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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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 M1jMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj1eYYxNThizszN NH[yUHozPC92OD:3NkBp MorIbY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= NELjSFYzPjJ{NE[4NS=>
SH-SY5Y MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7tc|VIOC16IN88US=> M1nvUlI1NzR6L{eyJIg> MmfibY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= MXuyOlIzPDZ6MR?=
SH-SY5Y  M{fJcmFxd3C2b4Ppd{BCe3OjeR?= NXTOcGh2OSEQvF2= M4rH[|AvPS1{NDDo MX7z[Y5{cXSrenXzJI5mfXKxYnzhd5RwdWFiY3XscJMhfG9iZH;4c5J2[mmlaX6tbY5lfWOnZDDhdI9xfG:|aYO= NEHSVXUzPjJ{NE[4NS=>
G 35 SC NIP5UYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvJNE4xPS1{MDFOwG0> M1v3OVI1Nzd{IHi= M2f6[2ROW09? NHXJfYdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NHy4fHkzPjF{MUK1NS=>
G 38 SC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vvOFAvODVvMkCg{txO MYGyOE84OiCq NFrWTJFFVVOR M{K0ZolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NHPSVZMzPjF{MUK1NS=>
G 40 SC M3:wR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nDclAvODVvMkCg{txO NIq5XWgzPC95MjDo NIPneYtFVVOR M2HRNIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MlLiNlYyOjF{NUG=
G 35 DC MlnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\EWnYxNjB3LUKwJO69VQ>? M{HyfVI1Nzd{IHi= MYTEUXNQ M3:z[YlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NXTHU4tGOjZzMkGyOVE>
G 38 DC NGnKR4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i0UFAvODVvMkCg{txO MkPXNlQwPzJiaB?= NH7pfldFVVOR NGPUfGdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MmTWNlYyOjF{NUG=
G 40 DC NYX6WmxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjKWIsxNjB3LUKwJO69VQ>? MoPjNlQwPzJiaB?= M3PCbGROW09? M4THdIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NX3tcGdWOjZzMkGyOVE>
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BT549 M{PGN2NmdGxiVnnhZoltcXS7IFHzd4F6 NUfVT5F5OC1|IN88US=> M2X0e|czKGh? MV7pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NWTsU3RWOjV5MkG0NVk>
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MDA-MB-468 NXvH[2ZoTnWwY4Tpc44hSXO|YYm= NUPTUpA2OC5yMT2xNEDPxE1? MYSyOEBp NXK0TFlJ\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MlPXNlU4OjF2MUm=
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HS578T MWLGeY5kfGmxbjDBd5NigQ>? MVKwMlAyNTFyIN88US=> MkTsNlQhcA>? NU\PeY9m\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MWCyOVczOTRzOR?=
SW872 NWrEVohKTnWwY4Tpc44hSXO|YYm= NUXHXGp7OC5yMT2wMlUh|ryP MUmyOEBp MXPy[YR2[2W|IFHLWEBxcG:|cHjvdplt[XSrb36gLJBCU1RrIHHu[EA1TUKSMTDwbI9{eGixconsZZRqd25iKIC0SWJROSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MV6yOFY6PTZ|Mh?=
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SW872 Mo\xRZBweHSxc3nzJGF{e2G7 M4T3[|AvODFvMD61JO69VQ>? NWnXU5lFPDhiaB?= MnnubY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MkPsNlQ3QTV4M{K=
SW982 NGjRUYlCeG:ydH;zbZMhSXO|YYm= NES4WGYxNjBzLUCuOUDPxE1? MmPFOFghcA>? MV7pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NVvZNXZrOjR4OUW2N|I>
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AGS LG NIDwO|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmCwTWM2OD1yLkC1JOKyKDBwMECxJO69VQ>? MWCyOFU6PzR5OB?=
HGC27 HG NF;rOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2C5eWlEPTB;MD6zPEDDuSByLkCyNkDPxE1? M1rSXVI1PTl5NEe4
HGC27 LG M4mwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwMEKgxtEhOC5yMESg{txO MkfpNlQ2QTd2N{i=
MKN45 HG NXTVfnJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrOWGlKSzVyPUGuNFEhyrFiMD6wOVEh|ryP NUTyNI5mOjR3OUe0O|g>
MKN45 LG NVvyXYU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwOEegxtEhOC5yM{Cg{txO MmDYNlQ2QTd2N{i=
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NUGC4 LG MnjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;obmlKSzVyPUG0MlAhyrFiNT6zNlEh|ryP MXeyOFU6PzR5OB?=
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H661 M3[xO2Z2dmO2aX;uJGF{e2G7 NVLUdVVvOC5{NT:wMlUwOSEQvF2= NWrKPIR3OjRiaB?= M1e2PYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= MV2yOFM2OTR{NR?=
SAS M1;hSWZ2dmO2aX;uJGF{e2G7 NFX0cJoxNjJ3L{CuOU8yKM7:TR?= NGDnd|gzPCCq MonQbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MUeyOFM2OTR{NR?=
UT5 MnfOSpVv[3Srb36gRZN{[Xl? MkXDNE4zPS9yLkWvNUDPxE1? NXmwfIVpOjRiaB?= NW\BN5FQcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NYjNeZBQOjR|NUG0NlU>
FaDu Mk\0SpVv[3Srb36gRZN{[Xl? MoL1NE4zPS9yLkWvNUDPxE1? MlrQNlQhcA>? NGDoRoVqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= MUCyOFM2OTR{NR?=
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SUM149PT MX\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3TrZlAvOyEQvF2= MX23NkBp MVzlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> MkjnNlM3ODFyN{S=
MDA-MB-468 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV6wMlMh|ryP NXXuSZkzPzJiaB?= MVHlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NV:xe|dqOjN4MEGwO|Q>
MDA-MB-231 MoHrR4VtdCCYaXHibYxqfHliQYPzZZk> NY\ITZZQOC5|IN88US=> MkfiO|IhcA>? MYDlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NVOxcm1lOjN4MEGwO|Q>
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RD MXnBdI9xfG:|aYOgRZN{[Xl? NVztbnMzOyEEtV2= NYfiSlNpOTJiaB?= NUT5TGpRTE2VTx?= NGjjNZV{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> M3y4SlI{OzByOEC5
TP5014 MYHBdI9xfG:|aYOgRZN{[Xl? M2jEU|MhyrWP MUSxNkBp MX7EUXNQ MoHud4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= MXOyN|MxODhyOR?=
HT1080 M3jLcWFxd3C2b4Ppd{BCe3OjeR?= NIHQflI{KML3TR?= M3HY[VEzKGh? NX3DOG8xTE2VTx?= Mn3Fd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= NE\mfFAzOzNyMEiwPS=>
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HCC827 Mn7MSpVv[3Srb36gRZN{[Xl? M2nte|AuOy5|IN88US=> MXq3NkBp MkntbY5lfWOnczDjc41xdGW2ZTDkc5dvemWpdXzheIlwdiCxZjDwRWtV NYntVW01OjN{NUm1PVE>
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ALL-SIL M4fiNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKx5qCK|ryP NYX0dGUzPyCm M3nYXIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M2\QW|I{ODN6Mkez
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MM1S MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXYNE0zKM7:TR?= MXKyOEBp NW[2bW5SUUN3ME2wMlUh|ryP MWKyNlgzQTJ|NB?=
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KMS12-BM  NITvV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnf1NE0zKM7:TR?= NV\wN5Y3OjRiaB?= NVvEN5hMUUN3MP-8olIh|ryP MUmyNlgzQTJ|NB?=
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PC-9  NV7wNmFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOwMVMh|ryP NHXEZmw4OiCq MlG0TWM2OD1yLkig{txO MWGyNVIzODR5NB?=
LN229 NGqzPZlHfW6ldHnvckBCe3OjeR?= NV76b4pQOSEQvF2= NHTSeWw1QCCq MnvsbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? M2PUelIyODZ{OUmz
U87 NILu[YJHfW6ldHnvckBCe3OjeR?= NV3kWHZpOSEQvF2= NF;WfFE1QCCq M{n3dYlv\HWlZYOgZZV1d3CqYXfvd49u\SCob4LtZZRqd25? Mn3UNlExPjJ7OUO=
U373 MXPGeY5kfGmxbjDBd5NigQ>? MkXpNUDPxE1? MojhOFghcA>? Ml\VbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? NIPQeYszOTB4Mkm5Ny=>
SF767 NWPaWGlKTnWwY4Tpc44hSXO|YYm= MWexJO69VQ>? MX:0PEBp MVnpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v NVLXbpVCOjFyNkK5PVM>
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518A2  MWHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYewMlAy6oDVMUFihKnPxE1? M2f3W|czKGh? NWS2N485cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M1nU[|IyODR6N{i1
Mel-Juso  NGfxWm1HfW6ldHnvckBCe3OjeR?= M4DBV|AvODBz4pETNgKBkc7:TR?= MXOyOEBp MojZd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= MV[yNVA1QDd6NR?=
518A2 Mn34SpVv[3Srb36gRZN{[Xl? MlrjNE4xODIkgKOx5qCK|ryP M1G3elI1KGh? MmPJd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= Mo\iNlExPDh5OEW=
PC3  M2exNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF33fYszPGh? MmW5S2k2OMLiPTCxNFAhdk1? MoHWNlA2PTFyNkG=
U87MG NUDq[5J6TnWwY4Tpc44hSXO|YYm= MXOwMlEuOSEQvF2= M3v3d|I16oDLaNMg NFSyUolFVVOR M2TYUolvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p NUTZWo9WOTl4M{O2PFM>
U138MG NXPJeJpCTnWwY4Tpc44hSXO|YYm= MYCwMlEuOSEQvF2= M1;yO|I16oDLaNMg NWDNSpFlTE2VTx?= MWTpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? NGTCV5IyQTZ|M{[4Ny=>
U118MG M{jiWGZ2dmO2aX;uJGF{e2G7 M3;qPVAvOS1zIN88US=> MmXPNlTjiImqwrC= NInLSlJFVVOR MVPpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? Mn[2NVk3OzN4OEO=
U87MG M3KzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfPblBKSzVyPUCuNVQh|ryP MVuxPVU5PDJ{Nx?=
IGROV-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXJVFdKSzVyPUCuNFYh|ryP MUmxPVU5PDJ{Nx?=
DETROIT562 NFe3eJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjUcZo6UUN3ME2wMlE{KM7:TR?= NI\GTYkyQTV6NEKyOy=>
PC3  NVLjN3hpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTBwMUCg{txO MUOxPVU5PDJ{Nx?=
SKOV-3 NGW1dZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfKPFFIUUN3ME2wMlEzKM7:TR?= MY[xPVU5PDJ{Nx?=
HUVEC M3zoemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTRTWM2OD1yLkC4JO69VQ>? M1zaeFE6PTh2MkK3
UCH-1  NUHjcFhzTnWwY4Tpc44hSXO|YYm= NXSxSpVFOC13IN88US=> NYPEOHl5cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDic5RpKEGNVDDhcoQhdVSRUjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MnPMNVk2Ojh2NEG=
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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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