Avutometinib (potassium)

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].

Product Specifications

CAS Number

[946128-90-1]

Product Name Alternative

Ro 5126766 (potassium) ; CH5126766 (potassium)

UNSPSC

12352005

Target

MEK; Raf

Type

Reference compound

Related Pathways

MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/avutometinib-potassium.html

Smiles

O=S(NC)(NC1=NC=CC(CC2=C(C)C3=CC=C(OC4=NC=CC=N4)C=C3OC2=O)=C1F)=O.[K]

Molecular Formula

C21H18FKN5O5S

Molecular Weight

510.56

References & Citations

[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.|[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.