ARN-21934 is a Highly Selective for Human Topoisomerase II α over β. ARN-21934 showed IC50 = 2 μM for inhibition of DNA relaxation, as compared to an IC50 = 120 μM for the anticancer drug etoposide with excellent metabolic stability and solubility. This new compound also shows ~100-fold selectivity for topoIIα over topoβ, a broad antiproliferative activity toward cultured human cancer cells, a favorable in vivo pharmacokinetic profile, and the ability to penetrate the blood−brain barrier. Thus, ARN-21934 is a highly promising lead for the development of novel and potentially safer topoII-targeted anticancer drugs.
MedKoo Cat#: 463236
Name: ARN-21934
CAS#: 2230854-93-8
Chemical Formula: C21H24N6
Exact Mass: 360.2062
Molecular Weight: 360.47
Elemental Analysis: C, 69.97; H, 6.71; N, 23.31
The following data is based on the product molecular weight 360.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
