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

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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 MnHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzSUpUxNThizszN NIHkfm8zPC92OD:3NkBp M2HTTolv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= NFu3WYYzPjJ{NE[4NS=>
SH-SY5Y MnLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTF[m1EOC16IN88US=> Ml;MNlQwPDhxN{KgbC=> NH\D[nRqdmS3Y3XzJJRqdWVvIHHu[EBkd26lZX70doF1cW:wLXTldIVv\GWwdDDpcohq[mm2aX;uJI9vKE6EIHPlcIwh\3Kxd4To NF7BZ3MzPjJ{NE[4NS=>
SH-SY5Y  MnzQRZBweHSxc3nzJGF{e2G7 NXrJfFFoOSEQvF2= M3m5TFAvPS1{NDDo NGrPdpp{\W6|aYTpfoV{KG6ndYLvZoxie3SxbXGgZ4VtdHNidH:g[I95d3K3YnnjbY4ucW6mdXPl[EBieG:ydH;zbZM> MWWyOlIzPDZ6MR?=
G 35 SC MorkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\rZYlPOC5yNT2yNEDPxE1? NH6zWGEzPC95MjDo NILCOpNFVVOR M1ztNIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? NV7uOGk6OjZzMkGyOVE>
G 38 SC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2wMlA2NTJyIN88US=> NIK0RXkzPC95MjDo NX\yUHRHTE2VTx?= M3LkTYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MXyyOlEzOTJ3MR?=
G 40 SC NHzsPYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;XWlMxNjB3LUKwJO69VQ>? Mk[zNlQwPzJiaB?= NFi1bGdFVVOR NIfrfGlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MX2yOlEzOTJ3MR?=
G 35 DC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOwMlA2NTJyIN88US=> NFrqTHczPC95MjDo NET4VppFVVOR NISzXY5qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NWjQdJNUOjZzMkGyOVE>
G 38 DC NVj0PYlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLJc2UxNjB3LUKwJO69VQ>? NGfqS3MzPC95MjDo NH7oOW9FVVOR NXfWVZd7cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M3zTTFI3OTJzMkWx
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BT549 NVW5c3ROS2WubDDWbYFjcWyrdImgRZN{[Xl? NYfYdlY5OC1|IN88US=> MkniO|IhcA>? M3ewbolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{TLOlI2PzJzNEG5
MDA-MB-231 NYDFcIx4S2WubDDWbYFjcWyrdImgRZN{[Xl? Mn7RNE0{KM7:TR?= NH7LfJM4OiCq MXHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MV[yOVczOTRzOR?=
MDA-MB-468 NGXT[4lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NG\XVJMxNTNizszN MYq3NkBp MVPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MUGyOVczOTRzOR?=
MDA-MB-436 NV:zXHlqS2WubDDWbYFjcWyrdImgRZN{[Xl? NETjXFQxNTNizszN MXy3NkBp NGDwOpNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MlzqNlU4OjF2MUm=
SUM149PT NH[1dVBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXqwMVMh|ryP NWDLXnJwPzJiaB?= M{\PPYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MlrNNlU4OjF2MUm=
MDA-MB-468 MVHGeY5kfGmxbjDBd5NigQ>? NFq2cVExNjBzLUGwJO69VQ>? NIfVXXEzPCCq M3G0VIRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? NVrwVpVUOjV5MkG0NVk>
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HS578T MW\GeY5kfGmxbjDBd5NigQ>? NVTkbI5pOC5yMT2xNEDPxE1? MWGyOEBp M324SIRwf26{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kDPui2WclPQNUwh[y2PeXOgZY5lKGO7Y3zpckBGKHC{b4TlbY5{yqB? M2rISlI2PzJzNEG5
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SW982 MVfBdI9xfG:|aYOgRZN{[Xl? NGL0SFUxNjBzLUCuOUDPxE1? M1rIPVQ5KGh? MVjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MmfkNlQ3QTV4M{K=
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HGC27 LG Ml3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfaNI1wUUN3ME2wMlAzKMLzIECuNFA1KM7:TR?= NHX0cnIzPDV7N{S3PC=>
MKN45 HG NXz5VlZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGWz[WRKSzVyPUGuNFEhyrFiMD6wOVEh|ryP NHzXRpIzPDV7N{S3PC=>
MKN45 LG MlvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HmN2lEPTB;MD64O{DDuSByLkCzNEDPxE1? MoXFNlQ2QTd2N{i=
NUGC4 HG NVr3[XJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml20TWM2OD1zND6wJOKyKDNwOUGzJO69VQ>? NVXhR|NuOjR3OUe0O|g>
NUGC4 LG NHjOcIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTF2LkCgxtEhPS5|MkGg{txO MkToNlQ2QTd2N{i=
A549 MX\GeY5kfGmxbjDBd5NigQ>? NFGzZnUxNjJ3L{CuOU8yKM7:TR?= MXWyOEBp NUPYS3NYcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|bHnnbJRtgQ>? MWeyOFM2OTR{NR?=
H460 NX;peGJkTnWwY4Tpc44hSXO|YYm= MkTTNE4zPS9yLkWvNUDPxE1? M4rEcFI1KGh? MWPpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNtcWeqdHz5 MWqyOFM2OTR{NR?=
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SAS M{L3XGZ2dmO2aX;uJGF{e2G7 M4TOWFAvOjVxMD61M|Eh|ryP M4PPdlI1KGh? NXmzc5E1cW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 NVjLbWNjOjR|NUG0NlU>
UT5 NVHpTZVbTnWwY4Tpc44hSXO|YYm= Mnv5NE4zPS9yLkWvNUDPxE1? NF\RfYYzPCCq MV7pcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? NWDBNok2OjR|NUG0NlU>
FaDu NGTTdFdHfW6ldHnvckBCe3OjeR?= MYSwMlI2NzBwNT:xJO69VQ>? NYi3bIRHOjRiaB?= MV7pcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MWmyOFM2OTR{NR?=
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DND41 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDMOWIy6oDLzszN M4T0S|ch\A>? NFHOVnFl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? NGLhdpEzOzB|OEK3Ny=>
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ALL-SIL M{XycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPKOphCOeLCid88US=> MlPLO{Bl NIPJU3hl\WO{ZXHz[ZMhfGinIHPlcIwhdnWvYnXyJJNq\26rZnnjZY51dHl? MVOyN|A{QDJ5Mx?=
KE37 Ml;vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWGx5qCK|ryP Mm[2O{Bl MWjk[YNz\WG|ZYOgeIhmKGOnbHygcpVu[mW{IIPp[45q\mmlYX70cJk> M324dVI{ODN6Mkez
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RPMI-8402 NFXhTJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnsOW13OeLCid88US=> NUTTe3pHPyCm M4rXe4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? MonzNlMxOzh{N{O=
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MOLT-16 NHzSeldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7nbG9zOeLCid88US=> NYfxbFJ{PyCm M2\sd4Rm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NHnlWYQzOzB|OEK3Ny=>
MM1S MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVruTYdXOC1{IN88US=> MmSwNlQhcA>? Mn7BTWM2OD1yLkWg{txO MnG5NlI5Ojl{M{S=
NCI-H929 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3uy[FAuOiEQvF2= MYWyOEBp Mn7lTWM2OD1yLkK1JO69VQ>? MnPVNlI5Ojl{M{S=
KMS12-BM  NXXRcFViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvPNE0zKM7:TR?= MmG1NlQhcA>? MVjJR|Ux97zgMjFOwG0> MV6yNlgzQTJ|NB?=
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PC-9  MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDnNWkxNTNizszN M1TjbFczKGh? M2T0cGlEPTB;MD64JO69VQ>? MVqyNVIzODR5NB?=
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U87 NV\rSVl2TnWwY4Tpc44hSXO|YYm= M{nUUlEh|ryP M4fEWVQ5KGh? MVzpcoR2[2W|IHH1eI9xcGGpb4PvcYUh\m:{bXH0bY9v Mln5NlExPjJ7OUO=
U373 MXjGeY5kfGmxbjDBd5NigQ>? NFvK[VAyKM7:TR?= M{HjRlQ5KGh? MnP2bY5lfWOnczDheZRweGijZ3;zc41mKG[xcn3heIlwdg>? MYSyNVA3Ojl7Mx?=
SF767 NV3sdIpPTnWwY4Tpc44hSXO|YYm= M1rieVEh|ryP NGLUS5E1QCCq NX;tNnk2cW6mdXPld{BifXSxcHjh[49{d22nIH\vdo1ifGmxbh?= NGXjfoozOTB4Mkm5Ny=>
Mel-Juso NGC0O4pE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnvINE4xOeLCk{Gw5qCK|ryP MYS3NkBp M3z3RYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NIPvTpMzOTB2OEe4OS=>
518A2  M{\CRWNmdGxiVnnhZoltcXS7IFHzd4F6 NIDGWm8xNjBz4pETNVDjiIoQvF2= M336ZlczKGh? MmjsbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NILDdIkzOTB2OEe4OS=>
Mel-Juso  NXnzcHd[TnWwY4Tpc44hSXO|YYm= MmS2NE4xODIkgKOx5qCK|ryP NH[5eWEzPCCq M{XLZpN2eHC{ZYPz[ZMheGixc4Doc5J6dGG2aX;uJI9nKHCqb4PwbIF1cWS7bDDpco9{cXSxbDCzMYtqdmG|ZTDkc5dve3S{ZXHtJJRiemendIO= NV3wb4oyOjFyNEi3PFU>
518A2 NXjzbG9YTnWwY4Tpc44hSXO|YYm= NELIZWUxNjByMfMAl|HjiIoQvF2= NFziUmgzPCCq MmrOd5VxeHKnc4Pld{BxcG:|cHjvdplt[XSrb36gc4YheGixc4DoZZRq\HmuIHnuc5NqfG:uIEOtb4lv[XOnIHTve45{fHKnYX2geIFz\2W2cx?= NU\X[XN1OjFyNEi3PFU>
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U138MG MoWySpVv[3Srb36gRZN{[Xl? MWOwMlEuOSEQvF2= MV6yOQKBkWkEoB?= MlXESG1UVw>? M2CxcYlvcGmkaYTzJHBKO0tvbXXkbYF1\WRic3nncoFtcW6p NW\3Xo1pOTl4M{O2PFM>
U118MG MWTGeY5kfGmxbjDBd5NigQ>? MUOwMlEuOSEQvF2= M17Z[lI16oDLaNMg MU\EUXNQ MUfpcohq[mm2czDQTVNMNW2nZHnheIVlKHOrZ37hcIlv\w>? M4qwVlE6PjN|Nkiz
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PC3  NEjMeVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTJZ2d5UUN3ME2wMlExKM7:TR?= NIDReZYyQTV6NEKyOy=>
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UCH-1  NXnBdZJqTnWwY4Tpc44hSXO|YYm= NIX5Z|AxNTVizszN MXvpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigRWtVKGGwZDDtWG9TKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXHKUlhWOTl3Mki0OFE>
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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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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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