For research use only. Not for therapeutic Use.
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[1].
BAY-293 inhibits the activation of RAS in HeLa cells, with IC50 values in the submicromolar range[1].
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 KRASG12C mutation (NCI-H358, Calu-1)[1].
BAY-293 efficiently inhibits pERK levels in K-562 cells after incubation for 60 min without affecting total protein levels of ERK[1].
| Catalog Number | I019466 |
| CAS Number | 2244904-70-7 |
| Synonyms | 6,7-dimethoxy-2-methyl-N-[(1R)-1-[4-[2-(methylaminomethyl)phenyl]thiophen-2-yl]ethyl]quinazolin-4-amine |
| Molecular Formula | C25H28N4O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C25H28N4O2S/c1-15(24-10-18(14-32-24)19-9-7-6-8-17(19)13-26-3)27-25-20-11-22(30-4)23(31-5)12-21(20)28-16(2)29-25/h6-12,14-15,26H,13H2,1-5H3,(H,27,28,29)/t15-/m1/s1 |
| InChIKey | WEGLOYDTDILXDA-OAHLLOKOSA-N |
| SMILES | CC1=NC2=CC(=C(C=C2C(=N1)NC(C)C3=CC(=CS3)C4=CC=CC=C4CNC)OC)OC |
| Reference | [1]. Hillig RC, et al. Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1interaction. Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2551-2560. |
