kras g12d inhibitor 1

KRAS G12D inhibitor 1 (example 243) is an inhibitor of KRAS G12D, exhibiting an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation [1].

KRAS G12D inhibitor 15 is a potent and specific inhibitor targeting the KRAS G12D mutation, showing potential for research into various diseases and disorders, including cancer and its metastases [1].

KRAS G12D inhibitor 19 (Compound 7) is used in cancer research [1]. As a specific inhibitor of KRAS G12D, it targets and potentially suppresses this mutation, which is frequently associated with various cancers.

KRAS G12D inhibitor 14 is a potent compound that binds the KRAS G12D protein (Kd: 33 nM) and selectively inhibits the active form KRAS G12D-GTP, but not KRAS G13D.

KRAS G12D inhibitor 12 is an effective inhibitor of KRAS G12D. The Ras protein family is an important intracellular signaling molecule, which plays an important role in growth and development. KRAS G12D inhibitor 12 has the potential to perform KRAS G12D-mediated cancer studies.

KRAS G12D inhibitor 11 is a potent inhibitor of KRAS G12D, a key protein in the Ras family involved in crucial intracellular signaling for growth and development. This inhibitor has shown potential for investigating KRAS G12D-mediated cancers [KRAS G12D, Ras family, intracellular signaling, growth, development, cancer].

KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D with potential for the investigation of KRAS G12D-mediated cancers.

KRAS G12D Inhibitor 10 is a potent agent targeting the KRAS G12D mutation, a variant in the Ras protein family crucial for cellular growth and development. This compound shows promise for investigating cancers mediated by KRAS G12D.

KRAS G12D Inhibitor 16 is a potent compound targeting the KRAS G12D and its mutation, exhibiting inhibitory activity with IC50 values of 0.7 nM and 0.35 μM, respectively. It is utilized in researching various malignant tumors including pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), and non-small cell lung carcinomas (NSCLC).

Zoldonrasib (RMC-9805) is a mutant-selective covalent KRAS G12D inhibitor with oral activity and significant antitumor activity, inducing tumor cell apoptosis in preclinical models of various KRAS-mutant cancers.

Setidegrasib is a PROTAC-mediated KRAS degrader (DC50: 37 nM). Setidegrasib induces the formation of a ternary complex between KRAS G12D and the VHL E3 ubiquitin ligase, thereby facilitating the ubiquitination and proteasomal degradation of the oncogenic protein. Setidegrasib inhibits the levels of p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates antitumor activity in various mouse xenograft models of cancer. Setidegrasib can be used to study solid tumors with KRAS(G12D) mutations.

AMG410 is a non-covalent, dual-modality KRAS inhibitor effective against both GDP (OFF) and GTP (ON) binding, with Kd (GDP) of 1 nM and Kd (GTP) of 22 nM, capable of blocking KRAS independently of the cell cycle. AMG410 does not affect HRAS and NRAS2, and exhibits high potency against KRAS G12D, G12V, G12C, G13D, and other mutants, with an IC₅₀ of 1–4 nM. It induces tumour regression and reduces phosphorylated ERK levels in KRAS-mutant cancer models.

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.

MEK/RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK/RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.

KRAS G12D inhibitor 25 (Compound 148) acts as an inhibitor for KRAS G12C and HSP90α, displaying IC50 values of <0.1 μM and 0.1-1 μM respectively. Additionally, it suppresses the proliferation of MIA PaCa-2 and NCI-H358 cell lines, with EC50 values of <0.1 μM and 0.1-1 μM correspondingly. This compound also promotes the degradation of ERBB2, exhibiting a DC50 of 0.1-1 μM.

KRAS inhibitor-27 (Compound 15h) is a KRAS inhibitor that effectively targets KRAS G12D/G12V mutated cells (AsPC-1 and SW620) and wild-type KRAS cells (HT-29), with IC50 values of 378 nM, 0.6 nM, and 3230 nM, respectively. It reduces ERK phosphorylation, with IC50 values of 0.6 nM and 1 nM in AsPC-1 and SW620 cells, respectively, and decreases DUSP4 expression, thereby inhibiting the MAPK signaling pathway.

KRAS G12D inhibitor 28 (Compound 1) is an inhibitor of KRAS G12D and can be utilized in cancer research.

pan-KRAS-IN-8 (Compound 38) is an inhibitor of the human tumor mutated gene KRAS. It effectively suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.07 nM and 0.18 nM, respectively.

Pan-KRAS-IN-10 (Compound 58) acts as an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells, specifically AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.7 and 0.24 nM, respectively.

pan-KRAS-IN-7 (Compound 25) is an inhibitor of the human tumorigenic mutant gene KRAS. It effectively suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with an IC50 of 0.35 nM and 0.51 nM, respectively.

Pan-KRAS-IN-8 (Compound 52) is an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 values of 0.24 nM and 0.30 nM, respectively.

KRASG12D-IN-5 (Compound 241) is an orally active KRAS(G12D) inhibitor with an IC50 of 11 nM. It demonstrates potent anticancer activity without significant cytotoxicity to BxPC-3 cells (wild-type), KRAS-mutant AsPC-1 cells (G12D), and MIAPaCa-2 cells (G12C), with CC50 values of 10.37, 0.76, and 0.3 μM, respectively. KRASG12D-IN-5 is applicable in cancer studies, including lung, pancreatic, and colorectal cancers.

(R)-KRAS G12D inhibitor 28 hydrochloride dihydrate is the dihydrate hydrochloride salt form of (R)-KRAS G12D inhibitor 28. KRAS G12D inhibitor 28 (Compound 1) acts as an inhibitor of the KRAS G12D protein and is utilized in cancer research.

KRAS G12D-IN-33 (Compound 1) is an inhibitor of KRAS G12D and is applicable in cancer research.