1. PI3K/Akt/mTOR
  2. PI3K
    mTOR

PI-103 Hydrochloride 

Cat. No.: HY-10115A Purity: 99.78%
Handling Instructions

PI-103 Hydrochloride is a potent PI3K and mTOR inhibitor with IC50s of 2 nM, 3 nM, 3 nM, 15 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 23 nM.

For research use only. We do not sell to patients.

PI-103 Hydrochloride Chemical Structure

PI-103 Hydrochloride Chemical Structure

CAS No. : 371935-79-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 78 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 432 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of PI-103 Hydrochloride:

    PI-103 Hydrochloride 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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PI-103 Hydrochloride is a potent PI3K and mTOR inhibitor with IC50s of 2 nM, 3 nM, 3 nM, 15 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 23 nM.

    IC50 & Target[1]

    p110α

    2 nM (IC50)

    p110β

    3 nM (IC50)

    p110δ

    3 nM (IC50)

    p110γ

    15 nM (IC50)

    mTORC1

    20 nM (IC50)

    mTORC2

    83 nM (IC50)

    DNA-PK

    23 nM (IC50)

    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]. PI-103 potently inhibits both the rapamycin-sensitive (mTORC1, IC50=20 nM) and rapamycin-insensitive (mTORC2, IC50=83 nM) complexes of the protein kinase mTOR[4].

    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 2.5986 mL 12.9931 mL 25.9862 mL
    5 mM 0.5197 mL 2.5986 mL 5.1972 mL
    10 mM 0.2599 mL 1.2993 mL 2.5986 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [4]

    IC50 values are measured using either a standard thin-layer chromatography (TLC) assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC50 determinations are repeated two to four times, and the reported value is the average of these independent measurements[4].
    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) [3H]-thymidine. The amounts of radioactivity 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]

    Mice[3]
    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

    384.82

    Formula

    C₁₉H₁₇ClN₄O₃

    CAS No.

    371935-79-4

    SMILES

    OC1=CC(C2=NC3=C(OC4=C3C=CC=N4)C(N5CCOCC5)=N2)=CC=C1.[H]Cl

    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

    DMSO: 4.1 mg/mL; H2O: < 4 mg/mL

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

    Purity: 99.78%

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