BAY-293 是化学探针,是一种有效的细胞活性 SOS1 抑制剂,可破坏 KRas-SOS1 相互作用,IC50为 21 nM。
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BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).
体外活性
BAY-293 is a SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM and displays no significant activity against KRAS WT-CRAF RBD, CDC42 and EGFR (>20 uM). It 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). BAY-293 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 the formation of the KRAS-SOS1 complex.
Cas No.
2244904-70-7
分子式
C25H28N4O2S
分子量
448.59
储存和溶解度
DMSO:110 mg/mL (245.22 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years