| 产品描述: | BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM). |
| 靶点: |
Ras; Raf;AChR |
| 体外研究: |
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. |
| 参考文献: |
1. Hillig RC, et al. Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1interaction. Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2551-2560. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.21 ml |
11.05 ml |
22.099 ml |
| 5 mM |
0.442 ml |
2.21 ml |
4.42 ml |
| 10 mM |
0.221 ml |
1.105 ml |
2.21 ml |
| 50 mM |
0.044 ml |
0.221 ml |
0.442 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |