1. PI3K/Akt/mTOR
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    mTOR
  3. Paxalisib

Paxalisib (Synonyms: GDC-0084)

Cat. No.: HY-19962 Purity: 99.28%
Handling Instructions

Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.

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

Paxalisib Chemical Structure

Paxalisib Chemical Structure

CAS No. : 1382979-44-3

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 72 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 85 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 370 In-stock
Estimated Time of Arrival: December 31
100 mg USD 680 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Paxalisib purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948.

    Cleaved-caspase-3 and cleaved-caspase-9 are significantly elevated in GDC-0084 (100-1000 nM)-treated cells.
    • Biological Activity

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    Description

    Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively[1].

    IC50 & Target[1]

    PI3Kα

    2 nM (Ki)

    PI3Kδ

    3 nM (Ki)

    PI3Kγ

    10 nM (Ki)

    PI3Kβ

    46 nM (Ki)

    mTOR

    70 nM (Ki)

    In Vitro

    Paxalisib (GDC-0084; Compound 16) maintains inhibition of each of the Class I PI3K isoforms but with more potent inhibition of mTOR. Paxalisib is also tested in five different GBM cell lines and is found to have antiproliferative EC50s ranging from 0.3 to 1.1 μM[1].

    In Vivo

    After a 25 mg/kg dose of Paxalisib (GDC-0084; Compound 16) administered orally, pAKT in normal mouse brain tissue is significantly inhibited at 1 and 6 h postdose. The potent inhibition of pAKT at both time points in this study demonstrates that Paxalisib inhibits its target behind a fully intact BBB. In addition to the pharmacodynamic effect in normal brain tissue, Paxalisib is studied in a subcutaneous U87 tumor xenograft model of glioblastoma in mice. In this study, Paxalisib achieves significant and dose-dependent tumor growth inhibition. Tumor growth inhibition is first observed at a 2.2 mg/kg dose level. Higher doses led to greater tumor growth inhibition, including tumor regressions at the 17.9 mg/kg dose level. Each of these doses is well tolerated for the duration of the study[1].

    Clinical Trial
    Molecular Weight

    382.42

    Formula

    C₁₈H₂₂N₈O₂

    CAS No.

    1382979-44-3

    SMILES

    NC1=NC=C(C2=NC(N3CCOCC3)=C4N=C(C(C)(C)OCC5)N5C4=N2)C=N1

    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 : 6 mg/mL (15.69 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6149 mL 13.0746 mL 26.1493 mL
    5 mM 0.5230 mL 2.6149 mL 5.2299 mL
    10 mM 0.2615 mL 1.3075 mL 2.6149 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Animal Administration
    [1]

    Mice[1]
    PTEN-null U-87 MG/M human glioblastoma cancer cells are cultured in RPMI 1640 media plus 1% L-glutamine with 10% fetal bovine serum. Cells in log-phase growth are harvested and resuspended in HBSS:Matrigel (1:1, v:v) for injection into female NCr nude mice aged 20 weeks. Animals receive five million cells subcutaneously in the right lateral thorax in 0.1 mL. Mice bearing established tumors in the range of 200-500 mm3 are separated into groups of equally sized tumors (n=6-7/group) to receive escalating doses of Paxalisib. Paxalisib is formulated once weekly in 0.5% methylcellulose and 0.2% Tween-80 at concentrations needed for target doses in a volume of 0.2 mL. All formulations are stored in a refrigerator and brought to room temperature and mixed well by vortex before oral administration by gavage once daily for 23 days. Tumor volumes are calculated. Changes in body weights are reported as a percentage change from the starting weight.

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

    References
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    Keywords:

    PaxalisibGDC-0084GDC0084GDC 0084PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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