PX-478 2HCl

Catalog No.S7612

PX-478 2HCl Chemical Structure

Molecular Weight(MW): 394.12

PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

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4 Customer Reviews

  • Canonical hedgehog transactivates HIF-1α, which mediates the angiogenic properties of HSCs. HSCs were treated with PX-478, cyclopamine or GANT-58 at indicated concentrations for 24 h (A-C) or 3 h (D). (A) Cell viability was determined using Cell Counting Kit-8. Data were expressed as percentage of control value (n = 6). *P < 0.05 versus control, non-parametric analyses with Kruskal-Wallis H test. (B, E) Real-time PCR analyses of angiogenic cytokines (B) and HIF-1α (E). Data were expressed as fold of control value (n = 6). *P < 0.05 versus control, non-parametric analyses with Kruskal-Wallis H test. (C, F) Western blot analyses of angiogenic cytokines (C) and HIF-1α (F) (n = 3). (D) Tubulogenesis assay with quantification of number of closed intercellular compartments (100× magnification) (n = 5). *P < 0.05 versus control, Student's t-test.

    Br J Pharmacol, 2017, 174(5):409-423. PX-478 2HCl purchased from Selleck.

    PX-478 inhibits EMT of ESCC. Expression levels of Vimentin and N-cadherin were decreased while E-cadherin was increased in the PX-478 treatment group

    Am J Cancer Res, 2017, 7(5):1198-1212. PX-478 2HCl purchased from Selleck.

  • (A) Cell proliferation was determined using MTT assay. Significance: *P < 0.05 versus control. (B) Real-time PCR analyses of mRNA expression of CD31 and vWF. Significance: *P < 0.05 versus control. (C) Western blot analyses of protein expression of CD31 and vWF.

    Biomed Pharmacother, 2017, 90:928-934. PX-478 2HCl purchased from Selleck.

    Following pretreatment with DMSO, PX-478 or trigonelline, NS-KD and TAK1-KD VSMCs were treated with PBS or IL-1a for 24 h. While whole cell lysates were immunoblotted with anti-C/EBPb and anti-b-actin, RNA and medium was analyzed for SDF-1 expression using qRT-PCR and ELISA.

    Biochem Biophys Res Commun, 2015, 463(1-2): 130-6. PX-478 2HCl purchased from Selleck.

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Biological Activity

Description PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.
Targets
HIF-1α [1]
In vitro

PX-478 lowers HIF-1α protein levels and HIF-1 transactivation in hypoxia and in normoxia in a variety of cancer cell lines, but has a more pronounced effect on translation of proteins, such as HIF-1α in hypoxia. [2] PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells. [3]

In vivo In HT-29 human colon cancer xenografts, PX-478 suppresses HIF-1alpha levels and inhibits the expression of HIF-1 target genes including vascular endothelial growth factor and the glucose transporter-1. In addition, PX-478 (100 or 120 mg/kg i.p.) also shows antitumor activity including cures against several established human tumor xenografts that is related to the levels of HIF-1α. [1] In high-fat-diet mice, PX-478 causes reduced fibrosis and fewer inflammatory infiltrates in their adipose tissues. [4]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Mice bearing MCF-7 human breast cancer, HT-29 colon cancer, PC-3 prostate cancer, DU-145 prostate cancer, OvCar-3 ovarian cancer, A-549 non-small cell lung cancer, SHP-77 small cell lung cancer, and Caki-1 renal cancer, Panc-1, MiaPaCa, or BxPC-3 pancreatic cancer xenografts.
  • Formulation: 0.9% NaCl
  • Dosages: 100 or 120 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (197.9 mM)
Water 78 mg/mL (197.9 mM)
Ethanol 78 mg/mL (197.9 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 394.12
Formula

C13H20Cl4N2O3

CAS No. 685898-44-6
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00522652 Completed Advanced Solid Tumors|Lymphoma Cascadian Therapeutics Inc. August 2007 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID