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PX-478 2HCl

Cat. No. M5146
PX-478 2HCl Structure
Synonym:

PX-478 dihydrochloride

Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 155 In stock
50mg USD 400 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 1. PX-478
Method Western blot
Cell Lines MiaPaCa2 cells
Concentrations 10, 20, 50, 100, and 200 μM
Incubation Time 6h
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 394.12
Formula C13H20Cl4N2O3
CAS Number 685898-44-6
Purity >98%
Solubility DMSO 70 mg/mL
Water 70 mg/mL
Storage 4°C, dry, sealed
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PX-478 2HCl, PX-478 dihydrochloride supplier, HIF, inhibitors

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