzPTd2OUO3PC=>
RH30  MYPBdI9xfG:|aYOgRZN{[Xl? M3j1NVEwOS53L{Kg{txO MXq3NkBp MoDSbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> NG\sflIzPTd2OUO3PC=>
VJ NH3iNFlCeG:ydH;zbZMhSXO|YYm= MYSxM|EvPS9{IN88US=> NUPXRphsPzJiaB?= MVLpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> MUWyOVc1QTN5OB?=
HS578T MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M13ybFAuOyEQvF2= MkLMO|IhcA>? M37vfYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NG\OPIEzPTd{MUSxPS=>
BT549 NIGzSYVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYHRcY14OC1|IN88US=> M2XnbVczKGh? MkTkbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MmWyNlU4OjF2MUm=
MDA-MB-231 MlLlR4VtdCCYaXHibYxqfHliQYPzZZk> MWmwMVMh|ryP M4[5ZlczKGh? M37z[IlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MYeyOVczOTRzOR?=
MDA-MB-468 NXLITYFZS2WubDDWbYFjcWyrdImgRZN{[Xl? M3HFWlAuOyEQvF2= MWG3NkBp NHXTU5VqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NH7v[mszPTd{MUSxPS=>
MDA-MB-436 MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M33YUlAuOyEQvF2= MWS3NkBp NVS3bHZtcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NGHncXAzPTd{MUSxPS=>
SUM149PT NXv0WlJLS2WubDDWbYFjcWyrdImgRZN{[Xl? NHj5[FIxNTNizszN MWC3NkBp MVLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFnyRWYzPTd{MUSxPS=>
MDA-MB-468 M162S2Z2dmO2aX;uJGF{e2G7 MWWwMlAyNTFyIN88US=> NWTVNGNJOjRiaB?= MmDm[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? NUj6S4lYOjV5MkG0NVk>
MDA-MB-231 NX:xcnExTnWwY4Tpc44hSXO|YYm= MV[wMlAyNTFyIN88US=> MWqyOEBp M1y3VIRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? M4XHd|I2PzJzNEG5
HS578T NI\2XXFHfW6ldHnvckBCe3OjeR?= MlTzNE4xOS1zMDFOwG0> M1\zWlI1KGh? M3LL[4Rwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? NEjYe4UzPTd{MUSxPS=>
SW872 MnfuSpVv[3Srb36gRZN{[Xl? Ml\4NE4xOS1yLkWg{txO NWHNUXZ[OjRiaB?= NWrMPXh7emWmdXPld{BCU1RicHjvd5Bpd3K7bHH0bY9vKCiyQVvULUBidmRiNFXCVFEheGixc4Doc5J6dGG2aX;uJEhxPEWEUEGpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyxsA> MXSyOFY6PTZ|Mh?=
SW982 MV7GeY5kfGmxbjDBd5NigQ>? MWSwMlAyNTBwNTFOwG0> MojUNlQhcA>? Mm\6doVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= MmH6NlQ3QTV4M{K=
SW872 NGTUc3dCeG:ydH;zbZMhSXO|YYm= NXTCd5F1OC5yMT2wMlUh|ryP NF:y[HA1QCCq MnrjbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MnPGNlQ3QTV4M{K=
SW982 NVXqOWN6SXCxcITvd4l{KEG|c3H5 NXz2O5V3OC5yMT2wMlUh|ryP NHvycm41QCCq NEXMSlRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NFvhOIMzPDZ7NU[zNi=>
AGS HG NXnzTnBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwNkigxtEhOC5yM{Gg{txO M{f5ZVI1PTl5NEe4
AGS LG NVTwOHpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVW1ZXg{UUN3ME2wMlA2KMLzIECuNFAyKM7:TR?= MVSyOFU6PzR5OB?=
HGC27 HG NWjSNlhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rmbmlEPTB;MD6zPEDDuSByLkCyNkDPxE1? M2nVWFI1PTl5NEe4
HGC27 LG NFzYV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXPTWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? MmjVNlQ2QTd2N{i=
MKN45 HG MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv5fFNKSzVyPUGuNFEhyrFiMD6wOVEh|ryP MkD3NlQ2QTd2N{i=
MKN45 LG NUXnbWJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnmdINKSzVyPUCuPFchyrFiMD6wN|Ah|ryP NIXHPGQzPDV7N{S3PC=>
NUGC4 HG MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\nfVdKSzVyPUG0MlAhyrFiMz65NVMh|ryP NIOySoYzPDV7N{S3PC=>
NUGC4 LG NWW3fWFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M136cmlEPTB;MUSuNEDDuSB3LkOyNUDPxE1? MkfBNlQ2QTd2N{i=
A549 NYK1XHFDTnWwY4Tpc44hSXO|YYm= MUmwMlI2NzBwNT:xJO69VQ>? Moq1NlQhcA>? NGO5cYhqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOuaXfoeIx6 MXiyOFM2OTR{NR?=
H460 MYDGeY5kfGmxbjDBd5NigQ>? NYP2OJJiOC5{NT:wMlUwOSEQvF2= M{j6UFI1KGh? MoTLbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> NYDxc3FLOjR|NUG0NlU>
H661 NYPLVYdWTnWwY4Tpc44hSXO|YYm= NVjHN4NWOC5{NT:wMlUwOSEQvF2= MkTYNlQhcA>? M2DNOolvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NY\GNoNkOjR|NUG0NlU>
SAS MnjxSpVv[3Srb36gRZN{[Xl? NHXYfHYxNjJ3L{CuOU8yKM7:TR?= Mnn6NlQhcA>? MoS3bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NWD1[mc5OjR|NUG0NlU>
UT5 MYDGeY5kfGmxbjDBd5NigQ>? NGDn[XIxNjJ3L{CuOU8yKM7:TR?= NWPDWWwxOjRiaB?= NYfjWmV6cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NXj1fVRDOjR|NUG0NlU>
FaDu MV3GeY5kfGmxbjDBd5NigQ>? MnzrNE4zPS9yLkWvNUDPxE1? MWqyOEBp MofSbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MWqyOFM2OTR{NR?=
RD Mk[1RZBweHSxc3nzJGF{e2G7 NFnCRWQyNzFwNT:yJO69VQ>? NFzRdIE4OiCq NWrZSHlXTE2VTx?= NWKydVB[cW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? MXqyN|Y5PDl{NR?=
TE671 MmPoRZBweHSxc3nzJGF{e2G7 MXWxM|EvPS9{IN88US=> MlXBO|IhcA>? NHzScllFVVOR M1uzT4lv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> NWLEdIxLOjN4OES5NlU>
RH30  Mmi5RZBweHSxc3nzJGF{e2G7 NXXldJV6OS9zLkWvNkDPxE1? MWq3NkBp NFfFOmJFVVOR MkjCbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NXrIcm9tOjN4OES5NlU>
RMS13 M{i2Z2Fxd3C2b4Ppd{BCe3OjeR?= MV[xM|EvPS9{IN88US=> MX[3NkBp NYjkenNHTE2VTx?= M2C2eolv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> NH;pWXMzOzZ6NEmyOS=>
SUM149PT MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkXVNE4{KM7:TR?= NUPxe|BiPzJiaB?= M2nBboVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NGTLSVEzOzZyMUC3OC=>
MDA-MB-468 MkDGR4VtdCCYaXHibYxqfHliQYPzZZk> M1:zbVAvOyEQvF2= MYi3NkBp MYnlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> MnXZNlM3ODFyN{S=
MDA-MB-231 MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGLWV5oxNjNizszN M4CwPFczKGh? MYDlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> M4fEWVI{PjBzMEe0
SY5Y NGLuZWJHfW6ldHnvckBCe3OjeR?= MnrJNU42NzJwNT:1JO69VQ>? MWWyOEBp M4T1[Ilv\HWlZYOgS|HDqGOnbHytZ5lkdGViYYLy[ZN1KGGwZDDhdI9xfG:|aYO= NH[5T2MzOzN5OEO0NS=>
SKNBE(2c) Ml2ySpVv[3Srb36gRZN{[Xl? MoDiNU42NzJwNT:1JO69VQ>? M3HuS|I1KGh? NUnyOoNUcW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> NFztfYczOzN5OEO0NS=>
RD NGfsWmJCeG:ydH;zbZMhSXO|YYm= NFzLRZI{KML3TR?= NYTYflN1OTJiaB?= M4DCdWROW09? MWXz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NWnNPVNEOjN|MEC4NFk>
TP5014 NHr4T5NCeG:ydH;zbZMhSXO|YYm= M1rZblMhyrWP M1T0TlEzKGh? M{nTRWROW09? NFfFcVF{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MX6yN|MxODhyOR?=
HT1080 MlOxRZBweHSxc3nzJGF{e2G7 NXTmVllwOyEEtV2= MnvyNVIhcA>? MYrEUXNQ MWHz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NIPNNZMzOzNyMEiwPS=>
A549 M1;4O2Z2dmO2aX;uJGF{e2G7 MUOwMVMvOyEQvF2= M2LZSFczKGh? M4\ZU4lv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? M2joN|I{OjV7NUmx
HCC827 MonjSpVv[3Srb36gRZN{[Xl? M3LYW|AuOy5|IN88US=> MXm3NkBp NIXPOXJqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? NV:yU2ZbOjN{NUm1PVE>
H3122 MWHGeY5kfGmxbjDBd5NigQ>? NYXWOVltOC1|LkOg{txO MYi3NkBp NVXXcYRUcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NHmyfIMzOzJ3OUW5NS=>
TALL-1 Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvQNgKBkc7:TR?= NXPlclNzPyCm NV\xfWRj\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NWTieZJHOjNyM{iyO|M>
HPB-ALL NVrqTng1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW4[pUxOeLCid88US=> M4T4U|ch\A>? MnrJ[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MnmyNlMxOzh{N{O=
DND41 NV\JZVBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3y5XlHjiIoQvF2= M2\YW|ch\A>? NGDHZYhl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M3T1NFI{ODN6Mkez
SUP-T1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn61NgKBkc7:TR?= NWLoWYN6PyCm M{ftW4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M1PLS|I{ODN6Mkez
PEER MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Lze|HjiIoQvF2= NXfLdWJ4PyCm M4LROoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M2iwNFI{ODN6Mkez
ALL-SIL M3HaXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XZOVHjiIoQvF2= Ml;FO{Bl M16zdIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MmDWNlMxOzh{N{O=
KE37 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:0NgKBkc7:TR?= MlWxO{Bl MmfN[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MkTqNlMxOzh{N{O=
Karpas-45 NGm1dZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHpNgKBkc7:TR?= MVi3JIQ> MonH[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M2XMfVI{ODN6Mkez
RPMI-8402 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\OTGlqOeLCid88US=> M4jISVch\A>? MYjk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NI\FUoUzOzB|OEK3Ny=>
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MM1S NYf3XoRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j4XlAuOiEQvF2= MUKyOEBp NUTpbYFqUUN3ME2wMlUh|ryP MV[yNlgzQTJ|NB?=
NCI-H929 NFnvU3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13w[FAuOiEQvF2= MYmyOEBp M4jmWGlEPTB;MD6yOUDPxE1? M2nkZlIzQDJ7MkO0
KMS12-BM  NYrMd4dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M161cVAuOiEQvF2= MoqxNlQhcA>? M1zkbWlEPTExvK6yJO69VQ>? M4jSZlIzQDJ7MkO0
MDA-MB-436 MoDNSpVv[3Srb36gRZN{[Xl? MoDMNUDPxE1? NVXLW4I1OjRiaB?= M3;YRZJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= NGnjN|IzOjR6OEW5NC=>
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SUM1315MO2 NVPWbXVvTnWwY4Tpc44hSXO|YYm= NYjJOZBJOSEQvF2= NF;we24zPCCq M{fzZpJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= NVvu[HRKOjJ2OEi1PVA>
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PC-9  MoHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nQfFAuOyEQvF2= MlPYO|IhcA>? NIK2V|ZKSzVyPUCuPEDPxE1? NH\TXokzOTJ{MES3OC=>
LN229 Mn;6SpVv[3Srb36gRZN{[Xl? NF;JSnYyKM7:TR?= MWi0PEBp MoD3bY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NXfLcXl3OjFyNkK5PVM>
U87 MWHGeY5kfGmxbjDBd5NigQ>? NHK0NXoyKM7:TR?= M1LSO|Q5KGh? MUDpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v NHy4WpgzOTB4Mkm5Ny=>
U373 M{ew[WZ2dmO2aX;uJGF{e2G7 NVzvZ48{OSEQvF2= NVP3eIJtPDhiaB?= NH71elJqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w NVL6[YhkOjFyNkK5PVM>
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518A2  NFrNNYtE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkS1NE4xOeLCk{Gw5qCK|ryP MXe3NkBp NG\RNYVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NFL6VoszOTB2OEe4OS=>
Mel-Juso  M{nCbmZ2dmO2aX;uJGF{e2G7 NYTrbXZ5OC5yMEJihLMy6oDLzszN M3HMV|I1KGh? NXn4V|FWe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> MYCyNVA1QDd6NR?=
518A2 NHfwN5FHfW6ldHnvckBCe3OjeR?= MV:wMlAxOeLCk{JihKnPxE1? NX7TTXhVOjRiaB?= MlzEd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= M1PWNlIyODR6N{i1
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U87MG M2q1c2Z2dmO2aX;uJGF{e2G7 NGH3[ZQxNjFvMTFOwG0> NYnm[YNzOjUkgJnoxsA> MlHxSG1UVw>? M13BNIlvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p MUCxPVY{OzZ6Mx?=
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U118MG M2DkOWZ2dmO2aX;uJGF{e2G7 MnPKNE4yNTFizszN M17qfFI16oDLaNMg NY\tXlJNTE2VTx?= M2\pV4lvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p MmPRNVk3OzN4OEO=
U87MG Ml:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPXSHVUUUN3ME2wMlE1KM7:TR?= NEjwenAyQTV6NEKyOy=>
IGROV-1 NF7ITZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3iTWltUUN3ME2wMlA3KM7:TR?= NV3mRWZnOTl3OESyNlc>
DETROIT562 NV\1N3ZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHkTWM2OD1yLkGzJO69VQ>? Mm\iNVk2QDR{Mke=
PC3  MnG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvIRnFKSzVyPUCuNVAh|ryP NVWwdWx4OTl3OESyNlc>
SKOV-3 M1W3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\IO2lEPTB;MD6xNkDPxE1? M1Hwc|E6PTh2MkK3
HUVEC MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzmUGZjUUN3ME2wMlA5KM7:TR?= NEXkUFcyQTV6NEKyOy=>
UCH-1  MkL4SpVv[3Srb36gRZN{[Xl? MYCwMVUh|ryP NWLrPYVHcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDic5RpKEGNVDDhcoQhdVSRUjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M3nVfFE6PTJ6NESx
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... Click to View More Cell Line Experimental Data

In vivo試験 When tumors reach 50-100 mm3, animals are randomized and treated with vehicle or PI-103. PI-103 exhibits significant activity, decreasing average tumor size by 4-fold after 18 days. [2] Mice treated with PI-103 have no obvious signs of toxicity premorbidly (based on body weight, food and water intake, activity, and general exam) or at necropsy. Treated tumors display decreased levels of phosphorylated Akt and S6, consistent with blockade of p110α and mTOR. PI-103 treatment is cytostatic to glioma xenografts. [2]
臨床試験
特集 The first potent, synthetic mTOR inhibitor.

プロトコル (参考用のみ)

キナーゼアッセイ: [3]

Enzyme Assays Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software.

細胞アッセイ: [2]

細胞株 U87MG cells
濃度 0.5 μM
反応時間 24 hours
実験の流れ U87MG cells are treated with PI-103 for 24 hours. Cell death is quantified by colorimetric determination of LDH activity using a cytotoxicity detection kit. Percentage of cell death (mean of three 12-well plates per experimental point) is calculated [(experimental value- low control)/(high control -low control) × 100], where the low-control cells are DMSO treated and high-control cells are Triton treated (1% Triton X-100, 30 min, 37 °

動物実験: [2]

動物モデル 6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
製剤 50% DMSO
投薬量 5 mg/kg
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download PI-103 SDF
分子量 348.36
化学式

C19H16N4O3

CAS No. 371935-74-9
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 24 mg/mL (68.89 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 Phenol, 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-

カスタマーフィードバック (4)


Click to enlarge
Rating
Source Mol Carcinog, 2012, 52, 667-75 . PI-103 purchased from Selleck
Method Western blot
Cell Lines MCF7 cells
Concentrations 0-1 μM
Incubation Time 24 h
Results In BRCA1-KD MCF7 cells, treatment of PI-103, a PI3K/mTOR inhibitor, abolished phosphorylation of AKT and its substrate GSK3b, in a dose dependent manner (Figure A). Treatment of PI-103 reduced the phosphorylation of AKT in all BRCA1 mutant breast cancer cells tested (Figure B). Phosphorylations of downstream targets of AKT, such as phospho-GSK3b (S9) and phospho-BAD(S112) were also reduced by PI-103 treatment. Phosphorylation of mTOR at S2448, which is also known to be phosphorylated by AKT, was also reduced by PI-103 resulting in reduced phosphorylation of S6 ribosomal protein at S235/236 (Figure B). The effect of PI-103 was much more potent than LY294002 in MDA-MB-436 cells (Figure B)

Click to enlarge
Rating
Source Mol Carcinog, 2012, ahead of print. PI-103 purchased from Selleck
Method MTT assay
Cell Lines MCF7 cells
Concentrations 0.01-1 μM
Incubation Time 48 h
Results Knockdown of BRCA1 can sensitize the MCF7 cells to Perifosine in a dose-dependent manner (Figure A). BRCA1-KD also sensitizes the MCF7 cells to dual PI3K/mTOR inhibitors, such as PI-103 or BEZ235 (Figure B, D). Another inhibitor, PIK-75 which specifically inhibits PI3Ka and PI3Kg, but not mTOR, also showed similar effects on proliferation of BRCA1-KD MCF7 cells (Figure C).

Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. PI-103 purchased from Selleck
Method Western blot
Cell Lines Breast cancer cells
Concentrations 0-1 nM
Incubation Time 24 h
Results PI-103 treatment resulted in a reduction of Akt phosphorylation in Breast cancer cells.

Click to enlarge
Rating
Source Saraswati Sukumar of Johns Hopkins University School of Medicine, PI-103 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations
Incubation Time 1 h
Results PI-103 treatment resulted in a reduction of Akt phosphorylation in T47D cells.

文献中の引用 (21)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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