PX-478 2HCl
Catalog No.S7612
Molecular Weight(MW): 394.12
PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.
4 Customer Reviews
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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.
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(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.
Purity & Quality Control
Choose Selective HIF Inhibitors
Biological Activity
| Description | PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1. | |
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| 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] |
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| 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] |
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Solubility (25°C)
| In vitro | DMSO | 78 mg/mL (197.9 mM) |
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| 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 |
| in solvent | |
| 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.|Seattle Genetics Inc. | August 2007 | Phase 1 |
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