ARN-21934 [2230854-93-8]

TargetMol Chemicals

ARN-21934 [2230854-93-8]

4

2230854-93-8

Chemical

Research Use Only

ARN-21934

C21H24N6

360.46

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II alpha over beta. It inhibits DNA relaxation with an IC50 of 2 microM, compared to 120 microM for Etoposide. ARN-21934 exhibits favorable in vivo pharmacokinetic properties and shows promise in anticancer research, displaying affinity for topoIIalpha with an IC50 of 2 microM and for topoIIbeta with an IC50 of 120 microM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 microM, G-361: 8.1 microM), breast (MCF7: 15.8 microM), endometrial (HeLa: 38.2 microM), lung (A549: 17.1 microM), and prostate (DU145: 11.5 microM) cancer cells. Following a single intraperitoneal injection of 10 mg/kg, ARN-21934 achieves a peak plasma concentration of 0.68 microg/mL in 15 minutes, with a half-life of 149 minutes, and remains detectable in plasma and the brain for up to 360 minutes. [1] Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II alpha over beta. J Med Chem. 2020 Nov 12;63(21):12873-12886.

3 years

CN(C)c1ccc(Nc2nc(nc3CCC(N)Cc23)-c2ccncc2)cc1

-20°C

12352200