1. Metabolic Enzyme/Protease
    Autophagy
  2. HIF/HIF Prolyl-Hydroxylase
    Autophagy
  3. PX-478

PX-478 

Cat. No.: HY-10231 Purity: >98.0%
Handling Instructions

PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.

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

PX-478 Chemical Structure

PX-478 Chemical Structure

CAS No. : 685898-44-6

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5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PX-478 purchased from MCE. Usage Cited in: Front Immunol. 2018 Jul 23;9:1667.

    Manipulation of the protein level of hypoxia-inducible factor 1 alpha (HIF-1α) in NR8383. 50 µM PX478 treatment for 20 h is used to downregulate the HIF-1α protein level in NR8383 cells (A). 1 mM DMOG treatment for 8 h is used to upregulate the HIF-1α protein level in NR8383 cells (B).

    PX-478 purchased from MCE. Usage Cited in: Sci Transl Med. 2020 Apr 8;12(538). pii: eaay1620.

    Representative pimonidazole staining of kidney sections from 16-week-old MRL/lpr mice treated with PBS or PX-478, and quantification of pimonidazole-positive cortical tubular cells.
    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier[1][2].

    IC50 & Target

    HIF-1α[1]

    In Vitro

    PC3 and DU 145 cells express HIF-1α protein are treated with PX-478 for 20 hr under normoxia. PC3 cells are more sensitive to PX-478 as compared with DU 145 cells. Densitometric analysis shows that the IC50 for HIF-1α inhibition for PC3 cells under normoxic condition is 20-25 μM, whereas the IC50 for HIF-1α inhibition for the DU 145 cells is 40-50 μM. PC3 and DU 145 cells are treated with different concentrations of PX-478 (10, 20, 30, 40, 50, and 60 μM) for 18-20 hr under normoxia or hypoxia. Under normoxia, PC3 cells are more sensitive to PX-478 than DU 145 cells. IC50 for clonogenic survival (n=3) is 17 μM for PC3 cells and 35 μM for DU 145 cells. When cells are treated with the drug under hypoxic condition for 18 hr, the IC50 is 16 μM for PC3 cells and 22 μM for DU 145 cells. Thus DU 145 cells are more sensitive to PX-478 under hypoxic condition[1].

    In Vivo

    PX-478 is administered to mice with congenital HO (Nfatc1-Cre/caACVR1fl/fl) every other day starting from birth for 2 wk. Treated mice have significantly less ectopic bone at the ankle joints compared with mutant mice treated with vehicle (6.8 mm3 vs. 2.2 mm3, P<0.01)[2].

    Clinical Trial
    Molecular Weight

    394.12

    Formula

    C₁₃H₂₀Cl₄N₂O₃

    CAS No.

    685898-44-6

    SMILES

    [O-][N+](CCCl)(CCCl)C(C=C1)=CC=C1C[[email protected]](N)C(O)=O.Cl.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, stored under nitrogen, away from moisture

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (253.73 mM; Need ultrasonic)

    H2O : ≥ 35 mg/mL (88.81 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5373 mL 12.6865 mL 25.3730 mL
    5 mM 0.5075 mL 2.5373 mL 5.0746 mL
    10 mM 0.2537 mL 1.2686 mL 2.5373 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [1]

    To determine the effect of PX-478 in combination with radiation, cells are treated with PX-478 for 24 hr under normoxic condition, irradiated and plated after 1 hr. Colonies are stained with crystal violet after 12 days and the colonies of >50 cells are counted. For combination treatments, net survival is calculated by correcting the toxicity of PX-478 alone. Enhancement factor (EF) is calculated by dividing the dose of radiation required to reduce plating efficiency to 10% when cells are treated with radiation alone by the dose of radiation required to reduce plating efficiency to 10% when cells are treated with PX-478 and radiation[1].

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

    Animal Administration
    [2]

    Mice[2]
    Burn/tenotomy or hybrid HO mice are administered PX-478 (100 mg/kg) or Rapamycin (5 mg/kg) in PBS solution via intraperitoneal injection. Mice receive injections every other day for the duration of the study. Nfatc1-Cre/caACVR1fl/wt mice are administered PX-478 (100 mg/kg) every other day for a total of 2 wk.

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

    References

    Purity: >98.0%

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    Keywords:

    PX-478PX478PX 478HIF/HIF Prolyl-HydroxylaseAutophagyHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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