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RO-5126766

Chemical Structure : RO-5126766

CAS No.: 946128-88-7

RO-5126766 (VS-6766, CH-5126766, Avutometinib)

Catalog No.: PC-45504Not For Human Use, Lab Use Only.

RO-5126766 (CH-5126766, Avutometinib, VS-6766) is a potent, first-in-class dual Raf/MEK inhibitor with IC50 of 56 nM/160 nM for C-Raf/MEK1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

RO-5126766 (CH-5126766, Avutometinib, VS-6766) is a potent, first-in-class dual Raf/MEK inhibitor with IC50 of 56 nM/160 nM for C-Raf/MEK1.
RO-5126766 (CH-5126766, Avutometinib) shows weak or no inhibition on CYP2C9, CYP3A4 and hERG.
RO-5126766 (CH-5126766, Avutometinib) inhibits ERK signaling output more effectively than a standard MEK inhibitor PD0325901 that induces MEK phosphorylation and has potent antitumor activity as well.

Physicochemical Properties

M.Wt 471.4615
Formula C21H18FN5O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Sulfamide, N-[3-fluoro-4-[[4-methyl-2-oxo-7-(2-pyrimidinyloxy)-2H-1-benzopyran-3-yl]methyl]-2-pyridinyl]-N'-methyl-

References

1. Aoki T, et al. ACS Med Chem Lett. 2014 Jan 22;5(4):309-14.

2. Ishii N, et al. Cancer Res. 2013 Jul 1;73(13):4050-60.

3. Wada M, et al. PLoS One. 2014 Nov 25;9(11):e113217.

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