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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電話番号: + 81 3-5632-9610mail@cosmobio.co.jp

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 NVXBb25wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nRO|AuQCEQvF2= MlvvNlQwPDhxN{KgbC=> M2\XOolv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= NHj5fZAzPjJ{NE[4NS=>
SH-SY5Y MlnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknmNE05KM7:TR?= NGn3VlgzPC92OD:3NkBp NYC1VZNncW6mdXPld{B1cW2nLTDhcoQh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgbY5pcWKrdHnvckBwdiCQQjDj[YxtKGe{b4f0bC=> NI\WcYczPjJ{NE[4NS=>
SH-SY5Y  M1voOGFxd3C2b4Ppd{BCe3OjeR?= NVm5fIFTOSEQvF2= NIS3OoExNjVvMkSgbC=> NFHmWWx{\W6|aYTpfoV{KG6ndYLvZoxie3SxbXGgZ4VtdHNidH:g[I95d3K3YnnjbY4ucW6mdXPl[EBieG:ydH;zbZM> NI[3OlgzPjJ{NE[4NS=>
G 35 SC NFTtT|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVGwMlA2NTJyIN88US=> NWLuN|JUOjRxN{KgbC=> NGTXW3pFVVOR MWTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MkDnNlYyOjF{NUG=
G 38 SC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWxNE4xPS1{MDFOwG0> M13FelI1Nzd{IHi= MXvEUXNQ NH;qO3VqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MYWyOlEzOTJ3MR?=
G 40 SC NYLJ[mZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWiwMlA2NTJyIN88US=> M3[yRVI1Nzd{IHi= NVHNXohJTE2VTx?= MY\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M2fy[FI3OTJzMkWx
G 35 DC NUTzUpo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlqzNE4xPS1{MDFOwG0> Mk\KNlQwPzJiaB?= MljTSG1UVw>? Mof1bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MVOyOlEzOTJ3MR?=
G 38 DC MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXxNE4xPS1{MDFOwG0> M17TZVI1Nzd{IHi= MmW2SG1UVw>? NHvFSWtqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M4DzfVI3OTJzMkWx
G 40 DC MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\YNE4xPS1{MDFOwG0> NUnTU4lNOjRxN{KgbC=> NEG5OHhFVVOR MkPDbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NHf1cWgzPjF{MUK1NS=>
RD MkjyRZBweHSxc3nzJGF{e2G7 NYm0cZNSOS9zLkWvNkDPxE1? NES0d2Q4OiCq M1i4eYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy MUiyOVc1QTN5OB?=
TE381.T M2XudGFxd3C2b4Ppd{BCe3OjeR?= MXOxM|EvPS9{IN88US=> M3XVelczKGh? M3Pnfolv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiR1HOWFYy M3f2WVI2PzR7M{e4
RMS13 NXrHWmdKSXCxcITvd4l{KEG|c3H5 NUXndFg5OS9zLkWvNkDPxE1? MV23NkBp NETiXnFqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFfBUnQ3OQ>? Moi0NlU4PDl|N{i=
RH30  NWr6OlZSSXCxcITvd4l{KEG|c3H5 Mn;1NU8yNjVxMjFOwG0> NVm0dYxLPzJiaB?= NWH4OGpCcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDHRW5VPjF? MlnHNlU4PDl|N{i=
VJ NVHZWmgxSXCxcITvd4l{KEG|c3H5 MW[xM|EvPS9{IN88US=> NYfQSlRxPzJiaB?= MUTpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEeDTmS2NS=> M2i3V|I2PzR7M{e4
HS578T NV7sU5VQS2WubDDWbYFjcWyrdImgRZN{[Xl? NHH6U5QxNTNizszN MWW3NkBp MW\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 Mnf6NlU4OjF2MUm=
BT549 M2\aSmNmdGxiVnnhZoltcXS7IFHzd4F6 NIewS|gxNTNizszN MYm3NkBp M2LTdIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NG[1NGozPTd{MUSxPS=>
MDA-MB-231 MXLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYCwMVMh|ryP Ml:0O|IhcA>? NWji[oNocW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M1zGN|I2PzJzNEG5
MDA-MB-468 NYfIfG9tS2WubDDWbYFjcWyrdImgRZN{[Xl? MU[wMVMh|ryP NUDCcXJ{PzJiaB?= MnjVbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NHrO[2gzPTd{MUSxPS=>
MDA-MB-436 MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVLBb5hsOC1|IN88US=> NW[wWYt3PzJiaB?= NGfMfVJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NGCyNpQzPTd{MUSxPS=>
SUM149PT MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlH3NE0{KM7:TR?= MoH4O|IhcA>? MVnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MkGwNlU4OjF2MUm=
MDA-MB-468 M2[2XGZ2dmO2aX;uJGF{e2G7 MUewMlAyNTFyIN88US=> MmH2NlQhcA>? MnfQ[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? M2DCfVI2PzJzNEG5
MDA-MB-231 MWjGeY5kfGmxbjDBd5NigQ>? NXvGTXV3OC5yMT2xNEDPxE1? Ml;ONlQhcA>? NV\ZcYFY\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MX:yOVczOTRzOR?=
HS578T MV3GeY5kfGmxbjDBd5NigQ>? NHL3UYkxNjBzLUGwJO69VQ>? NUX4[XJTOjRiaB?= NVXy[XhR\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= NHyxS48zPTd{MUSxPS=>
SW872 MojOSpVv[3Srb36gRZN{[Xl? MYqwMlAyNTBwNTFOwG0> NGLNc3QzPCCq NHX5[VFz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> NVXmNYZtOjR4OUW2N|I>
SW982 NEfT[JJHfW6ldHnvckBCe3OjeR?= NVHPNHZ1OC5yMT2wMlUh|ryP M2jYR|I1KGh? NFHEWFFz\WS3Y3XzJGFMXCCyaH;zdIhwenmuYYTpc44hMHCDS2SpJIFv\CB2RVLQNUBxcG:|cHjvdplt[XSrb36gLJA1TUKSMTmgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYNCpC=> MmTsNlQ3QTV4M{K=
SW872 NVrzW452SXCxcITvd4l{KEG|c3H5 MWKwMlAyNTBwNTFOwG0> NE\KPWY1QCCq M4rucYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NF;FV2MzPDZ7NU[zNi=>
SW982 MnXSRZBweHSxc3nzJGF{e2G7 M3[1WVAvODFvMD61JO69VQ>? NGX6e4g1QCCq M3TubIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NYXNbZJLOjR4OUW2N|I>
AGS HG NUPUXpBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwNkigxtEhOC5yM{Gg{txO M1rwZ|I1PTl5NEe4
AGS LG NGO1Z|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;aUoZ4UUN3ME2wMlA2KMLzIECuNFAyKM7:TR?= Ml7YNlQ2QTd2N{i=
HGC27 HG NXnnVIpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\kTWM2OD1yLkO4JOKyKDBwMEKyJO69VQ>? M3vPe|I1PTl5NEe4
HGC27 LG NGi4TmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXhTWM2OD1yLkCyJOKyKDBwMEC0JO69VQ>? NYjIfopPOjR3OUe0O|g>
MKN45 HG MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTFwMEGgxtEhOC5yNUGg{txO NUDIS2lqOjR3OUe0O|g>
MKN45 LG M1HleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIS0foRKSzVyPUCuPFchyrFiMD6wN|Ah|ryP M3XpWVI1PTl5NEe4
NUGC4 HG M4fFR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF2LkCgxtEhOy57MUOg{txO M{Dn[VI1PTl5NEe4
NUGC4 LG Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF2LkCgxtEhPS5|MkGg{txO MmK3NlQ2QTd2N{i=
A549 NUnHWmtnTnWwY4Tpc44hSXO|YYm= MYCwMlI2NzBwNT:xJO69VQ>? NWTidGRHOjRiaB?= Mkj5bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> M2m2dFI1OzVzNEK1
H460 NITNbmFHfW6ldHnvckBCe3OjeR?= MYOwMlI2NzBwNT:xJO69VQ>? Mlv4NlQhcA>? NIrkVZZqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOuaXfoeIx6 NFjRWpYzPDN3MUSyOS=>
H661 NUXvZWdkTnWwY4Tpc44hSXO|YYm= MYSwMlI2NzBwNT:xJO69VQ>? M1;FWFI1KGh? NUjCTYQ1cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NF[zb2czPDN3MUSyOS=>
SAS NYe5cnk4TnWwY4Tpc44hSXO|YYm= M1TTPVAvOjVxMD61M|Eh|ryP NHTHOZkzPCCq MX;pcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? NX7U[3R7OjR|NUG0NlU>
UT5 NIHlRmdHfW6ldHnvckBCe3OjeR?= MnTKNE4zPS9yLkWvNUDPxE1? MlG0NlQhcA>? MmTnbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 M4fpZ|I1OzVzNEK1
FaDu MWfGeY5kfGmxbjDBd5NigQ>? M{D4cFAvOjVxMD61M|Eh|ryP Mn\aNlQhcA>? NWDnXI5TcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 M{jOVFI1OzVzNEK1
RD MnzERZBweHSxc3nzJGF{e2G7 MX[xM|EvPS9{IN88US=> NYP4OIxpPzJiaB?= NGfSNWxFVVOR NVHCbI85cW6mdXPld{Bk[XOyYYPlMYRmeGWwZHXueEBieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDVU|EzPg>? NXSxeGRrOjN4OES5NlU>
TE671 Ml;pRZBweHSxc3nzJGF{e2G7 NHn6bm4yNzFwNT:yJO69VQ>? MnXEO|IhcA>? NIK5WXhFVVOR NImxU|JqdmS3Y3XzJINie3Cjc3Wt[IVx\W6mZX70JIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIGXPNVI3 NUDXVnJZOjN4OES5NlU>
RH30  M3;pOmFxd3C2b4Ppd{BCe3OjeR?= Ml2wNU8yNjVxMjFOwG0> NHSyTZI4OiCq NY\M[2hQTE2VTx?= MUfpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 M1\lb|I{Pjh2OUK1
RMS13 MXHBdI9xfG:|aYOgRZN{[Xl? NH;0VmwyNzFwNT:yJO69VQ>? Mk\FO|IhcA>? NHfBeoRFVVOR MWLpcoR2[2W|IHPhd5Bie2VvZHXw[Y5l\W62IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKFWRMUK2 NYDOcGtUOjN4OES5NlU>
SUM149PT NUPsdXVbS2WubDDWbYFjcWyrdImgRZN{[Xl? M2DYR|AvOyEQvF2= M4j0U|czKGh? NVeyOHQy\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| NIfCOW0zOzZyMUC3OC=>
MDA-MB-468 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUWwMlMh|ryP MlLJO|IhcA>? MX3lcohidmOnczDjfZRwfG:6aXOg[YZn\WO2czDv[kBRUTONL1HLWEBx[XSqd3H5JIlvcGmkaYTvdpM> NVrVU2tlOjN4MEGwO|Q>
MDA-MB-231 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVPOUnZlOC5|IN88US=> M4rCVFczKGh? NHn0enBmdmijbnPld{BkgXSxdH;4bYMh\W[oZXP0d{Bw\iCSSUPLM2FMXCCyYYToe4F6KGmwaHnibZRwenN? NWL0RZRVOjN4MEGwO|Q>
SY5Y MYPGeY5kfGmxbjDBd5NigQ>? MVexMlUwOi53L{Wg{txO MWiyOEBp NV\kfVBLcW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> MYGyN|M4QDN2MR?=
SKNBE(2c) MV;GeY5kfGmxbjDBd5NigQ>? M{HJWlEvPS9{LkWvOUDPxE1? NXP5O5dHOjRiaB?= NUfRW4x[cW6mdXPld{BIOcLiY3XscE1kgWOuZTDhdpJme3RiYX7kJIFxd3C2b4Ppdy=> MonVNlM{Pzh|NEG=
RD MY\BdI9xfG:|aYOgRZN{[Xl? MX6zJOK2VQ>? NYjmOnh7OTJiaB?= NEfLVI5FVVOR MYHz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= NFOxWG8zOzNyMEiwPS=>
TP5014 M{XRdWFxd3C2b4Ppd{BCe3OjeR?= M3HheFMhyrWP MmnYNVIhcA>? NXjkcWtqTE2VTx?= M1XLWJNmdnOrdHn6[ZMhWkRiY3XscJMhfG9iRF;YMYlv\HWlZXSgZZBweHSxc3nz Mn\GNlM{ODB6MEm=
HT1080 MUHBdI9xfG:|aYOgRZN{[Xl? NIe4Umw{KML3TR?= NVn0U3NXOTJiaB?= M37jNWROW09? MVzz[Y5{cXSrenXzJHJFKGOnbHzzJJRwKESRWD3pcoR2[2WmIHHwc5B1d3Orcx?= MXSyN|MxODhyOR?=
A549 MV;GeY5kfGmxbjDBd5NigQ>? M2riT|AuOy5|IN88US=> MX:3NkBp MWfpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> MmK4NlMzPTl3OUG=
HCC827 NEi5enJHfW6ldHnvckBCe3OjeR?= NUj3cHh4OC1|LkOg{txO MlfpO|IhcA>? NU\0eoZvcW6mdXPld{Bkd22ybHX0[UBld3ewcnXneYxifGmxbjDv[kBxSUuW NX7hW5l6OjN{NUm1PVE>
H3122 NX\nSW94TnWwY4Tpc44hSXO|YYm= MVWwMVMvOyEQvF2= M2LGdVczKGh? MWPpcoR2[2W|IHPvcZBt\XSnIHTve45z\We3bHH0bY9vKG:oIIDBT3Q> NEnTPHIzOzJ3OUW5NS=>
TALL-1 M3jHVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3Ic|l6OeLCid88US=> MUe3JIQ> NVXMN2Jv\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NYLMN2ZWOjNyM{iyO|M>
HPB-ALL Ml7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37Cb|HjiIoQvF2= MkT2O{Bl MoD1[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 MmDONlMxOzh{N{O=
DND41 NH;GOYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVyx5qCK|ryP NYHpN4tOPyCm MmTT[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M{j5TlI{ODN6Mkez
SUP-T1 NHuzSIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKx5qCK|ryP Mnv6O{Bl Ml\V[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M{Xx[VI{ODN6Mkez
PEER MmTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:x5qCK|ryP M1q3VVch\A>? Mnfi[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NVTsflBlOjNyM{iyO|M>
ALL-SIL MmT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqx5qCK|ryP NV;S[IljPyCm Mlru[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M1nXNFI{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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