AMG410 diTFA is a selective pan-KRAS inhibitor targeting various KRAS mutations, including G12D, G12V, and G13D, with IC50 values ranging from 1 to 4 nM. It exhibits over 100-fold selectivity against HRAS and NRAS and acts as a dual inhibitor of GTP-bound and GDP-bound states (Kd(GDP) of 1 nM; Kd(GTP) of 22 nM). AMG410 diTFA effectively disrupts KRAS signaling irrespective of cycling state and inhibits proliferation in wild-type KRAS-amplified tumor cells. This compound is valuable for research on colorectal, pancreatic, and lung cancers.
AMG410 diTFA is a selective pan-KRAS inhibitor targeting various KRAS mutations, including G12D, G12V, and G13D, with IC50 values ranging from 1 to 4 nM. It exhibits over 100-fold selectivity against HRAS and NRAS and acts as a dual inhibitor of GTP-bound and GDP-bound states (Kd(GDP) of 1 nM; Kd(GTP) of 22 nM). AMG410 diTFA effectively disrupts KRAS signaling irrespective of cycling state and inhibits proliferation in wild-type KRAS-amplified tumor cells. This compound is valuable for research on colorectal, pancreatic, and lung cancers.
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