BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
IC50&Target
KRAS-SOS1
21 nM (IC50)
体外研究
BAY-293 inhibits the activation of RAS in HeLa cells, with IC50 values in the submicromolar range.
BAY-293 (595 nM-3580 nM; 72 hours) shows efficient antiproliferative activity against wild-type KRAS cell lines (K-562, MOLM-13) and cell lines with KRAS mutation (NCI-H358, Calu-1).
BAY-293 efficiently inhibits pERK levels in K-562 cells after incubation for 60 min without affecting total protein levels of ERK.
Cell Proliferation Assay
Cell Line:
K-562, MOLM-13, H358 and Calu-1 cell lines
Concentration:
595-3580 nM
Incubation Time:
72 hours
Result:
IC50s of 1,090±170 nM, 995±400 nM, 3,480±100 nM and 3,190±50 nM for K-562, MOLM-13, H358 and Calu-1 cells, respectively.
分子式
C25H28N4O2S
分子量
448.58
CAS号
2244904-70-7
运输条件
Room temperature in continental US; may vary elsewhere.