| 产品描述: | SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS. |
| 靶点: |
KRAS-SOS1,KRas G12C:140 nM (EC50); KRas G12D:109 nM (EC50); KRas G12V:154 nM (EC50); KRas G12S:155 nM (EC50); KRas Q61H:175 nM (EC50) |
| 体外研究: |
SAH-SOS1A TFA (0.625-40 μM; 24 hours) dose-responsively impairs the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations with IC50 values in the 5- to 15-μM range. Cancer cells expressing wild-type KRAS, such as HeLa and Colo320-HSR cells, are similarly affected. SAH-SOS1A TFA (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation. |
| 体内研究: |
SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85DV12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2. |
| 保存条件: |
-80°C, 干燥, 避光, 氮气保存 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
0.434 ml |
2.172 ml |
4.345 ml |
| 5 mM |
0.087 ml |
0.434 ml |
0.869 ml |
| 10 mM |
0.043 ml |
0.217 ml |
0.434 ml |
| 50 mM |
0.009 ml |
0.043 ml |
0.087 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。 |