| Identification | Back 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 Properties | Back 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. | [InChIKey]
SRZCCUYFJZQLGE-UHFFFAOYSA-N | [SMILES]
O=C(C1=CC2=C(C=CC=C2)O1)NC3=CC=C(N4CCN(CC4)C(C(C)C)=O)C(Cl)=C3 |
| Hazard Information | Back 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 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|