cFMS Receptor Inhibitor II (BUN60856; BUN-60856) is a novel, cell-permeable and potent CSF1R (Colony stimulating factor 1 receptor) kinase inhibitor with an IC50 of 80 nM. It is an anilinoquinoline that functions as an effective, active site-targeting inhibitor of the cFMS/MCSF receptor. When it comes to blocking the cFMS-dependent growth of M-NSF-60 cells (IC50 = 0.1 µM), this inhibitor is just as effective as cFMS Receptor Inhibitor III, but it is significantly more targeted against the cFMS-independent growth of NSO cells (IC50 >50 µM). The CSF1R gene, also referred to as c-FMS, encodes the cell-surface protein known as colony stimulating factor 1 receptor (CSF1R), also referred to as CD115 (Cluster of Differentiation 115) and macrophage colony-stimulating factor receptor (M-CSFR).
Physicochemical Properties
| Molecular Formula | C23H20N4O |
| Molecular Weight | 368.431104660034 |
| Exact Mass | 368.16 |
| Elemental Analysis | C, 74.98; H, 5.47; N, 15.21; O, 4.34 |
| CAS # | 959860-85-6 |
| Related CAS # | Solid powder |
| PubChem CID | 25163930 |
| Appearance | Light yellow to yellow solid powder |
| LogP | 4.4 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 4 |
| Heavy Atom Count | 28 |
| Complexity | 535 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | BIICXZWYHQOUEQ-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C23H20N4O/c1-14-3-5-18(11-15(14)2)27-22-19-6-4-17(16-7-9-25-10-8-16)12-21(19)26-13-20(22)23(24)28/h3-13H,1-2H3,(H2,24,28)(H,26,27) |
| Chemical Name | 4-(3,4-dimethylanilino)-7-pyridin-4-ylquinoline-3-carboxamide |
| Synonyms | cFMS Receptor Inhibitor II; cFMS Receptor Inhibitor-II; BUN60856; BUN-60856; BUN 60856 |
| 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
| Targets | CSF1R |
| References |
[1]. Compositions and methods for obtaining enriched mesenchymal stem cell cultures. US20160032248A1. |
Solubility Data
| Solubility (In Vitro) | DMSO: ~83.3 mg/mL (~226.2 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 2.7142 mL | 13.5711 mL | 27.1422 mL | |
| 5 mM | 0.5428 mL | 2.7142 mL | 5.4284 mL | |
| 10 mM | 0.2714 mL | 1.3571 mL | 2.7142 mL |