SOS1-IN-21

SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 value of 15 nM. As a guanine nucleotide exchange factor (GEF), SOS1 activates KRAS by facilitating the conversion of GDP to GTP. SOS1-IN-21 demonstrates potent antiproliferative activity, with IC50 values of 16 nM for NCI-H358 cells and 17 nM for Mia Paca-2 cells. It exhibits significant antitumor activity in Mia Paca-2 xenograft models and is useful for researching KRAS-mutated tumors, such as pancreatic cancer.