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

CAS No.
674359-73-0
Chemical Name:
2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]-
Synonyms
Rasarfin;breast,cancer,Inhibitor,TNBC,Ras,negative,GPCR,inhibit,Rasarfin,internalization,triple;2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]-
CBNumber:
CB29777365
Molecular Formula:
C23H24ClN3O3
Molecular Weight:
425.91
MDL Number:
MOL File:
674359-73-0.mol
Last updated:2023-09-04 16:42:00

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

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.

2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- Chemical Properties,Uses,Production

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

References

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

2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- Preparation Products And Raw materials

Raw materials

Preparation Products

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

Global( 14)Suppliers
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ATK CHEMICAL COMPANY LIMITED
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2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- Spectrum

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

Rasarfin 2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- breast,cancer,Inhibitor,TNBC,Ras,negative,GPCR,inhibit,Rasarfin,internalization,triple 674359-73-0