/wp-content/uploads/2019/11/logo_white.png 0 0 webadmin /wp-content/uploads/2019/11/logo_white.png webadmin2020-10-28 16:18:042020-11-12 08:36:33The clinical candidate, ASTX029, is a novel, dual mechanism ERK1/2 Inhibitor and has potent activity in MAPK-activated cancer cell lines and in vivo tumor models
- The MAPK signaling pathway is commonly upregulated in human cancers due to oncogenic mutations of upstream
components such as BRAF or KRAS.
- MAPK pathway inhibition has been clinically validated by BRAF and MEK inhibitors.
- As the final node in the MAPK pathway, ERK is an attractive therapeutic target for the treatment of MAPK-activated cancers, including those resistant to upstream inhibition.
- Previously we described the fragment-based discovery of a chemical series targeting ERK. Here we disclose for the first time the structure of the clinical candidate, ASTX029.
- Heightman et al., (2018). J Med Chem 61; 4978