INCB159020 | KRAS G12D inhibitor | Probechem Biochemicals

Chemical Structure : INCB159020

INCB159020 (INCB 159020)

Catalog No.: PC-23776Not For Human Use, Lab Use Only.

INCB159020 is a potent, selective KRAS G12D inhibitor with SPR binding Kd of 22 nM, IC50 of 33 nM in HTRF pERK cell assays.

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Biological Activity

INCB159020 is a potent, selective KRAS G12D inhibitor with SPR binding Kd of 22 nM, IC50 of 33 nM in HTRF pERK cell assays.
INCB159020 shows significant selectivity over inhibition of wild-type KRAS, in binding (50× vs binding to KRAS WT), a pERK setting (80 fold selectivity vs a wild-type H838 line) and in a viability setting (28 fold vs a H838 wild-type line).
INCB159020 (30, 100 and 300 mg/kg, oral) dose dependently inhibits pERK levels in HPAC mouse model.

Physicochemical Properties

M.Wt	664.18
Formula	C37H35ClFN7O2
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-(1-((1R,4R,5S)-2-Azabicyclo[2.1.1]hexan-5-yl)-7-(3-chloro-2-methylphenyl)-6-fluoro-4-(5-methylpyrazin-2-yl)-2-((R)-1-(3-oxomorpholino)ethyl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile

References

1. Ye Q, et al. J Med Chem. 2025 Jan 8. doi: 10.1021/acs.jmedchem.4c02662.

INCB159020 (INCB 159020)

Biological Activity

Physicochemical Properties

References

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