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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
B-Raf; C-Raf; MEK
Available Sizes
Frequently Asked Questions
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