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

PX-478 

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

PX-478 est un inhibiteur de HIF-1α qui est oralement actif avec des activités puissantes antitumorales. PX-478 peut traverser la barrière hémato-encéphalique.

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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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 30 publication(s) in Google Scholar

PX-478 Related Antibodies

Top Publications Citing Use of Products

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

    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.

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

    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).

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • 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].

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

    PX-478 Related Antibodies
    In Vivo

    PX-478 is administered to mice with congenital heart disease (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].

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

    394.12

    Appearance

    Solid

    Formula

    C13H20Cl4N2O3
    CAS No.
    SMILES

    [O-][N+](CCCl)(CCCl)C(C=C1)=CC=C1C[C@H](N)C(O)=O.Cl.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

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

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

    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.
    In Vivo:
    • 1.

      Add each solvent one by one:  Saline

      Solubility: 16.67 mg/mL (42.30 mM); Clear solution; Need ultrasonic

    • 2.

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

      Solubility: ≥ 5 mg/mL (12.69 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 5 mg/mL (12.69 mM); Clear solution

    • 4.

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

      Solubility: ≥ 5 mg/mL (12.69 mM); Clear solution

    • 5.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    • 6.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    • 7.

      Add each solvent one by one:  1% DMSO    99% saline

      Solubility: ≥ 0.5 mg/mL (1.27 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: ≥98.0%

    COA (251 KB) HNMR (242 KB)

    Handling Instructions (2659 KB)
    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
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    PX-478 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

    Keywords:

    PX-478685898-44-6PX478PX 478HIF/HIF Prolyl-HydroxylaseAutophagyHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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