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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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
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SH-SY5Y MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTLU3MxNThizszN Mn61NlQwPDhxN{KgbC=> M2PDfYlv\HWlZYOgeIlu\S1iYX7kJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnubIljcXSrb36gc44hVkJiY3XscEBoem:5dHi= Mk\BNlYzOjR4OEG=
SH-SY5Y  NXG2e3JHSXCxcITvd4l{KEG|c3H5 NG\nfYUyKM7:TR?= NHf3VWUxNjVvMkSgbC=> NYH3WZhze2Wwc3n0bZpmeyCwZYXyc4Jt[XO2b33hJINmdGy|IITvJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[XCxcITvd4l{ MkLRNlYzOjR4OEG=
G 35 SC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHJNnFTOC5yNT2yNEDPxE1? Ml3oNlQwPzJiaB?= NVHLbFM2TE2VTx?= MX\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MX2yOlEzOTJ3MR?=
G 38 SC NXP6UlBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2e3eVAvODVvMkCg{txO NXXiOJVjOjRxN{KgbC=> NXnaSXA1TE2VTx?= NXX5WHpXcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NV;GWopnOjZzMkGyOVE>
G 40 SC MkH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\WZlAvODVvMkCg{txO NUPPSGVmOjRxN{KgbC=> NEfXdFdFVVOR NInvTHVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 M1;2NFI3OTJzMkWx
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G 40 DC MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoT5NE4xPS1{MDFOwG0> MVmyOE84OiCq NGK4OVVFVVOR M{\EO4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh[W6mIITpcYUh\GWyZX7k[Y51dHl? MlvyNlYyOjF{NUG=
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SW872 NHfud3NCeG:ydH;zbZMhSXO|YYm= NXTONItEOC5yMT2wMlUh|ryP MVi0PEBp MlTTbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MmfrNlQ3QTV4M{K=
SW982 NXzqblA2SXCxcITvd4l{KEG|c3H5 MnTpNE4xOS1yLkWg{txO NE\QRmM1QCCq M4rRU4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NULZ[3REOjR4OUW2N|I>
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AGS LG NVrXbYRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDhTo9KSzVyPUCuNFUhyrFiMD6wNFEh|ryP NITzfHczPDV7N{S3PC=>
HGC27 HG NGHNXpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWKyOlBCUUN3ME2wMlM5KMLzIECuNFIzKM7:TR?= MnHZNlQ2QTd2N{i=
HGC27 LG NXy4dm17T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXoV2RKSzVyPUCuNFIhyrFiMD6wNFQh|ryP MV:yOFU6PzR5OB?=
MKN45 HG NXzP[JhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnF[YhpUUN3ME2xMlAyKMLzIECuNFUyKM7:TR?= MoL2NlQ2QTd2N{i=
MKN45 LG NXfOe|NZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHRTWM2OD1yLki3JOKyKDBwMEOwJO69VQ>? MlzXNlQ2QTd2N{i=
NUGC4 HG M3fCTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:1eJlKSzVyPUG0MlAhyrFiMz65NVMh|ryP NVTmTFNrOjR3OUe0O|g>
NUGC4 LG MkLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PyTWlEPTB;MUSuNEDDuSB3LkOyNUDPxE1? MVSyOFU6PzR5OB?=
A549 NUDCRYo1TnWwY4Tpc44hSXO|YYm= MUiwMlI2NzBwNT:xJO69VQ>? NF7kfmUzPCCq NHT0dXJqdmirYnn0d{BCc3RicHjvd5Bpd3K7bHH0bY9vKHOuaXfoeIx6 MlL0NlQ{PTF2MkW=
H460 MYPGeY5kfGmxbjDBd5NigQ>? NEn4bGYxNjJ3L{CuOU8yKM7:TR?= M2jIOFI1KGh? MkXUbY5pcWKrdIOgRYt1KHCqb4PwbI9zgWyjdHnvckB{dGmpaITsfS=> MV[yOFM2OTR{NR?=
H661 NE\OZY5HfW6ldHnvckBCe3OjeR?= MYmwMlI2NzBwNT:xJO69VQ>? MoLkNlQhcA>? M{G4NIlvcGmkaYTzJGFsfCCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NVnBT2tpOjR|NUG0NlU>
SAS NVvmPHk5TnWwY4Tpc44hSXO|YYm= MXuwMlI2NzBwNT:xJO69VQ>? M{LO[VI1KGh? NWLKVGpXcW6qaXLpeJMhSWu2IIDoc5NxcG:{eXzheIlwdiC|aXfubYZq[2GwdHz5 M1jUW|I1OzVzNEK1
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FaDu MXfGeY5kfGmxbjDBd5NigQ>? M4i5VVAvOjVxMD61M|Eh|ryP MUWyOEBp MYfpcohq[mm2czDBb5QheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MXuyOFM2OTR{NR?=
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MDA-MB-468 NEmwTVVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWOwMlMh|ryP NIjsbnQ4OiCq MkG4[Y5p[W6lZYOgZ5l1d3SxeHnjJIVn\mWldIOgc4YhWEl|Sz;BT3QheGG2aIfhfUBqdmirYnn0c5J{ MVWyN|YxOTB5NB?=
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ALL-SIL MnfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXyx5qCK|ryP MYK3JIQ> M3nPdoRm[3KnYYPld{B1cGViY3XscEBvfW2kZYKgd4lodmmoaXPhcpRtgQ>? NHnyRWgzOzB|OEK3Ny=>
KE37 NFT0eVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUKx5qCK|ryP NVPOcok4PyCm MoLj[IVkemWjc3XzJJRp\SClZXzsJI52dWKncjDzbYdvcW[rY3HueIx6 M4TFW|I{ODN6Mkez
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MM1S MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPMb4FWOC1{IN88US=> NH7tUIwzPCCq NVn5NYJ{UUN3ME2wMlUh|ryP MnHzNlI5Ojl{M{S=
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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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