Drug intelligence / Profile preview

ARS-2102

Development stage
Unknown
Modality
Small Molecules
01

Overview

ARS-2102 is a potent, covalent inhibitor of KRAS G12C, an oncogenic mutant form of the KRAS protein. It is designed for use in cancer research and functions by irreversibly binding to the cysteine residue at position 12 (G12C) of the KRAS protein, thereby inhibiting its activity. This mechanism targets cancers driven by the KRAS G12C mutation, which is commonly found in certain types of non-small cell lung cancer and other solid tumors. ARS-2102 represents a first-generation covalent inhibitor with an atropisomeric biaryl scaffold, developed through advanced synthetic chemistry techniques to achieve high selectivity and potency against mutant KRAS G12C[1][3][7].

02

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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