MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor featuring an alkyne-based structure. It binds with high affinity to the switch II pocket of KRAS G12D, with an estimated KD of 0.2 pM, engaging three key substituents that enhance protein interactions. MRTX1133 inhibits SOS1-mediated nucleotide exchange and disrupts formation of the KRAS G12D/GTP/RAF1 complex, thereby blocking downstream mutant KRAS signaling. It selectively targets KRAS G12D mutant cells without affecting KRAS wild-type cells, exhibiting single-digit nanomolar potency in cellular assays and strong antitumor efficacy in KRAS G12D-driven in vivo models.
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor featuring an alkyne-based structure. It binds with high affinity to the switch II pocket of KRAS G12D, with an estimated KD of 0.2 pM, engaging three key substituents that enhance protein interactions. MRTX1133 inhibits SOS1-mediated nucleotide exchange and disrupts formation of the KRAS G12D/GTP/RAF1 complex, thereby blocking downstream mutant KRAS signaling. It selectively targets KRAS G12D mutant cells without affecting KRAS wild-type cells, exhibiting single-digit nanomolar potency in cellular assays and strong antitumor efficacy in KRAS G12D-driven in vivo models.
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 1 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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