kras inhibitor 9

KRAS inhibitor-9 (DUN09716) is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSC-LC cells with KRAS mutation but not normal lung cells

KRAS G12D inhibitor 9 is a potent agent targeting KRAS G12D, an important member of the RAS protein family involved in intracellular signaling crucial for growth and development. This inhibitor shows significant research potential for KRAS G12D-mediated cancer.

KRAS inhibitor FB9 can be used in studies about Ras.

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).

KRAS-IN-43 (Compound 9) is a broad-spectrum KRAS inhibitor with IC50 values of 0.15 μM for KRASG12V, 0.14 μM for KRASG12C, and 0.47 μM for wild-type KRAS. It disrupts the interaction between KRAS and cRAF and suppresses ERK phosphorylation. KRAS-IN-43 shows potential for research in KRAS mutation-associated cancers, including pancreatic, colorectal, and lung cancers.

SOS1-IN-20 (Compound 12f) is an orally active inhibitor of SOS1, exhibiting an IC50 of 5.11 nM against KRASG12C::SOS1. It prevents KRAS activation and its downstream signaling by disrupting the KRAS-SOS1 interaction. In PC-9 cells, it shows an IC50 of 253 nM for p-ERK, while its IC50 for the hERG channel is 16.71 μM. SOS1-IN-20 also inhibits tumor cell proliferation, displaying antitumor activity.

SOS1-IN-9 is a potent inhibitor of SOS1 that targets KRAS G12C-SOS1 with an IC50 of 116.5 nM.

KRAS inhibitor-17 (compound 3-9) is a potent inhibitor of KRAS G12C with an IC50 of 3.37 μM. It exhibits p-ERK inhibition with an IC50 of 9.25 μM in MIA PaCA-2 cells and greater than 33.3 μM in A549 cells. KRAS inhibitor-17 has potential applications in the study of pancreatic, colorectal, and lung cancers.

KRAS G12C inhibitor 61 (Example 3) demonstrates potent activity by inhibiting phospho-ERK 1/2 in MIA PaCa-2 cells, with an IC50 value of 9 nM, and is applicable in the research of pancreatic, colorectal, and lung cancers [1].