1. PI3K/Akt/mTOR
  2. PI3K
  3. PI-3065

PI-3065 

Cat. No.: HY-12235 Purity: 99.82%
Handling Instructions

PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.

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

PI-3065 Chemical Structure

PI-3065 Chemical Structure

CAS No. : 955977-50-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 134 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 768 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE PI-3065

    PI-3065 purchased from MCE. Usage Cited in: Cell Signal. 2016 Mar;28(3):148-56.

    Inhibition of PI3K p110δ signalling, either by PI3KCD-/- or using PI3K p110δ inhibitor PI-3065, significantly blocks LPS-induced GSK3α phosphorylation.
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    Description

    PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.

    IC50 & Target[1]

    p110δ

    5 nM (IC50)

    p110β

    600 nM (IC50)

    p110α

    910 nM (IC50)

    In Vitro

    PI-3065 exhibits no inhibition of the growth of 4T1 cells, which do not express detectable levels of p110δ[1].

    In Vivo

    PI-3065 (75 mg/kg, p.o.) inhibits the growth of 4T1 tumours in the BALB/c mice without obvious body weight loss[1].

    Molecular Weight

    506.64

    Formula

    C₂₇H₃₁FN₆OS

    CAS No.

    955977-50-1

    SMILES

    FC(C=CC1=C2C=CN1)=C2C3=NC4=C(SC(CN5CCN(CC6CC6)CC5)=C4)C(N7CCOCC7)=N3

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (49.34 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9738 mL 9.8689 mL 19.7379 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 mL
    10 mM 0.1974 mL 0.9869 mL 1.9738 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [1]

    Female WT BALB/c mice are orthotopically inoculated in the mammary fat pad on day 0 with 1×105 4T1 cells. Drug (75 mg/kg PI-3065, once daily) or vehicle (0.5% methylcellulose with 0.2% Tween 80) is administered by oral gavage from day -1 (administered 12 h prior to tumour cell inoculation). Tumour growth is monitored weekly by caliper measurement or by measuring luminescence using a Xenogen imaging platform. On day 35, mice are euthanized, tumours and peripheral organs extracted for in vitro luminescence measurement, followed by fixation in 4% PFA and H&E staining. KPC mice are allowed to develop advanced lesions of 5-10 mm (determined by ultrasound imaging) before treatment with vehicle or PI-3065 for a total of 14 days.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.82%

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    Product Name:
    PI-3065
    Cat. No.:
    HY-12235
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