BAY-293

SKU: orb1225608

Description

BAY-293 (BAY293, BAY 293) is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM; displays no significant activity against KRAS WT-CRAF RBD, CDC42 and EGFR (>20 uM); blocks reloading of KRAS with GTP, does not stabilize KRASWT or KRASG12C; inhibits the activation of RAS in HeLa cells with IC50 of 410 nM, efficiently inhibits pERK levels in K562 cells after incubation for 60 min without affecting total protein levels of ERK (IC50=180 nM); shows antiproliferative activity against wild-type KRAS cell lines (K562, MOLM-13; IC50~1 uM) and cell lines with KRASG12C mutation (NCI-H358, Calu-; IC50~3 uM) by preventing formation of the KRAS-SOS1 complex, also shows synergic antiproliferative effect with covalent KRASG12C inhibitor ARS-853; BAY-293 is a valuable chemical probe for investigation of the activation of KRAS by SOS1.

Key Properties

• CAS Number: 2244904-70-7
• MW: 448.585
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₈N₄O₂S
• SMILES: C[C@@H](NC1=C2C=C(OC)C(OC)=CC2=NC(C)=N1)C3=CC(C4=CC=CC=C4CNC)=CS3
• Target: Ras
• Solubility: DMSO : ≥ 125 mg/mL 278.66 mM

Bioactivity

• In Vitro:
  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 KRASG12C 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BAY293 | BAY 293

Quick Database Links

Gene Symbol

Ras