Avutometinib

Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively) .

Product Specifications

CAS Number

[946128-88-7]

Product Name Alternative

Ro 5126766; CH5126766

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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.html

Concentration

10mM

Purity

99.43

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S(NC)(NC1=NC=CC(CC2=C(C)C3=CC=C(OC4=NC=CC=N4)C=C3OC2=O)=C1F)=O

Molecular Formula

C21H18FN5O5S

Molecular Weight

471.46

Precautions

H302, H315, H319, H335

References & Citations

[1]Martinez-Garcia M, et al. First-in-human, phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of RO5126766, a first-in-class dual MEK/RAF inhibitor in patients with solid tumors. Clin Cancer Res. 2012 Sep 1;18 (17) :4806-19.|[2]Iizuka-Ohashi M, et al. Blockage of the mevalonate pathway overcomes the apoptotic resistance to MEK inhibitors with suppressing the activation of Akt in cancer cells. Oncotarget. 2018 Apr 13;9 (28) :19597-19612.|[3]Ishii N, et al. Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity. Cancer Res. 2013 Jul 1;73 (13) :4050-4060.