PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. 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. PX-478 causes reduced fibrosis and fewer inflammatory infiltrates in high-fat-diet mice adipose tissues.
|Source||Oncotarget (2017). Figure 1. PX-478|
|Cell Lines||MiaPaCa2 cells|
|Concentrations||10, 20, 50, 100, and 200 μM|
|Results||When MiaPaCa2 cells were exposed to the highest concentration of PX-478 and noscapine, HIF-1 expression levels equaled to 55% and 62% of the control value, respectively.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL
Water 70 mg/mL
Selective inhibition of hypoxia-inducible factor 1α ameliorates adipose tissue dysfunction.
Sun K, et al. Mol Cell Biol. 2013 Mar;33(5):904-17. PMID: 23249949.
PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells.
Palayoor ST, et al. Int J Cancer. 2008 Nov 15;123(10):2430-7. PMID: 18729192.
Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1alpha.
Koh MY, et al. Mol Cancer Ther. 2008 Jan;7(1):90-100. PMID: 18202012.
Antitumor activity and pharmacodynamic properties of PX-478, an inhibitor of hypoxia-inducible factor-1alpha.
Welsh S, et al. Mol Cancer Ther. 2004 Mar;3(3):233-44. PMID: 15026543.
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