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Rasarfin

Overview
Catalog # bs-83128c-5-mg
Product Name Rasarfin
Specifications
Storage Buffer Orange solid
Storage Condition -20°C
Target
Product Information Dual inhibitor of Ras and ARF6 discovered by screening a library of over 115,000 small molecules employing an endosomal BRET-based assay with the prototypical GPCR angiotensin II type 1 receptor (AT1R) seeking to identify inhibitors of receptor trafficking. IC50=7 and 0.7 µM for ARF and Ras respectively with no inhibition of Rac/Cdc42 and Rho up to 100 µM. It blocks agonist-mediated internalization of AT1R and other GPCRs. It also potently inhibits agonist-induced ERK1/2 signaling by GPCRs and MAPK and AKT signaling by EGFR (IC50=4-5 µM) and prevents cancer cell proliferation. Rasarfin’s direct action on Ras was also verified using purified H-Ras in an in vitro GEF exchange assay.1
Description CAS Number: 674359-73-0

Chemical Name: N-(3-Chloro-4-(4-isobutyrylpiperazin-1-yl)phenyl)benzofuran-2-carboxamide

Molecular weight: 425.91

Formula: C23H24ClN3O3

Solubility: DMSO (70 mg/ml)

Physical Properties: Yellow solid

Purity: 98% by TLC NMR (Conforms)