PI-103

PI-103は一種の多ターゲットPI3K阻害剤で、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

カスタマーフィードバック(4)

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阻害剤で、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 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\YfmoxNThizszN Mn3uNlQwPDhxN{KgbC=> MonqbY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= NXLhVXNOOjZ{MkS2PFE>
SH-SY5Y M2\w[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW4NE05KM7:TR?= MmG0NlQwPDhxN{KgbC=> NFvheVlqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To NFTpdlkzPjJ{NE[4NS=>
SH-SY5Y  MmPrRZBweHSxc3nzJGF{e2G7 MXOxJO69VQ>? NH7kTGkxNjVvMkSgbC=> NXi3Tmhye2Wwc3n0bZpmeyCwZYXyc4Jt[XO2b33hJINmdGy|IITvJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[XCxcITvd4l{ M4Tvd|I3OjJ2Nkix
G 35 SC M1LRcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LZcVAvODVvMkCg{txO NEXpVm0zPC95MjDo NULpXnMyTE2VTx?= MX3pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MkK4NlYyOjF{NUG=
G 38 SC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fRN|AvODVvMkCg{txO NGWzcFMzPC95MjDo NInL[GVFVVOR NYDpTFdDcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MYWyOlEzOTJ3MR?=
G 40 SC MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jOflAvODVvMkCg{txO MmDWNlQwPzJiaB?= M1zVb2ROW09? NEnQUIxqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MkfmNlYyOjF{NUG=
G 35 DC NIDVWGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jLOVAvODVvMkCg{txO NEPQT|IzPC95MjDo MWPEUXNQ NEmzTmdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M1fzOFI3OTJzMkWx
G 38 DC M1nSOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELhZ4oxNjB3LUKwJO69VQ>? Ml\tNlQwPzJiaB?= NVW0XnBpTE2VTx?= MUfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M2rVdVI3OTJzMkWx
G 40 DC NF3IOI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3KyVlAvODVvMkCg{txO NWrDVmtUOjRxN{KgbC=> M4DEemROW09? NH\zNIRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MY[yOlEzOTJ3MR?=
RD NH\neW9CeG:ydH;zbZMhSXO|YYm= MkfwNU8yNjVxMjFOwG0> NIfTOms4OiCq M1z5OYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M2SxT|I2PzR7M{e4
TE381.T MnLWRZBweHSxc3nzJGF{e2G7 MoLTNU8yNjVxMjFOwG0> MY[3NkBp NXHmfod2cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NVHwbWZCOjV5NEmzO|g>
RMS13 M{HpZ2Fxd3C2b4Ppd{BCe3OjeR?= MUexM|EvPS9{IN88US=> M4TVeFczKGh? M2DtV4lv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy NGCxd2YzPTd2OUO3PC=>
RH30  MkPjRZBweHSxc3nzJGF{e2G7 NXi5VoM6OS9zLkWvNkDPxE1? M1;FSVczKGh? NWfmNId3cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? NX\Q[5NzOjV5NEmzO|g>
VJ MVHBdI9xfG:|aYOgRZN{[Xl? NHLnVZYyNzFwNT:yJO69VQ>? MWG3NkBp MWPpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> NYjGNVRSOjV5NEmzO|g>
HS578T M2DKcmNmdGxiVnnhZoltcXS7IFHzd4F6 Mn2xNE0{KM7:TR?= NUf3ZXNyPzJiaB?= MVXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NETEeWczPTd{MUSxPS=>
BT549 NVOxOGdES2WubDDWbYFjcWyrdImgRZN{[Xl? Mm\1NE0{KM7:TR?= M3PQTVczKGh? M{PSTolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MoCzNlU4OjF2MUm=
MDA-MB-231 MnHvR4VtdCCYaXHibYxqfHliQYPzZZk> M{DqfVAuOyEQvF2= MUK3NkBp NHHqWolqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NFjqfFczPTd{MUSxPS=>
MDA-MB-468 M1vERWNmdGxiVnnhZoltcXS7IFHzd4F6 Mn7sNE0{KM7:TR?= M4n3PVczKGh? MkXobY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NFzscXIzPTd{MUSxPS=>
MDA-MB-436 MV\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2jzd|AuOyEQvF2= MUC3NkBp NFLMUmFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 Ml62NlU4OjF2MUm=
SUM149PT NVHE[XluS2WubDDWbYFjcWyrdImgRZN{[Xl? NH32fVkxNTNizszN M3jWXlczKGh? MUnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NX2z[GRTOjV5MkG0NVk>
MDA-MB-468 M{TvW2Z2dmO2aX;uJGF{e2G7 NXW0d5dLOC5yMT2xNEDPxE1? MoLyNlQhcA>? Mmns[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? NVPkPFNQOjV5MkG0NVk>
MDA-MB-231 NVKxSXBDTnWwY4Tpc44hSXO|YYm= MYKwMlAyNTFyIN88US=> NFPrdHkzPCCq M2fWTYRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? MnvtNlU4OjF2MUm=
HS578T NGTHVohHfW6ldHnvckBCe3OjeR?= M{DIOVAvODFvMUCg{txO M3LTUlI1KGh? MU\kc5dvemWpdXzheIV{KHSqZTDs[ZZmdHNib3[g{tIuXHKFUEGsJIMuVXmlIHHu[EBkgWOuaX6gSUBxem:2ZXnud:Kh MWiyOVczOTRzOR?=
SW872 MoDwSpVv[3Srb36gRZN{[Xl? MVqwMlAyNTBwNTFOwG0> NHzCO|IzPCCq MXTy[YR2[2W|IFHLWEBxcG:|cHjvdplt[XSrb36gLJBCU1RrIHHu[EA1TUKSMTDwbI9{eGixconsZZRqd25iKIC0SWJROSliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NGTwWpUzPDZ7NU[zNi=>
SW982 NH3hWmtHfW6ldHnvckBCe3OjeR?= NEL3UooxNjBzLUCuOUDPxE1? MXGyOEBp NFfIfIpz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> NUL0VXFxOjR4OUW2N|I>
SW872 Mo\kRZBweHSxc3nzJGF{e2G7 M{fMclAvODFvMD61JO69VQ>? NEfVeoM1QCCq MluybY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M3nvO|I1Pjl3NkOy
SW982 MVLBdI9xfG:|aYOgRZN{[Xl? NIHXXoQxNjBzLUCuOUDPxE1? M1\GVVQ5KGh? MXrpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MUSyOFY6PTZ|Mh?=
AGS HG NGnuTYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi3Zlc5UUN3ME2wMlY5KMLzIECuNFMyKM7:TR?= MnjZNlQ2QTd2N{i=
AGS LG M2fZe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlOyTWM2OD1yLkC1JOKyKDBwMECxJO69VQ>? M{PEdVI1PTl5NEe4
HGC27 HG MmXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUO4bHFOUUN3ME2wMlM5KMLzIECuNFIzKM7:TR?= NEW3UZUzPDV7N{S3PC=>
HGC27 LG MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfNXYM4UUN3ME2wMlAzKMLzIECuNFA1KM7:TR?= NUXodW1SOjR3OUe0O|g>
MKN45 HG MkfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTFwMEGgxtEhOC5yNUGg{txO NVyyVoFjOjR3OUe0O|g>
MKN45 LG NYXqPFRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwOEegxtEhOC5yM{Cg{txO NVrje5VsOjR3OUe0O|g>
NUGC4 HG MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHhTWM2OD1zND6wJOKyKDNwOUGzJO69VQ>? MnX5NlQ2QTd2N{i=
NUGC4 LG NWi4XohTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTF2LkCgxtEhPS5|MkGg{txO NEOybY0zPDV7N{S3PC=>
A549 M4XNfGZ2dmO2aX;uJGF{e2G7 NF7ISnIxNjJ3L{CuOU8yKM7:TR?= MUGyOEBp MnXQbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> NV\6PIdVOjR|NUG0NlU>
H460 M{C0fWZ2dmO2aX;uJGF{e2G7 NXvGZ4FCOC5{NT:wMlUwOSEQvF2= NH7RclEzPCCq NULz[3NJcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? MmH2NlQ{PTF2MkW=
H661 MUPGeY5kfGmxbjDBd5NigQ>? M{L1cVAvOjVxMD61M|Eh|ryP MYiyOEBp NUTsOlRwcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 MVyyOFM2OTR{NR?=
SAS M1:2S2Z2dmO2aX;uJGF{e2G7 MnPlNE4zPS9yLkWvNUDPxE1? MnHLNlQhcA>? MXHpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MVGyOFM2OTR{NR?=
UT5 M1Xzb2Z2dmO2aX;uJGF{e2G7 NXvQbG43OC5{NT:wMlUwOSEQvF2= MXyyOEBp NVvMNmc2cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 MmGwNlQ{PTF2MkW=
FaDu MXvGeY5kfGmxbjDBd5NigQ>? M3PQNlAvOjVxMD61M|Eh|ryP M3jCelI1KGh? M2n6fYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= Mmj3NlQ{PTF2MkW=
RD NI[zRWdCeG:ydH;zbZMhSXO|YYm= NX61bZNGOS9zLkWvNkDPxE1? NFP3NlE4OiCq MVPEUXNQ NGjrTm9qdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 M1\VNlI{Pjh2OUK1
TE671 MnfERZBweHSxc3nzJGF{e2G7 NHfmb|AyNzFwNT:yJO69VQ>? NUPBd3gxPzJiaB?= M4fJPGROW09? NVvqUoV2cW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? NHKwR20zOzZ6NEmyOS=>
RH30  NELyRYZCeG:ydH;zbZMhSXO|YYm= NXH3Z3RXOS9zLkWvNkDPxE1? M1;mNlczKGh? NH;tcJRFVVOR MojQbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDhdI9xfG:|aYOgZ49u[mmwZXSge4l1cCCXT{GyOi=> M2CyT|I{Pjh2OUK1
RMS13 NH3XXnhCeG:ydH;zbZMhSXO|YYm= MWixM|EvPS9{IN88US=> NFi5UJA4OiCq NF3aXnlFVVOR NYDjbY16cW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? NFjVbmYzOzZ6NEmyOS=>
SUM149PT NUf5eJVwS2WubDDWbYFjcWyrdImgRZN{[Xl? MlftNE4{KM7:TR?= MXm3NkBp NH\HW5lmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? MnSxNlM3ODFyN{S=
MDA-MB-468 NWTEPGVZS2WubDDWbYFjcWyrdImgRZN{[Xl? MWqwMlMh|ryP M1;tRlczKGh? MkXU[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ M2j1[|I{PjBzMEe0
MDA-MB-231 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEPSXosxNjNizszN M{i5TVczKGh? M1TUb4VvcGGwY3XzJIN6fG:2b4jpZ{Bm\m[nY4TzJI9nKFCLM1uvRWtVKHCjdHj3ZZkhcW6qaXLpeI9zew>? M1q4[FI{PjBzMEe0
SY5Y M12yc2Z2dmO2aX;uJGF{e2G7 MYOxMlUwOi53L{Wg{txO MW[yOEBp NUjOc3A1cW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> NHrnTFUzOzN5OEO0NS=>
SKNBE(2c) NIrjWpVHfW6ldHnvckBCe3OjeR?= MorJNU42NzJwNT:1JO69VQ>? NGrZXm0zPCCq MoHjbY5lfWOnczDHNeKh[2WubD3jfYNt\SCjcoLld5Qh[W6mIHHwc5B1d3Orcx?= M3S0dlI{Ozd6M{Sx
RD M{LKfmFxd3C2b4Ppd{BCe3OjeR?= MV2zJOK2VQ>? M{HwclEzKGh? NYS0[mIzTE2VTx?= MmDtd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= MX[yN|MxODhyOR?=
TP5014 NIf6fVBCeG:ydH;zbZMhSXO|YYm= NFn3N5I{KML3TR?= NUHmbJo1OTJiaB?= NVXt[nBlTE2VTx?= NELvVG1{\W6|aYTpfoV{KFKGIHPlcIx{KHSxIFTPXE1qdmS3Y3XkJIFxd3C2b4Ppdy=> MoHjNlM{ODB6MEm=
HT1080 M{\4RWFxd3C2b4Ppd{BCe3OjeR?= NGj4O|E{KML3TR?= MkjJNVIhcA>? M2Trc2ROW09? MYnz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= MVyyN|MxODhyOR?=
A549 Mm\vSpVv[3Srb36gRZN{[Xl? MUmwMVMvOyEQvF2= MYW3NkBp NEnP[lBqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? NVPKbWY6OjN{NUm1PVE>
HCC827 NHnFSFRHfW6ldHnvckBCe3OjeR?= MorBNE0{NjNizszN MmrqO|IhcA>? NGDaZ|JqdmS3Y3XzJINwdXCuZYTlJIRwf26{ZXf1cIF1cW:wIH;mJJBCU1R? NX;qepFFOjN{NUm1PVE>
H3122 M{HBSWZ2dmO2aX;uJGF{e2G7 NIm4dWUxNTNwMzFOwG0> NGPDc3M4OiCq M3rDS4lv\HWlZYOgZ49ueGyndHWg[I94dnKnZ4XsZZRqd25ib3[gdGFMXA>? NYLlZmZkOjN{NUm1PVE>
TALL-1 NVL1dnk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITkcJcy6oDLzszN MoC1O{Bl M3GwZoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NH;LPYszOzB|OEK3Ny=>
HPB-ALL MojZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrrNgKBkc7:TR?= NYjrUplKPyCm NUn0UHpq\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M4njc|I{ODN6Mkez
DND41 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDiU4puOeLCid88US=> M{O0eFch\A>? MkW5[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MkPWNlMxOzh{N{O=
SUP-T1 NHPvVIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUex5qCK|ryP NWiyUVZFPyCm NFq0UGZl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? M1TEblI{ODN6Mkez
PEER MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUex5qCK|ryP NHPUW|A4KGR? NYLFUo97\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NI\GOmkzOzB|OEK3Ny=>
ALL-SIL Mme5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;ve5My6oDLzszN NX3wcpF{PyCm Ml7z[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MkLVNlMxOzh{N{O=
KE37 Mlv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PQcFHjiIoQvF2= MVy3JIQ> NWLoT5lM\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 M3XUW|I{ODN6Mkez
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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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