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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Purity & Documentation Purity:
>98% (HPLC)
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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
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M.Wt
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455.493
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Formula
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C26H22FN5O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Malcolm P Huestis, et al. ACS Med Chem Lett. 2021 Apr 21;12(5):791-797.
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