| E6660 |
FMC-376 |
FMC-376 is a selective and irreversible dual inhibitor of both the ON and OFF states of KRASG12C. It binds covalently to the mutant cysteine at position 12 in KRAS G12C and directly blocks both the ON and OFF conformations of the mutant KRAS protein, leading to a complete and durable blockade of downstream signaling. FMC‑376 exhibits robust anti‑tumor activity in vivo. |
| E1577 |
AZD4747 |
AZD4747 is a selective, blood‑brain barrier‑permeable inhibitor of mutant GTPase KRASG12C, with the potential to treat KRAS^G12C‑positive tumors, including central nervous system (CNS) metastases. |
| E2540 |
Salvianolic acid F |
Salvianolic acid F acts as a KRAS inhibitor, with activity against KRAS G12D. It suppresses NF-kB, MMP-9, and NO production. In vitro studies show it reduces cancer cell proliferation, invasion, and migration while promoting apoptosis through the EP300/PI3K/AKT pathway. In vivo experiments demonstrate its inhibition of KRAS-dependent lung cancer cell growth via PI3K/AKT signaling. This compound has potential applications in studying multiple cancer types, particularly KRAS G12D-associated NSCLC and ovarian cancer. |
| E6638 |
VS-7375 (GFH375) |
VS-7375 (GFH375) is an oral small-molecule inhibitor that selectively targets KRAS G12D in both its active (GTP-bound) and inactive (GDP-bound) forms. This dual-state inhibition results in stronger tumor suppression compared to single-state inhibitors. It exhibits potent anti-proliferative and anti-tumor effects in KRAS G12D-mutant models, including an intracranial GP2D tumor model. |
| E6643 |
SS-3091 |
SS‑3091 is a potent inhibitor of pan‑KRas that targets the interaction interfaces of KRas, destabilizing critical KRas–protein complexes and thereby blocking its downstream signaling pathways. SS‑3091 effectively inhibits KRas‑driven signaling in multiple cancer cell lines, including those harboring G12D, G12V, and G13D mutations, leading to reduced ERK and AKT phosphorylation. |