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Deltarasin hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Deltarasin hydrochloride图片
CAS NO:1440898-82-7
规格:98%
分子量:640.22
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
inhibitor of KRAS-PDEδ interaction, potent and selective
CAS:1440898-82-7
分子式:C40H38ClN5O
分子量:640.22
纯度:98%
存储:Store at -20°C

Background:

Deltarasin hydrochloride is a selective inhibitor of KRAS-PDEδ interaction with IC50 value of 41±12 nM [1].


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 [1, 2].


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 [1].


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 [1].


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.