ChemicalBook--->CAS DataBase List--->674359-73-0

674359-73-0

674359-73-0 Structure

674359-73-0 Structure
IdentificationBack Directory
[Name]

2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]-
[CAS]

674359-73-0
[Synonyms]

Rasarfin
2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]-
[Molecular Formula]

C23H24ClN3O3
[MOL File]

674359-73-0.mol
[Molecular Weight]

425.91
Chemical PropertiesBack Directory
[Boiling point ]

552.7±50.0 °C(Predicted)
[density ]

1.309±0.06 g/cm3(Predicted)
[storage temp. ]

-20°C
[solubility ]

Soluble in DMSO (70 mg/ml)
[form ]

solid
[pka]

11.99±0.70(Predicted)
[color ]

Yellow
[Stability:]

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Hazard InformationBack Directory
[Description]

Rasarfin (674359-73-0) is a 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
[Uses]

Rasarfin is a dual Ras and ARF6 inhibitor[1].
[storage]

Store at -20°C
[References]

Giubilaro et al. (2021), Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen; Nat. Commun. 12 4688
Spectrum DetailBack Directory
[Spectrum Detail]

2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]-(674359-73-0)1HNMR
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