1. PI3K/Akt/mTOR
  2. PI3K
    mTOR

PI-103 

Cat. No.: HY-10115 Purity: 98.93%
Data Sheet SDS Handling Instructions

PI-103 is a potent PI3K/Akt and mTOR inhibitor with IC50 values of 2 nM for recombinant PI3K isoform p110α and 30 nM for mTOR.

For research use only. We do not sell to patients.
PI-103 Chemical Structure

PI-103 Chemical Structure

CAS No. : 371935-74-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO $55 In-stock
5 mg $50 In-stock
10 mg $65 In-stock
50 mg $200 In-stock
100 mg $360 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of PI-103:

    PI-103 purchased from MCE. Usage Cited in: Clin Cancer Res. 2014 Nov 1;20(21):5483-95.

    Effects of GSK1904529A and AZD6244 as single agents, respectively, on mediators of IGF-1R- and ERK1/ERK2-signaling pathways.(A–B) Effect of GSK1904529A on phosphorylation of IGF-1R (A) and Erk1/Erk2 (B). (C–E) Effect of AZD6244 on phosphorylation of IGF-1R (C), IGF-1R protein expression levels (D), and phosphorylation of Erk1/Erk2 (E). GSK1904529A is observed to inhibit phosphorylation of IGF-1R in a concentration-dependent manner (A), however shows no inhibitory activity against phosphorylation

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    • Biological Activity

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    • Technical Information

    • Purity & Documentation

    • References

    Description

    PI-103 is a potent PI3K/Akt and mTOR inhibitor with IC50 values of 2 nM for recombinant PI3K isoform p110α and 30 nM for mTOR.

    IC50 & Target

    IC50: 30 nM (mTOR), 2 nM/3 nM/3 nM/15 nM (p110α/β/δ/γ)[1]

    In Vitro

    PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines[1]. PI-103 is essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. 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 [2].

    In Vivo

    PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, and metastasis, as well as direct antiproliferative effects[1].PI-103 induces immunosuppression promoting in vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells[3].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.8706 mL 14.3530 mL 28.7059 mL
    5 mM 0.5741 mL 2.8706 mL 5.7412 mL
    10 mM 0.2871 mL 1.4353 mL 2.8706 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Phosphatidylinositide 3-kinase inhibitory activity is determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase is determined using a TR-FRET-based LanthaScreen method. Compounds (PI-103) are assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values are determined[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    For proliferation assays, MOLM14, OCI-AmL3 and MV4-11 cells are cultured during 48 h at 105 cells/mL, in triplicate, in 10% FCS, without or with 0.1 or 1 μM PI-103, and then pulsed 6 h with 1μCi (37 kBq) [4H]-thymidine. The amounts oadioactivity are determined after trichloracetic acid precipitation[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mouse: Five to six month old males of either FVB/N strain or nude BALB/c strain are injected subcutaneously with one million cells in PBS. When tumor reaches between 50 and 100 mm3, mice are treated with 10 mg/kg or 70 mg/kg of PI-103 and/or 50 mg/kg sorafenib by IP injection daily. Control mice are treated with the same volume of DMSO. Tumor size and mice weight is monitored every 2 days. When mice are sacrificed, tumors are dissected and processed[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    348.36

    Formula

    C₁₉H₁₆N₄O₃

    CAS No.

    371935-74-9

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    PI-103
    Cat. No.:
    HY-10115
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