Description
AS-703026 is an inhibitor of MEK1/2 that exhibits anticancer chemotherapeutic activity. In vitro, AS-703026 inhibits proliferation of melanoma cells. In both in vitro and in vivo models of colorectal cancer containing WT Ras or mutant KRAS, AS-703026 inhibits growth of cells and also of tumors. Additionally, AS-703026 inhibits growth and survival of multiple myeloma cells by inducing activation of caspase 3, cleavage of poly(ADP)-ribose polymerase (PARP), and apoptosis; this compound suppresses tumor growth and decreases microvessel numbers in animal models as well.
References
Park SJ, Hong SW, Moon JH, et al. The MEK1/2 inhibitor AS703026 circumvents resistance to the BRAF inhibitor PLX4032 in human malignant melanoma cells. Am J Med Sci. 2013 Dec;346(6):494-8. PMID: 24051957.
Yoon J, Koo KH, Choi KY. MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Cancer Res. 2011 Jan 15;71(2):445-53. PMID: 21118963.
Kim K, Kong SY, Fulciniti M, et al. Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Br J Haematol. 2010 May;149(4):537-49. PMID: 20331454.
