| 产品描述: | Deltarasin hydrochloride is a selective inhibitor of KRAS-PDEδ interaction with IC50 value of 41±12 nM. KRAS, also known as V-Ki-ras2 Kirsten rat sarcoma viral oncogene homolog, is a protein and works as a molecular on/off switch whose mutant is an essential step in the development of many cancers. PDEδ (prenyl binding protein) controls the spatial organization of K-Ras, which enhances Ras diffusion in the cytosol. Inhibition of the Ras-PDEδ interaction by small molecules impairs Ras localization and signaling has becoming a promising strategy to treat cancers in clinic. Deltarasin hydrochloride is a potent KRAS-PDEδ interaction inhibitor. When tested with human pancreatic ductal adenocarcinoma cells Deltarasin hydrochloride showed inhibition on KRAS-PDEδ interaction to inhibit oncogenic RAS signaling and suppressed cell proliferation by binding to PDEδ with Kd value of 41 nM. In nude mice model with Panc-Tu-I xenograft, administration of Deltarasin hydrochloride (10, 15 mg/kg) impaired cells growth and decreased tumor volume after 9 days in a dose-dependent manner. |
| 参考文献: |
1. Zimmermann, G., et al., Small molecule inhibition of the KRAS-PDEdelta interaction impairs oncogenic KRAS signalling. Nature, 2013. 497(7451): p. 638-42. 2. The KRAS-PDEdelta interaction is a therapeutic target. Cancer Discov, 2013. 3(7): p. Of20. |
| 溶解性: |
soluble in DMSO、DMF、Ethanol、PBS |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.562 ml |
7.81 ml |
15.62 ml |
| 5 mM |
0.312 ml |
1.562 ml |
3.124 ml |
| 10 mM |
0.156 ml |
0.781 ml |
1.562 ml |
| 50 mM |
0.031 ml |
0.156 ml |
0.312 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。 |