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 µM, compared to 120 µM 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 µM and for topoIIbeta with an IC50 of 120 µM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 µM, G-361: 8.1 µM), breast (MCF7: 15.8 µM), endometrial (HeLa: 38.2 µM), lung (A549: 17.1 µM), and prostate (DU145: 11.5 µM) cancer cells. Following a single intraperitoneal injection of 10 mg/kg, ARN-21934 achieves a peak plasma concentration of 0.68 µg/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.
Molekulargewicht:
360.46
Reinheit:
>99.99%
CAS Nummer:
[2230854-93-8]
Formel:
C21H24N6
Target-Kategorie:
Topoisomerase
T36968
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