CAS No: 685898-44-6
For research use only. Not Intended for Therapeutic Use!
|Synonyms:||(S)-4-(2-amino-2-carboxyethyl)-N,N-bis(2-chloroethyl)aniline oxide dihydrochloride|
|IC50:||20-30 μM |
|Tags:||HIF/HIF Prol |HIF/HIF Prol ||
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PX-478 is an inhibitor of HIF-1a with an IC50 of 20-30μM enhances radiosensitivity of prostate carcinoma cells.
IC50 value: 20-30 μM 
in vitro: PX-478 enhances the radiosensitivity of prostate carcinoma cells irradiated under normoxia. In addition to the inhibition of HIF-1a, treatment with PX-478 resulted in cell type-dependent alterations in cell cycle distribution and prolonged gH2AX expression in the irradiated cells. In PC3 cells, PX-478 significantly reduced the percentage of cells in G1 with an accumulation of cells in S/G2M. 
in vivo: PX-478 is an experimental HIF-1a inhibitor that has shown antitumor activity against several aggressive human tumor xenografts.  PX-478 shows antitumor activity against established (0.15-0.40 cm3) human tumor xenografts with cures of SHP-77 small cell lung cancer and log cell kills up to 3.0 for other tumors including HT-29 colon, PC-3 prostate, DU-145 prostate, MCF-7 breast, Caki-1 renal, and Panc-1 pancreatic cancers. Large (0.83 cm3) PC-3 prostate tumors showed 64% regression, which was greater than for smaller tumors. 
. Palayoor ST, et al. PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells. Int J Cancer. 2008 Nov 15;123(10):2430-2437.
. Welsh S, et al. Antitumor activity and pharmacodynamic properties of PX-478, an inhibitor of hypoxia-inducible factor-1alpha. Mol Cancer Ther. 2004 Mar;3(3):233-244.