GW284543 (also known as GW-284543; UNC10225170; UNC-10225170) is a novel, potent and selective MEK5 inhibitor that may be helpful in the treatment of cancer.
Physicochemical Properties
| Molecular Formula | C23H20N2O3 |
| Molecular Weight | 372.416505813599 |
| Exact Mass | 372.15 |
| Elemental Analysis | C, 74.18; H, 5.41; N, 7.52; O, 12.89 |
| CAS # | 790186-68-4 |
| Related CAS # | GW284543 hydrochloride;179246-08-3 |
| PubChem CID | 44531022 |
| Appearance | Off-white to gray solid powder |
| LogP | 5.2 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 6 |
| Heavy Atom Count | 28 |
| Complexity | 471 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | LEEMRFWMAIVHQY-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C23H20N2O3/c1-26-22-14-19-20(11-12-24-21(19)15-23(22)27-2)25-16-7-6-10-18(13-16)28-17-8-4-3-5-9-17/h3-15H,1-2H3,(H,24,25) |
| Chemical Name | 6,7-dimethoxy-N-(3-phenoxyphenyl)quinolin-4-amine |
| Synonyms | GW-284543; UNC-10225170; GW 284543; UNC 10225170; GW284543; UNC10225170 |
| 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 | MEK5 (IC50 = 1.5 nM); ERK5 (IC50 = 59 nM) |
| ln Vitro | In a dose-regulated manner, GW284543 treatment (10 and 20 μM; 6 hours) inhibits MEK5 and decreases pERK5 [1]. |
| Cell Assay |
Western Blot Analysis[1] Cell Types: MIA PaCa-2 cells Tested Concentrations: 10 and 20 μM Incubation Duration: 6 hour Experimental Results: ERK5 phosphorylation diminished and endogenous MYC protein diminished. |
| References |
[1]. KRAS Suppression-Induced Degradation of MYC Is Antagonized by a MEK5-ERK5 Compensatory Mechanism. Cancer Cell. 2018 Nov 12;34(5):807-822.e7. |
Solubility Data
| Solubility (In Vitro) | DMSO: 9~125 mg/mL (335.6~24.2 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.59 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. Solubility in Formulation 3: ≥ 2.08 mg/mL (5.59 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6851 mL | 13.4257 mL | 26.8514 mL | |
| 5 mM | 0.5370 mL | 2.6851 mL | 5.3703 mL | |
| 10 mM | 0.2685 mL | 1.3426 mL | 2.6851 mL |