MRTX-1133 (MRTX1133; MRTX 1133) is a novel, potent, noncovalent, and selective KRAS G12D inhibitor with antitumor activity. It is efficacious in a KRASG12D mutant xenograft mouse tumor model. KRASG12D, the most common oncogenic KRAS mutation, is a
promising target for the treatment of solid tumors. However, when
compared to KRASG12C, selective inhibition of KRASG12D presents a significant challenge due to the requirement of inhibitors to bind KRASG12D with high enough affinity to obviate the need for covalent interactions with the mutant KRAS protein.
理化性质和储存条件
Molecular Formula: C33H31F3N6O2
Exact Mass: 600.2461
Molecular Weight: 600.6462
Synonym: MRTX-1133; MRTX1133; MRTX 1133;
Chemical Name: 2-Naphthalenol, 4-[4-(3,8-diazabicyclo[3.2.1]oct-3-yl)-8-fluoro-2-[[(2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoro-
Solubility in DMSO :>100 mg/mL