Darlifarnib (KO-2806) | FTase inhibitor

Chemical Structure : Darlifarnib

Darlifarnib (KO-2806, KO2806)

Catalog No.: PC-24121Not For Human Use, Lab Use Only.

Darlifarnib (KO-2806, KO2806) is a potent, specific farnesyltransferase (FTase) inhibitor with IC50 of 2.4 nM, while sparing activity of GGTase (IC50>1 uM).

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Biological Activity

Darlifarnib (KO-2806, KO2806) is a potent, specific farnesyltransferase (FTase) inhibitor with IC50 of 2.4 nM, while sparing activity of GGTase (IC50>1 uM).

KO-2806 enhances adagrasib's inhibition of mTORC1 signaling by blocking RHEB farnesylation.

KO-2806 deepens responses of NSCLC models to KRASG12C inhibition and inhibits mTORC1 in vivo.

KO-2806 blocks rebound of mTOR signaling and deepens antitumor responses to mutant-selective and pan-RAS inhibitors in colorectal cancer.

KO-2806 resensitizes refractory or relapsing NSCLC tumors to mutant-selective or pan-RAS inhibition.

Physicochemical Properties

M.Wt	468.52
Formula	C29H20N6O
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	(S)-3-amino-3-(1-methyl-1H-imidazol-5-yl)-6-oxa-2(4,6)-quinolina-1,4(1,3)-dibenzenacyclohexaphane-22,44-dicarbonitrile

References

1. Patent WO2024137751 A1.

2. Patent WO2024233539 A1.

Darlifarnib (KO-2806, KO2806)

Biological Activity

Physicochemical Properties

References

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