IACS-13909

2160546-07-4

377.27

DMSO : 16.67 mg/mL (ultrasonic); H₂O : < 0.1 mg/mL

Metabolic Enzyme/Protease

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.
IC50 & Target: IC50: 15.7 nM (SHP2)

Kd: 32 nM (SHP2)
In Vitro: IACS-13909 (10 nM-10 uM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells.

IACS-13909 (1-5 uM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells.

IACS-13909 potently suppresses the proliferation of both the parental cells and NCI-H1975 CS cells in a dose-dependent manner, with similar potency (GI50 ca.1 uM). IACS-13909 (0.041-3.3 uM) suppresses pERK in NCI-H1975 CS cells in a dose-dependent manner.
In Vivo: IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing.