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。

価格 在庫  
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 M1K0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7hNE05KM7:TR?= MoPQNlQwPDhxN{KgbC=> MnrDbY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= NHnnSXMzPjJ{NE[4NS=>
SH-SY5Y MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fSeFAuQCEQvF2= MWWyOE81QC95MjDo MV7pcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq NXH2cHhCOjZ{MkS2PFE>
SH-SY5Y  M1XkWmFxd3C2b4Ppd{BCe3OjeR?= M{OwRlEh|ryP NF7zOXcxNjVvMkSgbC=> M3PYeJNmdnOrdHn6[ZMhdmW3cn;icIF{fG:vYTDj[YxteyC2bzDkc5hwenWkaXPpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> MYmyOlIzPDZ6MR?=
G 35 SC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUiwMlA2NTJyIN88US=> NFLhfWQzPC95MjDo MV7EUXNQ MUPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NFe3PYczPjF{MUK1NS=>
G 38 SC NI[0cZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LBdlAvODVvMkCg{txO MUmyOE84OiCq Mm\TSG1UVw>? MnSwbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M4fJNlI3OTJzMkWx
G 40 SC NEDtRnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHQV2UxNjB3LUKwJO69VQ>? NY\QN41GOjRxN{KgbC=> NH:wbnNFVVOR M{H3OIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MonQNlYyOjF{NUG=
G 35 DC MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml32NE4xPS1{MDFOwG0> M13VVFI1Nzd{IHi= MVfEUXNQ MVTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MX[yOlEzOTJ3MR?=
G 38 DC NX62RZlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXjNE4xPS1{MDFOwG0> MmrHNlQwPzJiaB?= NX7rcHFPTE2VTx?= NVr1[IRHcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NIrCSXUzPjF{MUK1NS=>
G 40 DC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFn1WWcxNjB3LUKwJO69VQ>? Ml3oNlQwPzJiaB?= MkHVSG1UVw>? NF\BNmpqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NGXsbnQzPjF{MUK1NS=>
RD NFnZVHFCeG:ydH;zbZMhSXO|YYm= MoD5NU8yNjVxMjFOwG0> M4W4NlczKGh? MYHpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NXmzUYROOjV5NEmzO|g>
TE381.T NX\0XW5oSXCxcITvd4l{KEG|c3H5 NVzoeoFWOS9zLkWvNkDPxE1? NWHRZYN2PzJiaB?= NGTYWndqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? NV\4OphZOjV5NEmzO|g>
RMS13 M4DUbWFxd3C2b4Ppd{BCe3OjeR?= NIHvbVEyNzFwNT:yJO69VQ>? M{fXfFczKGh? MmnSbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> NV\DTI1oOjV5NEmzO|g>
RH30  M37a[mFxd3C2b4Ppd{BCe3OjeR?= Mm\6NU8yNjVxMjFOwG0> M4i3cFczKGh? M3zOfYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy Mnn4NlU4PDl|N{i=
VJ MV;BdI9xfG:|aYOgRZN{[Xl? M1HjZVEwOS53L{Kg{txO MXK3NkBp M2rXUIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M3XUW|I2PzR7M{e4
HS578T M4rI[mNmdGxiVnnhZoltcXS7IFHzd4F6 MWOwMVMh|ryP MV[3NkBp Mn3sbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M2nEZVI2PzJzNEG5
BT549 Mkm3R4VtdCCYaXHibYxqfHliQYPzZZk> MXqwMVMh|ryP NWH4XoZlPzJiaB?= MmPFbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? Mn3hNlU4OjF2MUm=
MDA-MB-231 MoHqR4VtdCCYaXHibYxqfHliQYPzZZk> M3TTcVAuOyEQvF2= NGfsb4E4OiCq MUnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MkPQNlU4OjF2MUm=
MDA-MB-468 MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3vSVlAuOyEQvF2= MnXpO|IhcA>? M1ex[olvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NFn3[HYzPTd{MUSxPS=>
MDA-MB-436 MnrXR4VtdCCYaXHibYxqfHliQYPzZZk> MkWwNE0{KM7:TR?= NWXReGlzPzJiaB?= NVnHfmo4cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4HrbFI2PzJzNEG5
SUM149PT NE[xSVNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NIq3WHIxNTNizszN NFT0OG44OiCq M{jYeolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MmTVNlU4OjF2MUm=
MDA-MB-468 M{S4[mZ2dmO2aX;uJGF{e2G7 MkTYNE4xOS1zMDFOwG0> MmXlNlQhcA>? NGm3enNld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li NHvmVm0zPTd{MUSxPS=>
MDA-MB-231 NFX3dItHfW6ldHnvckBCe3OjeR?= M2juT|AvODFvMUCg{txO NGjFbZYzPCCq MoHk[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? MVOyOVczOTRzOR?=
HS578T M{XrdGZ2dmO2aX;uJGF{e2G7 NGL2T4ExNjBzLUGwJO69VQ>? MXGyOEBp MXrkc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh MorONlU4OjF2MUm=
SW872 NHL5XFRHfW6ldHnvckBCe3OjeR?= MmrnNE4xOS1yLkWg{txO NFzFbHIzPCCq NGq3c4Fz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> M33XVVI1Pjl3NkOy
SW982 MkW4SpVv[3Srb36gRZN{[Xl? M2\TSVAvODFvMD61JO69VQ>? MmTlNlQhcA>? NG\0PIJz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> MX[yOFY6PTZ|Mh?=
SW872 Mnm5RZBweHSxc3nzJGF{e2G7 MWCwMlAyNTBwNTFOwG0> NFrS[mc1QCCq NETCbVVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NWq2TXd6OjR4OUW2N|I>
SW982 M1zzdGFxd3C2b4Ppd{BCe3OjeR?= NFz5WWsxNjBzLUCuOUDPxE1? Mn7QOFghcA>? Mlz4bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MnznNlQ3QTV4M{K=
AGS HG MlHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\EXXY{UUN3ME2wMlY5KMLzIECuNFMyKM7:TR?= MYGyOFU6PzR5OB?=
AGS LG NYr6OGRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;aTWM2OD1yLkC1JOKyKDBwMECxJO69VQ>? MljlNlQ2QTd2N{i=
HGC27 HG M1;sRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfDTWM2OD1yLkO4JOKyKDBwMEKyJO69VQ>? M4TpW|I1PTl5NEe4
HGC27 LG NH\LfFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTBwMEKgxtEhOC5yMESg{txO NWDZT443OjR3OUe0O|g>
MKN45 HG M1LRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HmNGlEPTB;MT6wNUDDuSByLkC1NUDPxE1? MW[yOFU6PzR5OB?=
MKN45 LG MnTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\WTWM2OD1yLki3JOKyKDBwMEOwJO69VQ>? Ml\kNlQ2QTd2N{i=
NUGC4 HG NI\m[mpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TufmlEPTB;MUSuNEDDuSB|LkmxN{DPxE1? MUGyOFU6PzR5OB?=
NUGC4 LG NHPYRoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3EVoQ6UUN3ME2xOE4xKMLzIEWuN|IyKM7:TR?= MkHENlQ2QTd2N{i=
A549 MV7GeY5kfGmxbjDBd5NigQ>? NWTJSnpEOC5{NT:wMlUwOSEQvF2= M4jLZlI1KGh? MWDpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 Mlr6NlQ{PTF2MkW=
H460 NUHlUHNMTnWwY4Tpc44hSXO|YYm= NGjhOmQxNjJ3L{CuOU8yKM7:TR?= MWmyOEBp M37wO4lvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2yrZ3j0cJk> NIjmenkzPDN3MUSyOS=>
H661 MVfGeY5kfGmxbjDBd5NigQ>? NYe4dXBxOC5{NT:wMlUwOSEQvF2= MVKyOEBp M3fkeYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= MXeyOFM2OTR{NR?=
SAS MVPGeY5kfGmxbjDBd5NigQ>? M4PhUVAvOjVxMD61M|Eh|ryP M1LQV|I1KGh? NF35R|JqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= M4LvZ|I1OzVzNEK1
UT5 MWPGeY5kfGmxbjDBd5NigQ>? NGHmU4kxNjJ3L{CuOU8yKM7:TR?= MX[yOEBp MkjRbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MWiyOFM2OTR{NR?=
FaDu MVjGeY5kfGmxbjDBd5NigQ>? M{PK[FAvOjVxMD61M|Eh|ryP MV[yOEBp MkD5bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MWeyOFM2OTR{NR?=
RD MnPSRZBweHSxc3nzJGF{e2G7 NE\MXlYyNzFwNT:yJO69VQ>? M{exelczKGh? MXHEUXNQ Mn\ubY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NYX6fHZPOjN4OES5NlU>
TE671 MYXBdI9xfG:|aYOgRZN{[Xl? NH24ZXEyNzFwNT:yJO69VQ>? M1LadVczKGh? NIDPSnJFVVOR NGTBd3ZqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 M4DndVI{Pjh2OUK1
RH30  NX\WU2l3SXCxcITvd4l{KEG|c3H5 NEXoXI0yNzFwNT:yJO69VQ>? MoLzO|IhcA>? M1vvZmROW09? MlzrbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NYfBT3Y4OjN4OES5NlU>
RMS13 NGT5S2pCeG:ydH;zbZMhSXO|YYm= MoroNU8yNjVxMjFOwG0> MUe3NkBp NX25W|BSTE2VTx?= M1S4Xolv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> M1XpO|I{Pjh2OUK1
SUM149PT NE\hSnNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NF;NcWkxNjNizszN NX;hT4ptPzJiaB?= NH3R[HdmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? M{DmN|I{PjBzMEe0
MDA-MB-468 M2SxbWNmdGxiVnnhZoltcXS7IFHzd4F6 NEPvT4YxNjNizszN M1\BN|czKGh? NXjxSY9W\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| M4C2UVI{PjBzMEe0
MDA-MB-231 NHTERXlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHHpe4kxNjNizszN M1nJblczKGh? M2rCNIVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NED3eZYzOzZyMUC3OC=>
SY5Y MXTGeY5kfGmxbjDBd5NigQ>? NWe1WldrOS53L{KuOU82KM7:TR?= MYOyOEBp M{nDSIlv\HWlZYOgS|HDqGOnbHytZ5lkdGViYYLy[ZN1KGGwZDDhdI9xfG:|aYO= NFGx[4czOzN5OEO0NS=>
SKNBE(2c) MWHGeY5kfGmxbjDBd5NigQ>? NXS2T5RNOS53L{KuOU82KM7:TR?= NXHFO2RuOjRiaB?= Mnf2bY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= MmDBNlM{Pzh|NEG=
RD MWXBdI9xfG:|aYOgRZN{[Xl? MX6zJOK2VQ>? MlLXNVIhcA>? NEmyU4xFVVOR NYDTO3Jte2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> MUKyN|MxODhyOR?=
TP5014 MljERZBweHSxc3nzJGF{e2G7 NXjIe|IyOyEEtV2= MoPzNVIhcA>? M{fvcGROW09? NXLifFZoe2Wwc3n0bZpmeyCURDDj[YxteyC2bzDEU3gucW6mdXPl[EBieG:ydH;zbZM> MW[yN|MxODhyOR?=
HT1080 NWD2XIdoSXCxcITvd4l{KEG|c3H5 MWSzJOK2VQ>? MW[xNkBp MYTEUXNQ NIPicVd{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MVSyN|MxODhyOR?=
A549 NUjVO4NkTnWwY4Tpc44hSXO|YYm= NFHweHkxNTNwMzFOwG0> MkPCO|IhcA>? M3fMS4lv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? M3mxO|I{OjV7NUmx
HCC827 NVfafYV3TnWwY4Tpc44hSXO|YYm= NIHyS|UxNTNwMzFOwG0> MnXyO|IhcA>? NFTXdG9qdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? NFTORWMzOzJ3OUW5NS=>
H3122 M1HIbWZ2dmO2aX;uJGF{e2G7 MVWwMVMvOyEQvF2= NVn0RopCPzJiaB?= NV;x[HkxcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW MkmwNlMzPTl3OUG=
TALL-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f4bVHjiIoQvF2= MkL3O{Bl NFfMVIVl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MX2yN|A{QDJ5Mx?=
HPB-ALL MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LtcFHjiIoQvF2= M3PhbFch\A>? MWrk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NXv4b5lMOjNyM{iyO|M>
DND41 NEf4eVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqx5qCK|ryP NIO5fXg4KGR? NYfEOI9Y\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MorVNlMxOzh{N{O=
SUP-T1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TDR|HjiIoQvF2= NG\DZnE4KGR? MoXP[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MlXiNlMxOzh{N{O=
PEER NUfnVZJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHpOIN1OeLCid88US=> NXzmcldDPyCm NIXjPI9l\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M2ridFI{ODN6Mkez
ALL-SIL MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2x5qCK|ryP M2fpSFch\A>? NWD5OnR1\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MlThNlMxOzh{N{O=
KE37 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf5WJEy6oDLzszN M3jTWFch\A>? M4TCPIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NYnXbINCOjNyM{iyO|M>
Karpas-45 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jncFHjiIoQvF2= NUnFNmdrPyCm M4LxVIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NELvXYgzOzB|OEK3Ny=>
RPMI-8402 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\ZTFHjiIoQvF2= M{LCe|ch\A>? NEDOVJBl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NIWyNo0zOzB|OEK3Ny=>
Jurkat NGXLO4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfjZ3p4OeLCid88US=> NHraS3o4KGR? MYTk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NXLl[pdPOjNyM{iyO|M>
MOLT-4 NID4XndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrENgKBkc7:TR?= MYW3JIQ> MWnk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NFzDeYszOzB|OEK3Ny=>
PF-382 NWTzZ204T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYix5qCK|ryP NVTaUlNWPyCm MV;k[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MmC5NlMxOzh{N{O=
CCRF-CEM MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYex5qCK|ryP M4q5[Fch\A>? M37vTIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NXzlfYQzOjNyM{iyO|M>
LOUCY M13uPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTJS5hOOeLCid88US=> NV\KXZZUPyCm NETtSXpl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MV:yN|A{QDJ5Mx?=
MOLT-16 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoiyNgKBkc7:TR?= MXq3JIQ> NW[0fW1x\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MWmyN|A{QDJ5Mx?=
MM1S MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXpVZNyOC1{IN88US=> NIO4NXYzPCCq NX7CR|d6UUN3ME2wMlUh|ryP MmPDNlI5Ojl{M{S=
NCI-H929 NYLrbJFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTvWGkxNTJizszN NX34TZZQOjRiaB?= Mm\5TWM2OD1yLkK1JO69VQ>? MoTxNlI5Ojl{M{S=
KMS12-BM  M1j1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzuNE0zKM7:TR?= MV:yOEBp MnX5TWM2OO,:nkKg{txO MWiyNlgzQTJ|NB?=
MDA-MB-436 Mn6zSpVv[3Srb36gRZN{[Xl? NV3jS4NSOSEQvF2= M3\WSVI1KGh? MUXy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW M3;PO|IzPDh6NUmw
SUM149PT NIP3b4dHfW6ldHnvckBCe3OjeR?= NHPleJUyKM7:TR?= MV2yOEBp M4XXepJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2S= M1[4T|IzPDh6NUmw
SUM1315MO2 MVTGeY5kfGmxbjDBd5NigQ>? NWDmVoZQOSEQvF2= MVqyOEBp NFf2TW9z\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU MVeyNlQ5QDV7MB?=
HCC1937 Ml7ZSpVv[3Srb36gRZN{[Xl? MnGwNUDPxE1? M1;peVI1KGh? MXvy[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW NGL5cnMzOjR6OEW5NC=>
HCC827 M1G2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Ta[VAuOyEQvF2= NGjycFI4OiCq NInDT|BKSzVyPUCuN{DPxE1? NXfWcJpGOjF{MkC0O|Q>
PC-9  MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2GwUlAuOyEQvF2= NWLiVm9KPzJiaB?= NVrJeJdSUUN3ME2wMlgh|ryP MlfFNlEzOjB2N{S=
LN229 NVXhUGNmTnWwY4Tpc44hSXO|YYm= Mn;GNUDPxE1? MmLyOFghcA>? MWXpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v M3nx[FIyODZ{OUmz
U87 M{G0N2Z2dmO2aX;uJGF{e2G7 NWLH[XprOSEQvF2= NVTGUm9jPDhiaB?= MnPzbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NE\aPHAzOTB4Mkm5Ny=>
U373 NXG3bVhwTnWwY4Tpc44hSXO|YYm= M1[4XlEh|ryP NXW3eZJVPDhiaB?= NEHjb4VqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w MUiyNVA3Ojl7Mx?=
SF767 MXHGeY5kfGmxbjDBd5NigQ>? MoWxNUDPxE1? MkPlOFghcA>? MnSxbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? MmOyNlExPjJ7OUO=
Mel-Juso Mke3R4VtdCCYaXHibYxqfHliQYPzZZk> NX[xR2J[OC5yMfMAl|Ex6oDLzszN MoLaO|IhcA>? NFLh[otqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M{exeVIyODR6N{i1
518A2  M4npVGNmdGxiVnnhZoltcXS7IFHzd4F6 MYmwMlAy6oDVMUFihKnPxE1? M{DLTlczKGh? NVK3OFRzcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MnPWNlExPDh5OEW=
Mel-Juso  M2i2UWZ2dmO2aX;uJGF{e2G7 MnLUNE4xODIkgKOx5qCK|ryP NG[5T40zPCCq MXXzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| NYjpXZI{OjFyNEi3PFU>
518A2 M4fEN2Z2dmO2aX;uJGF{e2G7 MnHZNE4xODIkgKOx5qCK|ryP NI\pRXQzPCCq Mnzod5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= MkXuNlExPDh5OEW=
PC3  MlLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr3Z4VzOjSq NYK5Z5lWT0l3MNMgQUAyODBibl2= MVyyNFU2OTB4MR?=
U87MG M2\1OWZ2dmO2aX;uJGF{e2G7 M3naOlAvOS1zIN88US=> M{TL[VI16oDLaNMg MnrDSG1UVw>? M{fx[olvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p MUixPVY{OzZ6Mx?=
U138MG MoH2SpVv[3Srb36gRZN{[Xl? NWS2cG14OC5zLUGg{txO MX6yOQKBkWkEoB?= NHT4NWNFVVOR M{jsXIlvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p MUCxPVY{OzZ6Mx?=
U118MG MXHGeY5kfGmxbjDBd5NigQ>? MoHONE4yNTFizszN M1nrPFI16oDLaNMg MWjEUXNQ NHPv[|FqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= Mnq3NVk3OzN4OEO=
U87MG Mmr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMUSg{txO NVHOUJRPOTl3OESyNlc>
IGROV-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf4OnM4UUN3ME2wMlA3KM7:TR?= NHfudpYyQTV6NEKyOy=>
DETROIT562 M4XVN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnubItKSzVyPUCuNVMh|ryP M3HtZlE6PTh2MkK3
PC3  M1mzRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn0So1KSzVyPUCuNVAh|ryP NVrJXFRlOTl3OESyNlc>
SKOV-3 NH3HV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETXN3dKSzVyPUCuNVIh|ryP MUexPVU5PDJ{Nx?=
HUVEC M{[5XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfmTWM2OD1yLkC4JO69VQ>? MlzTNVk2QDR{Mke=
UCH-1  Mk\rSpVv[3Srb36gRZN{[Xl? NETUc28xNTVizszN M2e5[olvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NF\CTVIyQTV{OES0NS=>
UCH-1  NWj1PWFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fpZ|AvODFvMUCg{txO M3vDOFYh\A>? M3TZPYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iZH;z[UBl\XCnbnTlcpRtgQ>? Mo[wNVk2Ojh2NEG=
UCH-1  MnyyRZBweHSxc3nzJGF{e2G7 NH\URnQxNjFvMUCg{txO NHnpOm0zPCCq NGLSfoxFVVOR NEDVUnFqdmS3Y3XzJIFxd3C2b4Ppdy=> MWSxPVUzQDR2MR?=

... 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)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related PI3K 阻害剤

  • GDC-0032

    GDC-0032 is a potent, next-generation PI3K inhibitor targeting PI3K alpha.

    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147)

    Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

  • GNE-317

    GNE-317 is a potent, brain-penetrant PI3K inhibitor.

  • PI-3065

    PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.

  • LY294002

    LY294002は、p110α、p110δとp110βのPI3K阻害剤で、IC50 がそれぞれ 0.5 μM、0.57 μM、0.97 μMです。

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA) は選択の自噬とリン酸イノシトール3キナーゼ(キナーゼ)阻害剤、Vps34 と PI3Kγ に作用する時、 IC50 がそれぞれ 25 nM と 60 nM になる。自動食物胞の形成を妨害すること。

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101)は、2.5nMのIC50によるp110δの選択的なPI3KクラスI阻害剤です。

  • Wortmannin

    ワートマニンはミオシン軽鎖キナーゼ(MLCK)のマルチターゲットの阻害剤、IC50がぞれぞれ0.17μMと3nMになる。自動食物胞の形成を妨害すること。

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235, Dactolisib)は競争性的なPI3K、mTOR 阻害剤、 p110α, p110γ, p110δ と p110β を作用すると、 IC50 がぞれぞれ 4 nM, 5 nM, 7 nM と 75 nMになる.

  • BKM120 (NVP-BKM120, Buparlisib)

    BKM120 (NVP-BKM120, Buparlisib)は、p110α、p110β、p110δとp110γの選択的なPI3K阻害剤で、IC50 がそれぞれ 52-99 nM、166 nM、 116 nM、 262 nMです。

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
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ