| 产品描述: | LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer. |
| 体外研究: |
LUNA18 (2 μmol/L, 36 小时) 对 NCI-H2122, MiaPaCa-2, NCI-H441, LS 180, GSU 细胞株的增殖有较强的抑制作用,是一种选择性 RAS 抑制剂。 LUNA18 (0-100 nM, 4 小时) 以浓度依赖性的方式降低 NCI-H441 细胞系中 GTP-KRAS、pERK1/2 和 pAKT 的表达。 |
| 体内研究: |
LUNA18 (10 mg/kg, 口服, 一天一次, 持续 14 天) 在小鼠 NCI-H441 异种移植小鼠模型中导致剂量依赖性抗肿瘤活性,体重没有显著减轻。 |
| 保存条件: |
-20°C, 干燥, 避光, 氮气保存 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
0.696 ml |
3.478 ml |
6.956 ml |
| 5 mM |
0.139 ml |
0.696 ml |
1.391 ml |
| 10 mM |
0.07 ml |
0.348 ml |
0.696 ml |
| 50 mM |
0.014 ml |
0.07 ml |
0.139 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。 |