K-Ras (G12C) inhibitor 6 is a novel, potent, allosteric, irreversible,/covalent cysteine-reactive small molecule KRAS G12C inhibitor with anticancer activity.
BAY-293 (BAY293) is a novel, potent, cell-active small-molecule SOS1 inhibitor with anticancer activity.
CCG-203971 is a novel, 2nd generation small-molecule inhibitor of the Rho/MRTF/SRF [RhoA/myocardin-related transcription factor A (MRTF-A)] pathway with an IC50 value of 0.64 μM for SRE.
ZT-12-037-01 is a novel, potent, ATP-competitive and specific STK19-targeted inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively.
K-Ras-IN-1 (formerly known as K-Ras-Inhibitor-1) is a novel small molecule K-Ras inhibitor that binds to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure, in other words, K-Ras-IN-1 binds directly to K-Ras between switch I and switch II and inhibit Sos-catalyzed K-Ras activation.
Sotorasib (AMG-510; AMG510; Lumakras; Lumykras) is a novel, first-in-class and covalent/irreversible inhibitor of KRAS G12C that has been approved by FDA on 5/28/2021 to treat non-small-cell lung cancer (NSCLC).
ARS-1630 is a less active isomer of ARS-1620, which is a novel and potent inhibitor of mutant K-ras G12C found in patent WO 2015054572 A1.
kobe2602 is a novel, potent and selective small-molecule inhibitor of Ras–Raf interaction identified by SBDD (structure based drug design); it exhibits competitively inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 149 ± 55 μM.
ARS-1323 is the racemic mixture of ARS-1620, and is a novel and potent inhibitor of mutant K-ras G12C.
ARS-1620 is a novel, potent, orally bioavailable and covalent inhibitor of KRASG12C with antitumor activity.