2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]-
- Product Name
- 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
- Formula Weight
- 425.91
- MOL File
- 674359-73-0.mol
2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- Property
- 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)
- pka
- 11.99±0.70(Predicted)
- form
- solid
- 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,Usage,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
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