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 MlfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEGyXG0xNThizszN NEfxWGUzPC92OD:3NkBp Ml[2bY5lfWOnczD0bY1mNSCjbnSgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRiaX7obYJqfGmxbjDvckBPSiClZXzsJIdzd3e2aB?= MkLLNlYzOjR4OEG=
SH-SY5Y Mn2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\INFAuQCEQvF2= Moe2NlQwPDhxN{KgbC=> MVTpcoR2[2W|IITpcYUuKGGwZDDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCrbnjpZol1cW:wIH;uJG5DKGOnbHyg[5Jwf3Sq Mn\CNlYzOjR4OEG=
SH-SY5Y  M1XLcmFxd3C2b4Ppd{BCe3OjeR?= NV3pZXVDOSEQvF2= NUD5fIliOC53LUK0JIg> M4HIOJNmdnOrdHn6[ZMhdmW3cn;icIF{fG:vYTDj[YxteyC2bzDkc5hwenWkaXPpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> NV7MeFRrOjZ{MkS2PFE>
G 35 SC NVHoPJFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfTfIJFOC5yNT2yNEDPxE1? M1XjTFI1Nzd{IHi= M3\GeWROW09? MUTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 NHfHVYUzPjF{MUK1NS=>
G 38 SC NUC0VpVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTQfYdtOC5yNT2yNEDPxE1? NGPTZ2UzPC95MjDo NWWwW2RvTE2VTx?= M1HIfYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MYiyOlEzOTJ3MR?=
G 40 SC MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuwMlA2NTJyIN88US=> MkLNNlQwPzJiaB?= MoLwSG1UVw>? NUToXXpScW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M4fJc|I3OTJzMkWx
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G 38 DC NETIWlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLiNE4xPS1{MDFOwG0> MkDBNlQwPzJiaB?= NVKyXpZNTE2VTx?= M{XEdYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MmfkNlYyOjF{NUG=
G 40 DC MoOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuwMlA2NTJyIN88US=> M1P3dFI1Nzd{IHi= MX7EUXNQ NInDS3dqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M1XPZVI3OTJzMkWx
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HS578T NGrGSHpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHX1ZpcxNTNizszN NXPVW41XPzJiaB?= MVTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NUe0OnRqOjV5MkG0NVk>
BT549 NUPTZYNPS2WubDDWbYFjcWyrdImgRZN{[Xl? MmfaNE0{KM7:TR?= NWX1dFl[PzJiaB?= Mkj0bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MVGyOVczOTRzOR?=
MDA-MB-231 NUO3VnNoS2WubDDWbYFjcWyrdImgRZN{[Xl? NF\ocHExNTNizszN NUDORnl1PzJiaB?= NILTXJRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NV;1XY14OjV5MkG0NVk>
MDA-MB-468 NI\BdIRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MonWNE0{KM7:TR?= M3m0b|czKGh? NHrVeWJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1vtSlI2PzJzNEG5
MDA-MB-436 NITHXHdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1izO|AuOyEQvF2= M2X6cVczKGh? NE\jWZNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MYCyOVczOTRzOR?=
SUM149PT MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NF\6e2kxNTNizszN M{TpW|czKGh? NEfTOXpqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MV:yOVczOTRzOR?=
MDA-MB-468 NXfUe5lrTnWwY4Tpc44hSXO|YYm= M3PQUFAvODFvMUCg{txO MVuyOEBp Mke0[I94dnKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJO6zNVS{Q2CxMEBkNU27YzDhcoQh[3mlbHnuJGUheHKxdHXpcpPDqA>? M164d|I2PzJzNEG5
MDA-MB-231 MXLGeY5kfGmxbjDBd5NigQ>? MV6wMlAyNTFyIN88US=> NYm4OndvOjRiaB?= NYLq[G5l\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= M1ThTlI2PzJzNEG5
HS578T MnfMSpVv[3Srb36gRZN{[Xl? NGHrRpQxNjBzLUGwJO69VQ>? NEfFVJQzPCCq NVnReJZQ\G:5boLl[5Vt[XSnczD0bIUhdGW4ZXzzJI9nKM7{LWTyR3AyNCClLV35Z{BidmRiY4njcIlvKEVicILveIVqdnQEoB?= MUeyOVczOTRzOR?=
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SW982 MnPjRZBweHSxc3nzJGF{e2G7 NGS0[XgxNjBzLUCuOUDPxE1? MlP0OFghcA>? MUDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M1\EelI1Pjl3NkOy
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AGS LG NGq0UnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwMEWgxtEhOC5yMEGg{txO M13US|I1PTl5NEe4
HGC27 HG MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3jOFNKSzVyPUCuN|ghyrFiMD6wNlIh|ryP M1Py[FI1PTl5NEe4
HGC27 LG NULNNJhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwMEKgxtEhOC5yMESg{txO Mm\YNlQ2QTd2N{i=
MKN45 HG NXnGPJJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f4d2lEPTB;MT6wNUDDuSByLkC1NUDPxE1? M{HSfFI1PTl5NEe4
MKN45 LG NITSbGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLiTWM2OD1yLki3JOKyKDBwMEOwJO69VQ>? NWXRbo9WOjR3OUe0O|g>
NUGC4 HG NF;i[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF2LkCgxtEhOy57MUOg{txO MkTMNlQ2QTd2N{i=
NUGC4 LG MkToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTQTWM2OD1zND6wJOKyKDVwM{KxJO69VQ>? NIfrd5IzPDV7N{S3PC=>
A549 M2rUd2Z2dmO2aX;uJGF{e2G7 NFnD[HQxNjJ3L{CuOU8yKM7:TR?= M{S4VlI1KGh? NV25U|REcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? NF;IeFgzPDN3MUSyOS=>
H460 NXTEdWtYTnWwY4Tpc44hSXO|YYm= MmXHNE4zPS9yLkWvNUDPxE1? MVKyOEBp Mne0bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> NEjvRXAzPDN3MUSyOS=>
H661 MYfGeY5kfGmxbjDBd5NigQ>? MonMNE4zPS9yLkWvNUDPxE1? NW\mVmp{OjRiaB?= NFfXXI1qdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= M4\EeFI1OzVzNEK1
SAS MmP2SpVv[3Srb36gRZN{[Xl? M1;NSVAvOjVxMD61M|Eh|ryP NWfTZlRPOjRiaB?= NYTlU5g2cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 MkL1NlQ{PTF2MkW=
UT5 MoPkSpVv[3Srb36gRZN{[Xl? M3;KcFAvOjVxMD61M|Eh|ryP MYSyOEBp Mkm5bY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NWPmZWRHOjR|NUG0NlU>
FaDu M2nY[2Z2dmO2aX;uJGF{e2G7 MXGwMlI2NzBwNT:xJO69VQ>? NY[xWnFZOjRiaB?= M2\pNYlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= MWCyOFM2OTR{NR?=
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MDA-MB-468 NV7aUVVoS2WubDDWbYFjcWyrdImgRZN{[Xl? Mn;pNE4{KM7:TR?= NFv0VJM4OiCq NWPnWWRO\W6qYX7j[ZMh[3m2b4TvfIlkKGWoZnXjeJMhd2ZiUFmzT{9CU1RicHH0bJdigSCrbnjpZol1d3K| MWCyN|YxOTB5NB?=
MDA-MB-231 M1n1XGNmdGxiVnnhZoltcXS7IFHzd4F6 NVjFRoZpOC5|IN88US=> MoHTO|IhcA>? MkXU[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ NXTzUXB7OjN4MEGwO|Q>
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HT1080 MlLjRZBweHSxc3nzJGF{e2G7 MnnCN{DDvU1? NFLjZ5kyOiCq M2LtTWROW09? Mn7Sd4Vve2m2aYrld{BTTCClZXzsd{B1dyCGT2itbY5lfWOnZDDhdI9xfG:|aYO= MnrhNlM{ODB6MEm=
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HPB-ALL MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;OUFHjiIoQvF2= NHL6W5M4KGR? MofL[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M3HPSFI{ODN6Mkez
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SUP-T1 M2TYc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jpPVHjiIoQvF2= NHfXXpQ4KGR? M3nzPIRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? M4HpdFI{ODN6Mkez
PEER Mnr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTuNgKBkc7:TR?= MW[3JIQ> Mo[5[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 NHSwV3czOzB|OEK3Ny=>
ALL-SIL M{LEV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7n[WYy6oDLzszN NGG4dHU4KGR? NVPoU3Y5\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 MYqyN|A{QDJ5Mx?=
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Karpas-45 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXRfVUy6oDLzszN M37pdlch\A>? MUXk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M{HJ[lI{ODN6Mkez
RPMI-8402 MmjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3WNgKBkc7:TR?= NUPrUXI4PyCm MYjk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> MnH0NlMxOzh{N{O=
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MOLT-4 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDnNgKBkc7:TR?= M3S0b|ch\A>? NX3QVolQ\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NIL3V2szOzB|OEK3Ny=>
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LOUCY NXPsbpZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moe3NgKBkc7:TR?= MnjoO{Bl MWfk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> NEixW28zOzB|OEK3Ny=>
MOLT-16 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEC3N4Ey6oDLzszN MYC3JIQ> NVfhN2x6\GWlcnXhd4V{KHSqZTDj[YxtKG63bXLldkB{cWewaX\pZ4FvfGy7 NWDZUVBKOjNyM{iyO|M>
MM1S MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPacJYxNTJizszN NXnONo5HOjRiaB?= MoLBTWM2OD1yLkWg{txO NX7tUodyOjJ6MkmyN|Q>
NCI-H929 MkHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;XeFAuOiEQvF2= M4Owe|I1KGh? NEnxZ3RKSzVyPUCuNlUh|ryP NHuyUY4zOjh{OUKzOC=>
KMS12-BM  M3;4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PVd|AuOiEQvF2= NVvxfIxnOjRiaB?= NILTNFRKSzVy78{eNkDPxE1? MlfuNlI5Ojl{M{S=
MDA-MB-436 NX7lVlZWTnWwY4Tpc44hSXO|YYm= NH\TbJMyKM7:TR?= MnHsNlQhcA>? NITyfpZz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU NV\pNnV2OjJ2OEi1PVA>
SUM149PT M4HSSmZ2dmO2aX;uJGF{e2G7 MVexJO69VQ>? NHjUXJkzPCCq NVyxfYMxemWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWC=> MVmyNlQ5QDV7MB?=
SUM1315MO2 MnPzSpVv[3Srb36gRZN{[Xl? MVKxJO69VQ>? NUDXXY5POjRiaB?= NIfIfZVz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvU MXeyNlQ5QDV7MB?=
HCC1937 NGTKd5lHfW6ldHnvckBCe3OjeR?= M4XmZlEh|ryP MUCyOEBp MWry[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4YhSUuW M1XWUlIzPDh6NUmw
HCC827 NVz2[mo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnNeJhDOC1|IN88US=> NF\UZWQ4OiCq MnnYTWM2OD1yLkOg{txO NEjkOHUzOTJ{MES3OC=>
PC-9  NX7HOGFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rxeVAuOyEQvF2= M3O3[VczKGh? NGnzb|JKSzVyPUCuPEDPxE1? NIHYS40zOTJ{MES3OC=>
LN229 NIH1cZFHfW6ldHnvckBCe3OjeR?= NGT4c|gyKM7:TR?= M3;ESFQ5KGh? MnrvbY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? MmnvNlExPjJ7OUO=
U87 M2[3Z2Z2dmO2aX;uJGF{e2G7 MlzpNUDPxE1? NH74UoY1QCCq MV7pcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v NHXz[o0zOTB4Mkm5Ny=>
U373 M3G2OGZ2dmO2aX;uJGF{e2G7 MYmxJO69VQ>? NF3SNW01QCCq NFfabHVqdmS3Y3XzJIF2fG:yaHHnc5NwdWViZn;ycYF1cW:w M33OPVIyODZ{OUmz
SF767 NFjRdnpHfW6ldHnvckBCe3OjeR?= MUmxJO69VQ>? NH;USmo1QCCq NXf6SldNcW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= NFTkbnkzOTB4Mkm5Ny=>
Mel-Juso NIrMRm9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHLxXHExNjBz4pETNVDjiIoQvF2= NFOySng4OiCq M3y1OolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MYGyNVA1QDd6NR?=
518A2  NV;kN21TS2WubDDWbYFjcWyrdImgRZN{[Xl? NXrvc3Z1OC5yMfMAl|Ex6oDLzszN NGD6dYk4OiCq NGjBcZRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M17iSlIyODR6N{i1
Mel-Juso  M3;pe2Z2dmO2aX;uJGF{e2G7 NXPsTI1tOC5yMEJihLMy6oDLzszN MmXqNlQhcA>? MorKd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= NFzqXJAzOTB2OEe4OS=>
518A2 MWnGeY5kfGmxbjDBd5NigQ>? MVmwMlAxOeLCk{JihKnPxE1? MkDuNlQhcA>? NV7ySnF7e3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZicHjvd5Bp[XSrZInsJIlvd3OrdH;sJFMuc2mwYYPlJIRwf26|dILlZY0hfGG{Z3X0dy=> NXy3[oN7OjFyNEi3PFU>
PC3  MlPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKyOIg> MXrHTVUxyqB;IEGwNEBvVQ>? NXL1[2ZJOjB3NUGwOlE>
U87MG MmjKSpVv[3Srb36gRZN{[Xl? M{L0WlAvOS1zIN88US=> MmLINlTjiImqwrC= M3\rRmROW09? NFvNPZVqdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= M3LPc|E6PjN|Nkiz
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U118MG M2rPeWZ2dmO2aX;uJGF{e2G7 M2izUFAvOS1zIN88US=> NVvKflRROjUkgJnoxsA> NUX0OY96TE2VTx?= NFjDdW9qdmirYnn0d{BRUTONLX3l[IlifGWmIIPp[45idGmwZx?= NXfGOIM1OTl4M{O2PFM>
U87MG M2Lpd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4m1VWlEPTB;MD6xOEDPxE1? NWT0e3g1OTl3OESyNlc>
IGROV-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzxTWM2OD1yLkC2JO69VQ>? M{HoZVE6PTh2MkK3
DETROIT562 NILFdpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\6TWM2OD1yLkGzJO69VQ>? NFHWfnUyQTV6NEKyOy=>
PC3  M2PQNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzDSo9{UUN3ME2wMlExKM7:TR?= MkHjNVk2QDR{Mke=
SKOV-3 NVL1Tm91T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX1NVdKSzVyPUCuNVIh|ryP NGn3Ro8yQTV6NEKyOy=>
HUVEC MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlf0TWM2OD1yLkC4JO69VQ>? M2fMOVE6PTh2MkK3
UCH-1  NULiNY5bTnWwY4Tpc44hSXO|YYm= M4HuW|AuPSEQvF2= M{f4R4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYn;0bEBCU1RiYX7kJI1VV1JiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MX:xPVUzQDR2MR?=
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UCH-1  Mon3RZBweHSxc3nzJGF{e2G7 NX7yUmxJOC5zLUGwJO69VQ>? MnjDNlQhcA>? NH;hfGFFVVOR M2LaTolv\HWlZYOgZZBweHSxc3nz MnXHNVk2Ojh2NEG=

... 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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