产品说明书
BAY-293
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同义名 : | - |
| CAS号 : | 2244904-70-7 | |
| 货号 : | A1167268 | |
| 分子式 : | C25H28N4O2S | |
| 纯度 : | 99%+ | |
| 分子量 : | 448.58 | |
| MDL号 : | MFCD31813755 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 120 mg/mL(267.51 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | 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 known[1]. 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 SOS1[1]. 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 KRASG12C 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 ERK[1]. | ||
| 作用机制 | The side-chain amino group of BAY-293 forms two new hydrogen bonds, to Asp887 and Tyr884, and is in a favorable position for a cation–π interaction with the side chain of Tyr884. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.23mL 0.45mL 0.22mL |
11.15mL 2.23mL 1.11mL |
22.29mL 4.46mL 2.23mL |
| 参考文献 |
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