Deltarasin (cas# 1440898-82-7) is a useful research chemical.Deltarasin was used as a reagent in studying small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling.
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].
[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.
