Chemical Structure : INCB159020
CAS No.:
2923669-20-7
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.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
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.
Contact Us
sales@probechem.com
