PI-103

PI-103は一種の多ターゲットPI3K抑制剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は2 nM/3 nM/3 nM/15 nMです。PI-103はmTOR/DNA-PKに作用する効果が弱くて、このIC50値が30 nM/23 nMになります。

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PI-103 化学構造
分子量: 348.36

高品質保証

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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は一種の多ターゲットPI3K抑制剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は2 nM/3 nM/3 nM/15 nMです。PI-103はmTOR/DNA-PKに作用する効果が弱くて、このIC50値が30 nM/23 nMになります。
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 M3P4[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\PVJQxNThizszN NV3kSnBHOjRxNEivO|IhcA>? M1\NN4lv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= MXqyOlIzPDZ6MR?=
SH-SY5Y M{\6[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[wNE05KM7:TR?= M{X4XFI1NzR6L{eyJIg> NX\sbVR4cW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> M{K4TlI3OjJ2Nkix
SH-SY5Y  MnyyRZBweHSxc3nzJGF{e2G7 NGDY[VcyKM7:TR?= NYjO[2FtOC53LUK0JIg> MmfOd4Vve2m2aYrld{Bv\XW{b3LsZZN1d22jIHPlcIx{KHSxIHTvfI9zfWKrY3nuMYlv\HWlZXSgZZBweHSxc3nz MkK5NlYzOjR4OEG=
G 35 SC MnzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HYb|AvODVvMkCg{txO NECxR3QzPC95MjDo M3nCOGROW09? NV6xXnlScW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MoGwNlYyOjF{NUG=
G 38 SC MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLkV|MxNjB3LUKwJO69VQ>? NYi3SJJEOjRxN{KgbC=> NVeyRmF3TE2VTx?= MlH1bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NXHSN3o1OjZzMkGyOVE>
G 40 SC NE\lVpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXPdWNwOC5yNT2yNEDPxE1? MWCyOE84OiCq MXTEUXNQ Mmf0bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NV\SfphxOjZzMkGyOVE>
G 35 DC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTmPHY6OC5yNT2yNEDPxE1? NHv1U3MzPC95MjDo MVfEUXNQ M{DMNolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NVrxXpI4OjZzMkGyOVE>
G 38 DC NV\ISZRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXEd|gxNjB3LUKwJO69VQ>? NIrzSo8zPC95MjDo M2HzeWROW09? NX7kbGJRcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MlXyNlYyOjF{NUG=
G 40 DC NFXGeoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2e5OFAvODVvMkCg{txO M{DnflI1Nzd{IHi= MknXSG1UVw>? NGLwVotqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 Mnr5NlYyOjF{NUG=
RD NYrQZZJVSXCxcITvd4l{KEG|c3H5 NH\PUHQyNzFwNT:yJO69VQ>? M176TFczKGh? MXLpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NU\Y[II6OjV5NEmzO|g>
TE381.T M1\yZmFxd3C2b4Ppd{BCe3OjeR?= MYixM|EvPS9{IN88US=> NWjHcoNFPzJiaB?= Mn7sbY5lfWOnczDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCJQV7UOlE> M{HSSFI2PzR7M{e4
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VJ MmnNRZBweHSxc3nzJGF{e2G7 M4C0R|EwOS53L{Kg{txO MYi3NkBp MVvpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> M1;4RlI2PzR7M{e4
HS578T MkPkR4VtdCCYaXHibYxqfHliQYPzZZk> M3viT|AuOyEQvF2= MVi3NkBp MXHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MX[yOVczOTRzOR?=
BT549 NVLkcnB1S2WubDDWbYFjcWyrdImgRZN{[Xl? Mm\0NE0{KM7:TR?= M{PlR|czKGh? M1zmT4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MkWxNlU4OjF2MUm=
MDA-MB-231 NF3UN2NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmX2NE0{KM7:TR?= NFvRfpI4OiCq MX7pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NWPGPItrOjV5MkG0NVk>
MDA-MB-468 NUH6WYI4S2WubDDWbYFjcWyrdImgRZN{[Xl? M1XsSVAuOyEQvF2= NEHOT2Y4OiCq MVLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 Mn;NNlU4OjF2MUm=
MDA-MB-436 M1TrOWNmdGxiVnnhZoltcXS7IFHzd4F6 M3LVWVAuOyEQvF2= NXr3bXFyPzJiaB?= MXTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MY[yOVczOTRzOR?=
SUM149PT NXHoPIl3S2WubDDWbYFjcWyrdImgRZN{[Xl? MYCwMVMh|ryP M17q[FczKGh? MlnZbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MVGyOVczOTRzOR?=
MDA-MB-468 MlzkSpVv[3Srb36gRZN{[Xl? NFvLbmExNjBzLUGwJO69VQ>? MWiyOEBp NF;Rc2Vld3ewcnXneYxifGW|IITo[UBt\X[nbIOgc4Yh|rJvVILDVFEtKGNvTYnjJIFv\CCleXPsbY4hTSCycn;0[Ylve8Li NXvk[pdMOjV5MkG0NVk>
MDA-MB-231 NFfhSmxHfW6ldHnvckBCe3OjeR?= M1\JeVAvODFvMUCg{txO NWLBUpp4OjRiaB?= M13YS4Rwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? MXiyOVczOTRzOR?=
HS578T M4rXfWZ2dmO2aX;uJGF{e2G7 NF;TdI8xNjBzLUGwJO69VQ>? NGm1eJUzPCCq M2jyeIRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? NIfaNJczPTd{MUSxPS=>
SW872 MYnGeY5kfGmxbjDBd5NigQ>? MoDBNE4xOS1yLkWg{txO MoThNlQhcA>? MY\y[YR2[2W|IFHLWEBxcG:|cHjvdplt[XSrb36gLJBCU1RrIHHu[EA1TUKSMTDwbI9{eGixconsZZRqd25iKIC0SWJROSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MlHQNlQ3QTV4M{K=
SW982 NHjnT4pHfW6ldHnvckBCe3OjeR?= MlXKNE4xOS1yLkWg{txO NXrVRXRzOjRiaB?= NYTicXdxemWmdXPld{BCU1RicHjvd5Bpd3K7bHH0bY9vKCiyQVvULUBidmRiNFXCVFEheGixc4Doc5J6dGG2aX;uJEhxPEWEUEGpJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyxsA> Mli2NlQ3QTV4M{K=
SW872 NIjLfWNCeG:ydH;zbZMhSXO|YYm= MXewMlAyNTBwNTFOwG0> Mn3HOFghcA>? NEnGbYhqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NYC2epN2OjR4OUW2N|I>
SW982 MmHGRZBweHSxc3nzJGF{e2G7 NH31NnExNjBzLUCuOUDPxE1? MoLjOFghcA>? Mm\HbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M4jSO|I1Pjl3NkOy
AGS HG NEjXem5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwNkigxtEhOC5yM{Gg{txO MnrJNlQ2QTd2N{i=
AGS LG M2PDWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTBwMEWgxtEhOC5yMEGg{txO MnO2NlQ2QTd2N{i=
HGC27 HG MnvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwM{igxtEhOC5yMkKg{txO NIXKdnYzPDV7N{S3PC=>
HGC27 LG NFS3RmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\2TWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? NV7QXIcxOjR3OUe0O|g>
MKN45 HG MoHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDETWM2OD1zLkCxJOKyKDBwMEWxJO69VQ>? NFiyTZUzPDV7N{S3PC=>
MKN45 LG MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnpeWs4UUN3ME2wMlg4KMLzIECuNFMxKM7:TR?= MlzONlQ2QTd2N{i=
NUGC4 HG MoLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\EbGlEPTB;MUSuNEDDuSB|LkmxN{DPxE1? MWKyOFU6PzR5OB?=
NUGC4 LG MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvT[XR{UUN3ME2xOE4xKMLzIEWuN|IyKM7:TR?= NGDkV3kzPDV7N{S3PC=>
A549 NF[5S41HfW6ldHnvckBCe3OjeR?= M4O4[VAvOjVxMD61M|Eh|ryP NXnlWHRjOjRiaB?= NHXwNVRqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOuaXfoeIx6 NX\rPGtCOjR|NUG0NlU>
H460 MnrQSpVv[3Srb36gRZN{[Xl? NX\CcZV6OC5{NT:wMlUwOSEQvF2= MlTzNlQhcA>? Mlf3bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> NHSyU5YzPDN3MUSyOS=>
H661 MXHGeY5kfGmxbjDBd5NigQ>? NXjXXHpjOC5{NT:wMlUwOSEQvF2= NXn4OY1JOjRiaB?= MUXpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MY[yOFM2OTR{NR?=
SAS MkG2SpVv[3Srb36gRZN{[Xl? M{PrVFAvOjVxMD61M|Eh|ryP M2HaUVI1KGh? M4Cwd4lvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NXX5bWRCOjR|NUG0NlU>
UT5 NW[w[oZWTnWwY4Tpc44hSXO|YYm= NHrpVIwxNjJ3L{CuOU8yKM7:TR?= MUCyOEBp NWfCRZFZcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NVfaSWlGOjR|NUG0NlU>
FaDu MmPTSpVv[3Srb36gRZN{[Xl? NEHEOnAxNjJ3L{CuOU8yKM7:TR?= M2DIZ|I1KGh? NVTDV2hGcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 MknqNlQ{PTF2MkW=
RD NFzTdmRCeG:ydH;zbZMhSXO|YYm= MVmxM|EvPS9{IN88US=> NV61NYZiPzJiaB?= NUDm[WFTTE2VTx?= M{S3folv\HWlZYOgZ4F{eGG|ZT3k[ZBmdmSnboSgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiVV:xNlY> MXuyN|Y5PDl{NR?=
TE671 M3u2OGFxd3C2b4Ppd{BCe3OjeR?= MYmxM|EvPS9{IN88US=> MlrJO|IhcA>? MUHEUXNQ MlLqbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> Mn3TNlM3QDR7MkW=
RH30  NGjXOGhCeG:ydH;zbZMhSXO|YYm= NHnKd3UyNzFwNT:yJO69VQ>? NWPDdm9lPzJiaB?= MneySG1UVw>? MmLZbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> NEXjWpAzOzZ6NEmyOS=>
RMS13 NWDPZlJySXCxcITvd4l{KEG|c3H5 M{ezOFEwOS53L{Kg{txO NYP0[pg6PzJiaB?= MkLGSG1UVw>? MVzpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 NXi5T3VpOjN4OES5NlU>
SUM149PT NVTV[pNtS2WubDDWbYFjcWyrdImgRZN{[Xl? NIHGRZkxNjNizszN MlLnO|IhcA>? NYrOeXdi\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| NX2xWlNUOjN4MEGwO|Q>
MDA-MB-468 MnLKR4VtdCCYaXHibYxqfHliQYPzZZk> NXjCNZhGOC5|IN88US=> MYq3NkBp MXnlcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NUTyc5Z1OjN4MEGwO|Q>
MDA-MB-231 MmT5R4VtdCCYaXHibYxqfHliQYPzZZk> MX[wMlMh|ryP NVizNFZHPzJiaB?= M37OOoVvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? NHfyOJMzOzZyMUC3OC=>
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SKNBE(2c) NVnEXoxwTnWwY4Tpc44hSXO|YYm= MmL4NU42NzJwNT:1JO69VQ>? MlzXNlQhcA>? MofNbY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= NHv3UVgzOzN5OEO0NS=>
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TP5014 MXPBdI9xfG:|aYOgRZN{[Xl? NUnKUmxkOyEEtV2= NXX3OpdmOTJiaB?= MV;EUXNQ NHn0dJB{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MoHxNlM{ODB6MEm=
HT1080 NYjkbWdlSXCxcITvd4l{KEG|c3H5 M4nPU|MhyrWP M{HrSFEzKGh? MorwSG1UVw>? Mnvid4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= M33OfFI{OzByOEC5
A549 M13BW2Z2dmO2aX;uJGF{e2G7 Mnj2NE0{NjNizszN MofiO|IhcA>? MkjsbY5lfWOnczDjc41xdGW2ZTDkc5dvemWpdXzheIlwdiCxZjDwRWtV NELXVlQzOzJ3OUW5NS=>
HCC827 NV;HNIZMTnWwY4Tpc44hSXO|YYm= NUTFUXI4OC1|LkOg{txO NVjPR5ZiPzJiaB?= M{TZWYlv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? MWWyN|I2QTV7MR?=
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DND41 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DueFHjiIoQvF2= MXq3JIQ> NH;Ne2tl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NU\KZpFbOjNyM{iyO|M>
SUP-T1 NYqyd4wyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DBZlHjiIoQvF2= MnjZO{Bl MWfk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MkjXNlMxOzh{N{O=
PEER NGHLWG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHoNgKBkc7:TR?= NXP2bWhjPyCm MUnk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NHfZWlQzOzB|OEK3Ny=>
ALL-SIL MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;EcmFIOeLCid88US=> MVq3JIQ> MWLk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M4ThfFI{ODN6Mkez
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Karpas-45 NX[zNJN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfvNgKBkc7:TR?= M2\Jelch\A>? MoO0[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MlvyNlMxOzh{N{O=
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MOLT-16 NH\ySlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqx5qCK|ryP M3W3OFch\A>? M4LYTYRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NGj3TIczOzB|OEK3Ny=>
MM1S M1jQVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTze4J3OC1{IN88US=> MV[yOEBp M1m2W2lEPTB;MD61JO69VQ>? NVzLcmZqOjJ6MkmyN|Q>
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PC-9  MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHnNE0{KM7:TR?= NVX5[JM1PzJiaB?= NGHFO|BKSzVyPUCuPEDPxE1? M3fCfVIyOjJyNEe0
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518A2  NELSZotE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWLGZ|J6OC5yMfMAl|Ex6oDLzszN M2T1bFczKGh? NEe1SmNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MX6yNVA1QDd6NR?=
Mel-Juso  MXrGeY5kfGmxbjDBd5NigQ>? MnfWNE4xODIkgKOx5qCK|ryP MXeyOEBp MVLzeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBxcG:|cHjheIllgWxiaX7vd4l1d2xiMz3rbY5ie2ViZH;3cpN1emWjbTD0ZZJo\XS| NVrlWHpJOjFyNEi3PFU>
518A2 MXfGeY5kfGmxbjDBd5NigQ>? NXjBNGdnOC5yMEJihLMy6oDLzszN M4fPclI1KGh? NY\FNohwe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> NVLMdWtxOjFyNEi3PFU>
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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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 24 mg/mL (68.89 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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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