| E6537 |
Eras-4001 |
ERAS-4001 is a pan-KRAS inhibitor with potent antitumor activity. It inhibits proliferation of wild-type and mutant KRAS-driven cancer cells, including KRAS G12D, G12V, and G12C, and suppresses tumor growth in GP2D and Panc0403 xenograft mouse models. |
| E6638 |
VS-7375 (GFH375) |
GFH375(VS-7375) 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. |
| E6757 |
BBO-11818 |
BBO‑11818 is an orally active and non‑covalent inhibitor of pan‑KRAS that binds both the active (GTP‑bound, “ON”) and inactive (GDP‑bound, “OFF”) forms of multiple oncogenic KRAS mutants, including KRAS G12D and G12V. It potently suppresses MAPK signaling and viability in KRAS‑driven cell lines, induces tumor regressions in KRAS‑mutant xenograft models. |
| 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. |