BAY-293

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAY-293 (BAY293, BAY 293) 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。

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.

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 AssayCell Line:K-562, MOLM-13, H358 and Calu-1 cell linesConcentration:595-3580 nMIncubation Time:72 hoursResult: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.

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BAY293 | BAY 293

MAPK/ERK Signaling

Ras

KRAS-SOS1interaction

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2244904-70-7

448.585

C25H28N4O2S

>98% (HPLC)

DMSO : ≥ 125 mg/mL 278.66 mM

C[C@@H](NC1=C2C=C(OC)C(OC)=CC2=NC(C)=N1)C3=CC(C4=CC=CC=C4CNC)=CS3

(R)-6,7-dimethoxy-2-methyl-N-(1-(4-(2-((methylamino)methyl)phenyl)thiophen-2-yl)ethyl)quinazolin-4-amine

(-20℃)

With Ice Pack

≥ 2 years