We are happy to continue our series of posts which are inspired by Drug Hunter’s “Molecules of the Month”!
Here are two molecules that were recently highlighted by Drug Hunter!
1. RP-6306 is a selective and orally active inhibitor of protein kinase, membrane-associated tyrosine/threonine 1 (PKMYT1). PKMYT1 belongs to the WEE family of serine/threonine kinases and phosphorylates threonine 14 of cyclin-dependent kinase 1 (CDK1) that leads to inhibiting of trigger mitosis. Currently, RP-6306 is in Phase 1 as the first-in-class clinical candidate for treating different solid tumors.
You can find the analogs to this molecule here!
2. MRTX0902 is an orally bioavailable, selective, and potent inhibitor of the SOS1:KRAS protein-protein interaction (PPI) that can penetrate the blood-brain barrier. KRAS as a small GTPase takes part in switching “on”/”off” positions in GTP/GDP-loaded states which is important for surviving and proliferation of cells. Son of Sevenless (SOS) protein plays the role of activator for KRAS function. Disrupting the SOS1:KRAS complex is a promising strategy across KRAS mutant-driven cancers. MRTX0902 oral administration in combination with another KRASG12C inhibitor shows a significant increase in antitumor activity compared to a single compound and total tumor regressions in mouse xenograft models.
You can find the analogs to this molecule here!
Use chem-space.com/search to find off-the-shelf and Make-on-Demand molecules of your interest!
