BAY-293
BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM [1].
Members of the RAS family of GTPases (which comprises KRAS, NRAS, and HRAS) are major oncogenes, mutants of RAS occur in many human cancers. SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
BAY-293 efficiently disrupted the interaction between KRAS and its exchange factor SOS1. In cells with wild-type KRAS (K-562, MOLM-13), BAY-293 showed complete inhibition of the RAS-RAF-MEK-ERK pathway. In mutant KRAS cell line (NCI-H358, Calu-1), BAY-293 exhibited synergistic anti-proliferative effects with KRASG12C inhibitor ARS-853.
[1] Hillig RC, Sautier B, Schroeder J, et al. Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction. Proc Natl Acad Sci U S A. 2019;116(7):2551–2560.
| Storage | Store at -20°C |
| M.Wt | 448.58 |
| Cas No. | 2244904-70-7 |
| Formula | C25H28N4O2S |
| Solubility | insoluble in H2O; ≥24 mg/mL in EtOH; ≥57.3 mg/mL in DMSO |
| Chemical Name | (R)-6,7-dimethoxy-2-methyl-N-(1-(4-(2-((methylamino)methyl)phenyl)thiophen-2-yl)ethyl)quinazolin-4-amine |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(C=C(C2=C1)N=C(N=C2N[C@@H](C3=CC(C4=C(C=CC=C4)CNC)=CS3)C)C)OC |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
