Rasarfin is a novel dual Ras and ARF6 inhibitor, which blocks agonist-mediated internalization of AT1R and other GPCRs. Rasarfin also effectively suppresses the growth of cancer cells by blocking EGFR-induced MAPK and Akt signaling as well as agonist-induced ERK1/2 signaling by GPCRs.
Physicochemical Properties
| Molecular Formula | C23H24CLN3O3 |
| Molecular Weight | 425.907964706421 |
| Exact Mass | 425.15 |
| Elemental Analysis | C, 64.86; H, 5.68; Cl, 8.32; N, 9.87; O, 11.27 |
| CAS # | 674359-73-0 |
| PubChem CID | 1396167 |
| Appearance | White to yellow solid powder |
| LogP | 4.6 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 4 |
| Heavy Atom Count | 30 |
| Complexity | 623 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | SRZCCUYFJZQLGE-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C23H24ClN3O3/c1-15(2)23(29)27-11-9-26(10-12-27)19-8-7-17(14-18(19)24)25-22(28)21-13-16-5-3-4-6-20(16)30-21/h3-8,13-15H,9-12H2,1-2H3,(H,25,28) |
| Chemical Name | N-[3-chloro-4-[4-(2-methylpropanoyl)piperazin-1-yl]phenyl]-1-benzofuran-2-carboxamide |
| Synonyms | Rasarfin |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | Rasarfin effectively inhibits coagulant-induced ERK1/2 signaling through GPCR, MAPK and Akt signaling through EGFR, and by inhibiting ischemia [1]. Rasarfin inhibits ARF6 and inhibits GPCR internalization [1]. Rasarfin causes MDA-MB- Rasarfin inhibits AP-2 recruitment to β-arrestin2 and receptor internalization, both processes requiring active ARF6 [1]. 231 cells decreased in a dose-dependent manner [1]. |
| References |
[1]. Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen. Nat Commun. 2021 Aug 3;12(1):4688. |
Solubility Data
| Solubility (In Vitro) | DMSO: ~50 mg/mL (~117.4 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3479 mL | 11.7396 mL | 23.4791 mL | |
| 5 mM | 0.4696 mL | 2.3479 mL | 4.6958 mL | |
| 10 mM | 0.2348 mL | 1.1740 mL | 2.3479 mL |