MRTX849 acid, a derivative of MRTX849, can be used in the synthesis ofPROTACLC-2 (HY-137516). LC-2 is a potent and first-in-classPROTACcapable of degrading endogenous KRAS G12C (DC⁵⁰s between 0.25 and 0.76 μM)^[1][2].

LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC₅₀s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via abona fidePROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h^[1].
LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines^[1].

662.15

C₃₄H₃₇ClFN₇O₄

2561529-96-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.