PX-478 Inhibitor CAS No. 685898-44-6

Cat. No.	Name	Size	Price
KI1473	PX-478	10 mg	$440
	PX-478	25 mg	$830
	PX-478	50 mg	$1470

Chemical Characteristic

Product Name	PX-478
CAS No.	685898-44-6
Molecular Weight	394.1
Formula	C₁₃H₂₀Cl₄N₂O₃
Chemical Name	(S)-4-(2-amino-2-carboxyethyl)-N,N-bis(2-chloroethyl)aniline oxide dihydrochloride
Smiles	N(C1=CC=C(C2C1O2)C[C@@H](C(=O)O)N)(CCCl)CCCl Cl Cl
Chemical Structure

Biological activities

PX-478 is a hypoxia-inducible factor-1 (HIF-1)α inhibitor. PX-478 inhibits the hypoxia-induced increase in HIF-1α protein in PC-3, MCF-7, HT-29, Panc-1, BxPC-3 cell lines.PX-478 also decreases the low but measurable HIF-1α protein levels observed in PC-3 prostate and Panc-1 pancreatic cancer cells under normoxic conditions with IC50 of 2.5 and 3.2 µM, respectively. PX-478 also lowers HIF-1α levels in isogenic HCT116 p53^+/+ and HCT116 p53^-/- cells. PX-478 treatment results in decreased levels of HIF-1α mRNA, decreases translation of HIF-1α protein during both normoxia and hypoxia, and increases deubiquitination of HIF-1α.^[1]PX-478 reduces cell survival and enhances the radiosensitivity of prostate carcinoma cells irradiated under normoxic and hypoxic condition. ^[2] PX-478 given to mice suppresses HIF-1α levels in HT-29 human colon cancer xenografts. Administration of PX-478 to mice results in a significant decrease in tumor HIF-1α staining, with a maximum decrease at 5 hours to 29.3% of non-drug-treated tumor values. PX-478 inhibits tumor HIF-1α and the expression the downstream genes for VEGF and Glut-1.^[3] PX-478 inhibits adaptive postradiation tumor HIF-1α signaling in vivo and provides durable enhancement of radiation growth delay. ^[4]

Protocols

PX-478 is prepared in 0.9% NaCl. ^[3]

References

[1] Koh MY, et al. Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1alpha. Mol Cancer Ther. 2008, 7(1): 90-100. [2] Palayoor ST, et al. PX-478, an inhibitor of hypoxia-inducible factor-0alpha, enhances radiosensitivity of prostate carcinoma cells. Int J Cancer. 2008, 123(10): 2430-2437. [3] Welsh S, et al. Antitumor activity and pharmacodynamic properties of PX-478, an inhibitor of hypoxia-inducible factor-1alpha. Mol Cancer Ther. 2004, 3(3): 233-244. [4] Schwartz DL, et al. The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects. Mol Cancer Ther. 2009, 8(4): 947-958.

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