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

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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 MoWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[wMVgh|ryP NWT5bZBxOjRxNEivO|IhcA>? NEX0SFVqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To M1;DSVI3OjJ2Nkix
SH-SY5Y NWLjXWV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGwMVgh|ryP M4mzW|I1NzR6L{eyJIg> M3\mPIlv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= MnX5NlYzOjR4OEG=
SH-SY5Y  Mnr2RZBweHSxc3nzJGF{e2G7 M{fvclEh|ryP M1zV[VAvPS1{NDDo MXXz[Y5{cXSrenXzJI5mfXKxYnzhd5RwdWFiY3XscJMhfG9iZH;4c5J2[mmlaX6tbY5lfWOnZDDhdI9xfG:|aYO= NH2xW5IzPjJ{NE[4NS=>
G 35 SC M2X6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGwMlA2NTJyIN88US=> NGjpVpMzPC95MjDo NYHacJd3TE2VTx?= NIno[4hqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MkPjNlYyOjF{NUG=
G 38 SC MoTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOwMlA2NTJyIN88US=> M4XQV|I1Nzd{IHi= NXTDSFBGTE2VTx?= NGK5XIVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MUiyOlEzOTJ3MR?=
G 40 SC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjvZnZyOC5yNT2yNEDPxE1? NG\VeXYzPC95MjDo M3jsbmROW09? NYfRb4JrcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MU[yOlEzOTJ3MR?=
G 35 DC Mlf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWwMlA2NTJyIN88US=> MUiyOE84OiCq M4nIZWROW09? NVOwVHpJcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NVPFV25[OjZzMkGyOVE>
G 38 DC MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml33NE4xPS1{MDFOwG0> M2rEdVI1Nzd{IHi= M33vbmROW09? NF7ndllqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NGPGSWYzPjF{MUK1NS=>
G 40 DC MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[2PFAvODVvMkCg{txO MWiyOE84OiCq NXvWVWhpTE2VTx?= MnjvbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MkHUNlYyOjF{NUG=
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RH30  NF7nOVdCeG:ydH;zbZMhSXO|YYm= MYKxM|EvPS9{IN88US=> NE\TeIk4OiCq NXzIRo5HcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? M{\hdFI2PzR7M{e4
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HS578T NGLXcIZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4X5eVAuOyEQvF2= MVm3NkBp MVXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MojhNlU4OjF2MUm=
BT549 NWDWdlQ1S2WubDDWbYFjcWyrdImgRZN{[Xl? NWnlcYh4OC1|IN88US=> M37DN|czKGh? NFjMO2pqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NH\oemQzPTd{MUSxPS=>
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MDA-MB-468 MVXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoTkNE0{KM7:TR?= NELpSpg4OiCq M2nvfYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NEjucFYzPTd{MUSxPS=>
MDA-MB-436 NGizfZJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4HIZlAuOyEQvF2= M2e0SFczKGh? MUXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NXn2blZuOjV5MkG0NVk>
SUM149PT MWHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkjxNE0{KM7:TR?= NUiydmptPzJiaB?= MVPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MWiyOVczOTRzOR?=
MDA-MB-468 MX3GeY5kfGmxbjDBd5NigQ>? MX6wMlAyNTFyIN88US=> Mnq5NlQhcA>? MULkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh M2fhVFI2PzJzNEG5
MDA-MB-231 NFzCOVBHfW6ldHnvckBCe3OjeR?= M3jRfFAvODFvMUCg{txO NEf6[VkzPCCq MlTr[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? NYnnU25iOjV5MkG0NVk>
HS578T MXjGeY5kfGmxbjDBd5NigQ>? M3H1elAvODFvMUCg{txO NGW5V4wzPCCq NYqzUYRG\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MVKyOVczOTRzOR?=
SW872 NHnwXnpHfW6ldHnvckBCe3OjeR?= MmPUNE4xOS1yLkWg{txO MYiyOEBp MljMdoVlfWOnczDBT3QheGixc4Doc5J6dGG2aX;uJEhxSUuWKTDhcoQhPEWEUEGgdIhwe3Cqb4L5cIF1cW:wIDjwOGVDWDFrIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= MVOyOFY6PTZ|Mh?=
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SW982 MnXERZBweHSxc3nzJGF{e2G7 NVfqNm81OC5yMT2wMlUh|ryP Mn72OFghcA>? MlL0bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MWeyOFY6PTZ|Mh?=
AGS HG M{j5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TweWlEPTB;MD62PEDDuSByLkCzNUDPxE1? M{jiclI1PTl5NEe4
AGS LG M1TxZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwMEWgxtEhOC5yMEGg{txO M1jxW|I1PTl5NEe4
HGC27 HG NFXoN3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrLbnhKSzVyPUCuN|ghyrFiMD6wNlIh|ryP NILpeI8zPDV7N{S3PC=>
HGC27 LG MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwMEKgxtEhOC5yMESg{txO MoPrNlQ2QTd2N{i=
MKN45 HG NFLFUmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\KTWM2OD1zLkCxJOKyKDBwMEWxJO69VQ>? NHTFR2UzPDV7N{S3PC=>
MKN45 LG M{W3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP0bo1UUUN3ME2wMlg4KMLzIECuNFMxKM7:TR?= NFvUOZozPDV7N{S3PC=>
NUGC4 HG NXqxRWJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFS2U4VKSzVyPUG0MlAhyrFiMz65NVMh|ryP NFfJ[lYzPDV7N{S3PC=>
NUGC4 LG NV\ZUmp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\rfmtKUUN3ME2xOE4xKMLzIEWuN|IyKM7:TR?= NHX3enQzPDV7N{S3PC=>
A549 NXvvelViTnWwY4Tpc44hSXO|YYm= M3Sz[lAvOjVxMD61M|Eh|ryP NXjWb5ZKOjRiaB?= NIq3SHFqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOuaXfoeIx6 NYfqSnc3OjR|NUG0NlU>
H460 NXfiNYxuTnWwY4Tpc44hSXO|YYm= M1HlXFAvOjVxMD61M|Eh|ryP NWT0Z29uOjRiaB?= M2rKOolvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> NEe2[FczPDN3MUSyOS=>
H661 M13KXmZ2dmO2aX;uJGF{e2G7 M4iy[lAvOjVxMD61M|Eh|ryP MXGyOEBp MWTpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MXOyOFM2OTR{NR?=
SAS MXfGeY5kfGmxbjDBd5NigQ>? MWWwMlI2NzBwNT:xJO69VQ>? MYKyOEBp M2rOV4lvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NYLFXHplOjR|NUG0NlU>
UT5 MnHySpVv[3Srb36gRZN{[Xl? NISwfWgxNjJ3L{CuOU8yKM7:TR?= NG\1cXMzPCCq MWrpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MW[yOFM2OTR{NR?=
FaDu NYDDfmJxTnWwY4Tpc44hSXO|YYm= MnzWNE4zPS9yLkWvNUDPxE1? NHXweHczPCCq NIXCbmlqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= M16zZlI1OzVzNEK1
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RH30  M373bGFxd3C2b4Ppd{BCe3OjeR?= MVqxM|EvPS9{IN88US=> M4nqOFczKGh? MUHEUXNQ MkHUbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NITkb5EzOzZ6NEmyOS=>
RMS13 NYPGZ2dkSXCxcITvd4l{KEG|c3H5 MYixM|EvPS9{IN88US=> MXS3NkBp NGPUXpVFVVOR NY\SOWR4cW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? MoDVNlM3QDR7MkW=
SUM149PT NEHhNJhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVWwMlMh|ryP M{Kx[FczKGh? MnX0[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ MXKyN|YxOTB5NB?=
MDA-MB-468 NVqxT|Z7S2WubDDWbYFjcWyrdImgRZN{[Xl? NXmwZnluOC5|IN88US=> NXPwSItiPzJiaB?= MWnlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> MnjlNlM3ODFyN{S=
MDA-MB-231 MkHGR4VtdCCYaXHibYxqfHliQYPzZZk> MYewMlMh|ryP NHnRc2Y4OiCq M2nr[4VvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? M2PCR|I{PjBzMEe0
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SKNBE(2c) NFPM[2ZHfW6ldHnvckBCe3OjeR?= M{\4V|EvPS9{LkWvOUDPxE1? NWjReXBzOjRiaB?= NYnpXYRNcW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> M33aNlI{Ozd6M{Sx
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TP5014 NWP1SHpXSXCxcITvd4l{KEG|c3H5 NGLxTGw{KML3TR?= NWjvTJlDOTJiaB?= NXuxbYFbTE2VTx?= MVnz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= M1vwb|I{OzByOEC5
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HCC827 NGjrdItHfW6ldHnvckBCe3OjeR?= MVOwMVMvOyEQvF2= MlHXO|IhcA>? MoPDbY5lfWOnczDjc41xdGW2ZTDkc5dvemWpdXzheIlwdiCxZjDwRWtV MknrNlMzPTl3OUG=
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HPB-ALL NV7QOmJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDWNgKBkc7:TR?= NXrVSYF6PyCm M3TVNoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NVHqWWNXOjNyM{iyO|M>
DND41 Mn3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rmZVHjiIoQvF2= NVjYNHJoPyCm NETDUnhl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MmHjNlMxOzh{N{O=
SUP-T1 NHn3VVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjoO2Uy6oDLzszN NYfNUG9bPyCm MU\k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NXOzboZROjNyM{iyO|M>
PEER MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NISxWYoy6oDLzszN NUizZpRkPyCm NFHifXZl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MYSyN|A{QDJ5Mx?=
ALL-SIL NIfubIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2m4dFHjiIoQvF2= Mn22O{Bl M4P2Z4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NH60WGczOzB|OEK3Ny=>
KE37 MknUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWna[4c5OeLCid88US=> NVyxbIxJPyCm Mnv4[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NX7SXZBTOjNyM{iyO|M>
Karpas-45 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInpVmwy6oDLzszN MV[3JIQ> M1:1PIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M2XGNFI{ODN6Mkez
RPMI-8402 M363Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXQOIYy6oDLzszN M37xcFch\A>? Mn7M[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MYCyN|A{QDJ5Mx?=
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MOLT-16 MoDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPWNHNbOeLCid88US=> NFHjVGs4KGR? MV;k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NF63Z5IzOzB|OEK3Ny=>
MM1S MnzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HmN|AuOiEQvF2= MVqyOEBp M4KxcmlEPTB;MD61JO69VQ>? MWmyNlgzQTJ|NB?=
NCI-H929 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TlZVAuOiEQvF2= MYWyOEBp MVXJR|UxRTBwMkWg{txO NVX1TYNSOjJ6MkmyN|Q>
KMS12-BM  NHvuSI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH30e|MxNTJizszN NGnSeVEzPCCq M1HQS2lEPTExvK6yJO69VQ>? MmLxNlI5Ojl{M{S=
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SUM149PT NFXINXBHfW6ldHnvckBCe3OjeR?= NHvMfFAyKM7:TR?= NVXxTnBIOjRiaB?= M{Dm[5Jm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= NHz0[nczOjR6OEW5NC=>
SUM1315MO2 M2DE[2Z2dmO2aX;uJGF{e2G7 MoD2NUDPxE1? NHHIXnczPCCq NHv0cXdz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU MXGyNlQ5QDV7MB?=
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HCC827 M{HmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTsNE0{KM7:TR?= Mn;wO|IhcA>? NWDw[Vg3UUN3ME2wMlMh|ryP NH3JO2QzOTJ{MES3OC=>
PC-9  M1;Sb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMVMh|ryP NIPWRpA4OiCq MUfJR|UxRTBwODFOwG0> NYPBOXg2OjF{MkC0O|Q>
LN229 MUfGeY5kfGmxbjDBd5NigQ>? MVixJO69VQ>? M{HHcFQ5KGh? MYHpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v Mmq2NlExPjJ7OUO=
U87 NGjFd45HfW6ldHnvckBCe3OjeR?= M3XIflEh|ryP MoLsOFghcA>? NXLRSJJUcW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= NHTJTWUzOTB4Mkm5Ny=>
U373 M3TSTmZ2dmO2aX;uJGF{e2G7 NWruXnRWOSEQvF2= MlPDOFghcA>? M1;s[4lv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? MUmyNVA3Ojl7Mx?=
SF767 MmrqSpVv[3Srb36gRZN{[Xl? NELOcpYyKM7:TR?= NVHiXIpiPDhiaB?= MYLpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v NYm5Nno6OjFyNkK5PVM>
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Mel-Juso  Mm[2SpVv[3Srb36gRZN{[Xl? NEPG[3IxNjByMfMAl|HjiIoQvF2= M{XQWVI1KGh? MVvzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| NGHScogzOTB2OEe4OS=>
518A2 MY\GeY5kfGmxbjDBd5NigQ>? NF;xOI0xNjByMfMAl|HjiIoQvF2= NILK[pUzPCCq NVO1ZnFZe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> MniwNlExPDh5OEW=
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U87MG Ml74SpVv[3Srb36gRZN{[Xl? NUHjOZdoOC5zLUGg{txO NYfnSZNkOjUkgJnoxsA> M4fXS2ROW09? M3\UeolvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p NIXhTZAyQTZ|M{[4Ny=>
U138MG M4TpSWZ2dmO2aX;uJGF{e2G7 NWXVVJBqOC5zLUGg{txO Mmj1NlTjiImqwrC= M{nwemROW09? MoTWbY5pcWKrdIOgVGk{Uy2vZXTpZZRm\CC|aXfuZYxqdmd? NHv2RVYyQTZ|M{[4Ny=>
U118MG Mme0SpVv[3Srb36gRZN{[Xl? NF3VS2oxNjFvMTFOwG0> NUHKfpFWOjUkgJnoxsA> NXvwcY17TE2VTx?= NXO5T2pPcW6qaXLpeJMhWEl|Sz3t[YRq[XSnZDDzbYdv[Wyrbne= NWr2cWh1OTl4M{O2PFM>
U87MG NXT1NGdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfINXNjUUN3ME2wMlE1KM7:TR?= M3r1Z|E6PTh2MkK3
IGROV-1 NFrnd2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXGT5VzUUN3ME2wMlA3KM7:TR?= NX2zeJp6OTl3OESyNlc>
DETROIT562 Mk\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwMUOg{txO M{TlZVE6PTh2MkK3
PC3  M1zNRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XqRWlEPTB;MD6xNEDPxE1? MV[xPVU5PDJ{Nx?=
SKOV-3 MkDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwMUKg{txO MXSxPVU5PDJ{Nx?=
HUVEC MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vzOGlEPTB;MD6wPEDPxE1? Ml3PNVk2QDR{Mke=
UCH-1  M1;LOmZ2dmO2aX;uJGF{e2G7 MYmwMVUh|ryP M3\SNYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MXexPVUzQDR2MR?=
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UCH-1  NULGWJVZSXCxcITvd4l{KEG|c3H5 NFzoNIYxNjFvMUCg{txO MVOyOEBp NUexSFNwTE2VTx?= NV;FVnJ[cW6mdXPld{BieG:ydH;zbZM> NVnJU5NbOTl3Mki0OFE>

... 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]-

文献中の引用 (21)

技術サポート&よくある質問(FAQ)

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最近チェックしたアイテム

Tags: PI-103を買う | PI-103供給者 | PI-103を購入する | PI-103費用 | PI-103生産者 | オーダーPI-103 | PI-103代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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