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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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.
(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
|Description||PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.|
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.  PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells. 
|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.  In high-fat-diet mice, PX-478 causes reduced fibrosis and fewer inflammatory infiltrates in their adipose tissues. |
|In vitro||DMSO||78 mg/mL (197.9 mM)|
|Water||78 mg/mL (197.9 mM)|
|Ethanol||78 mg/mL (197.9 mM)|
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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|
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