PI-103

製品コードS1038 バッチS103804

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H16N4O3
分子量 348.36 CAS No. 371935-74-9
Solubility (25°C)* 体外 DMSO 24 mg/mL (68.89 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.000mg/ml (2.87mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
in vitro

PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. [1] This compound inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. [2] In blast cells, it inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. This chemical inhibits p110α >200-fold more potently than p110β. It also potently blocks production of PI(3,4)P2 and PIP3 in adipocytes and PIP3 in myotubes. [2] This compound inhibits phosphorylation of Akt with an IC95 100-fold lower than that for LY294002. Strikingly, it completely protects animals from stimulated decline in blood glucose. It has additive proapoptotic effects in blast cells and in immature leukemic cells. [2]
in vivo

When tumors reach 50-100 mm3, animals are randomized and treated with vehicle or PI-103. This compound exhibits significant activity, decreasing average tumor size by 4-fold after 18 days. [2] Mice treated with this chemical 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. This treatment is cytostatic to glioma xenografts. [2]
特徴 The first potent, synthetic mTOR inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ 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. This compound was 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 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 動物モデル 6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
投薬量 5 mg/kg
投与方法 Administered via i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/16647110/
  • https://pubmed.ncbi.nlm.nih.gov/16697955/
  • https://pubmed.ncbi.nlm.nih.gov/19584227/

カスタマーフィードバック

, Saraswati Sukumar of Johns Hopkins University School of Medicine

Data from [Mol Carcinog, 2012, 52, 667-75 ]

Data from [Mol Carcinog, 2012, ahead of print]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

hnRNPL phase separation activates PIK3CB transcription and promotes glycolysis in ovarian cancer [ Nat Commun, 2025, 16(1):4828] PubMed: 40413189
Bile acid-FXR signaling facilitates the long-term maintenance of hepatic characteristics in human iPSC-derived organoids [ Cell Rep, 2025, 44(5):115675] PubMed: 40367952
Autophagy and PXR Crosstalk in the Regulation of Cancer Drug Metabolism and Resistance According to Gene Mutational Status in Colorectal Cancer [ Genes (Basel), 2025, 16(8)892] PubMed: 40869940
Development of Acquired Resistance in Alpelisib-treated Gastric Cancer Cells With PIK3CA Mutations and Overcoming Strategies [ Anticancer Res, 2025, 45(5):1877-1896] PubMed: 40295072
TMEM176B Promotes EMT via FGFR/JNK Signalling in Development and Tumourigenesis of Lung Adenocarcinoma [ Cancers (Basel), 2024, 16(13)2447] PubMed: 39001509
Overcoming brain-derived therapeutic resistance in HER2+ breast cancer brain metastasis [ bioRxiv, 2024, 2024.02.19.581073] PubMed: 38529509
Young and undamaged recombinant albumin alleviates T2DM by improving hepatic glycolysis through EGFR and protecting islet β cells in mice [ J Transl Med, 2023, 21(1):89] PubMed: 36747238
Young and undamaged recombinant albumin alleviates T2DM by improving hepatic glycolysis through EGFR and protecting islet β cells in mice [ J Transl Med, 2023, 21(1):89] PubMed: 36747238
RIDR-PI-103, ROS-activated prodrug PI3K inhibitor inhibits cell growth and impairs the PI3K/Akt pathway in BRAF and MEK inhibitor-resistant BRAF-mutant melanoma cells [ Anticancer Drugs, 2023, 34(4):519-531] PubMed: 36847042
Synergistic effects of complex drug combinations in colorectal cancer cells predicted by logical modelling [ Front Syst Biol, 2023, Volume 3] PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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