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.
6 Customer Reviews
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Glucose uptake and lactate production were determined in H460 and A549 lung cancer cells in the presence of the HIF1α inhibitor, PX-478 (10 μM) (** p < 0.01)
Theranostics, 2018, 8(15):4050-4061. PX-478 2HCl purchased from Selleck.
Cells were untreated or treated with PX-478 and stimulated with cytokines. iNOS protein expression was examined by immunoblot at 6 h post-stimulation *p < 0.05, ***p < 0.001.
Free Radic Biol Med, 2018, 130:278-287. PX-478 2HCl purchased from Selleck.
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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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| Cell Data |
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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 |
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| 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 |
| NCT00522652 | Completed | Advanced Solid Tumors|Lymphoma | Cascadian Therapeutics Inc.|Seattle Genetics 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.
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