BAY-293

Mutations in the RAS genes have been recognized as major oncogenes with a high occurrence rate in human cancers. RAS proteins act as molecular switches that cycle between an active, GTP-bound state and an inactive, GDP-bound state. Activated by guanine nucleotide exchange factors (GEFs), RAS in its GTP bound state interacts with a number of effectors. The most-studied GEF for RAS is the protein Son of Sevenless (SOS) for which two human isoforms, SOS1 and SOS2, are known¹. 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 SOS1¹. BAY-293 (595 nM-3580 nM; 72h) shows efficient antiproliferative activity against wild-type KRAS cell lines (K-562, MOLM-13) and cell lines with KRAS^G12C mutation (NCI-H358, Calu-1). BAY-293 efficiently inhibited pERK (extracellular signal-regulated kinase) levels in K-562 cells after incubation for 60 min without affecting total protein levels of ERK¹.

溶解方案(细胞实验)

DMSO 中的溶解度 : 100 mg/mL (222.93 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.08 mg/mL (4.64 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.08 mg/mL (4.64 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"