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Product Name:Rasarfin
CAS:674359-73-0
Purity:98% Package:5MG;10MG;50MG;100MG,1G,5G,100G
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| | 2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- Basic information |
| Product Name: | 2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- | | Synonyms: | 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 | | CAS: | 674359-73-0 | | MF: | C23H24ClN3O3 | | MW: | 425.91 | | EINECS: | | | Product Categories: | | | Mol File: | 674359-73-0.mol | ![2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- Structure](CAS/20210305/GIF/674359-73-0.gif) |
| | 2-Benzofurancarboxamide, N-[3-chloro-4-[4-(2-methyl-1-oxopropyl)-1-piperazinyl]phenyl]- Chemical 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]- Usage And Synthesis |
| 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 |
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