KRAS inhibitor 11
Names
[ CAS No. ]:
900897-56-5
[ Name ]:
KRAS inhibitor 11
[Synonym ]:
2-[4-(2-Methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)-1-piperazinyl]ethanol
1-Piperazineethanol, 4-(2-methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)-
Biological Activity
[Description]:
KRAS inhibitor 11 is a first-in-class, high-affinity, noncovalent allosteric KRAS inhibitor, disrupts KRAS-Raf interaction with Kd of 1.2 uM; binds to activated KRAS with sub-micromolar affinity and disrupts effector binding, thereby inhibiting KRAS signaling and cancer cell growth; dose-dependently decreases both p-ERK and p-cRaf levels in BHK cells expressing KRASG12D and KRASG12V, suggesting inhibition of RAS signaling via the MAPK pathway.
[References]
References 1. McCarthy MJ, et al. ACS Omega. 2019 Feb 28;4(2):2921-2930. View Related Products by Target Ras
Chemical & Physical Properties
[ Density]:
1.3±0.1 g/cm3
[ Molecular Formula ]:
C25H27N5O
[ Molecular Weight ]:
413.515
[ Exact Mass ]:
413.221558
[ LogP ]:
2.90
[ Index of Refraction ]:
1.672