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946128-90-1

946128-90-1 Structure

946128-90-1 Structure
IdentificationBack Directory
[Name]

Avutometinib potassium
[CAS]

946128-90-1
[Synonyms]

Avutometinib potassium
Sulfamide, N-[3-fluoro-4-[[4-methyl-2-oxo-7-(2-pyrimidinyloxy)-2H-1-benzopyran-3-yl]methyl]-2-pyridinyl]-N′-methyl-, potassium salt (1:1)
[Molecular Formula]

C21H18FN5O5S.K
[MOL File]

946128-90-1.mol
[Molecular Weight]

510.56
Hazard InformationBack Directory
[Uses]

Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC)[1][2].
[References]

[1] McNamara B, et al. Preclinical efficacy of RAF/MEK clamp avutometinib in combination with FAK inhibition in low grade serous ovarian cancer. Gynecol Oncol. 2024 Apr;183:133-140. DOI:10.1016/j.ygyno.2024.01.028
[2] Coma S, et al. Abstract A091: The RAF/MEK clamp avutometinib as the backbone of therapy for pancreatic cancer: Novel combinations with standard of care chemotherapy, FAK inhibitors, KRAS G12D inhibitors and/or autophagy inhibitors[J]. Cancer Research, 2024, 84(2_Supplement): A091-A091.
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