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GNE-9815

Chemical Structure : GNE-9815

CAS No.: 2729996-45-4

GNE-9815 (GNE9815)

Catalog No.: PC-72469Not For Human Use, Lab Use Only.

GNE-9815 (GNE9815) is a potent, selective, oral Type II pan-RAF inhibitor with Ki of 0.062 and 0.19 nM for CRAF and BRAF, respectively.

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Biological Activity

GNE-9815 (GNE9815) is a potent, selective, oral Type II pan-RAF inhibitor with Ki of 0.062 and 0.19 nM for CRAF and BRAF, respectively.
GNE-9815 displays clean kinase selectivity against a panel of 223 kinases (no inhibition > 70% at a concentration of 0.1 μM) besides RAF kinases).
GNE-9815 demonstrates synergistic activity in KRAS mutant A549 and HCT116 cancer cells in combination with the MEK inhibitor cobimetinib.
GNE-9815 in combination with the MEK inhibitor cobimetinib demonstrated synergistic MAPK pathway modulation in an HCT116 xenograft mouse model.

 

Physicochemical Properties

M.Wt 455.493
Formula C26H22FN5O2
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

3-(2-cyanopropan-2-yl)-N-(2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl)benzamide

References

1. Malcolm P Huestis, et al. ACS Med Chem Lett. 2021 Apr 21;12(5):791-797.

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