ARN-21934 |
| Catalog No.GC62425 |
L'ARN-21934 est un puissant inhibiteur de pénétration de la barrière hémato-encéphalique (BHE) hautement sélectif pour la topoisomérase II humaine α sur β. L'ARN-21934 inhibe la relaxation de l'ADN avec une IC50 de 2 μM par rapport À l'agent anticancéreux Etoposide (IC50 = 120 μM). L'ARN-21934 présente un profil pharmacocinétique in vivo favorable et est un composé phare prometteur pour la recherche anticancéreuse.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2230854-93-8
Sample solution is provided at 25 µL, 10mM.
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ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research[1].
ARN-21934 display a different affinity for topoIIα and topoIIβ. ARN-21934 is more potent against the α isoform, the IC50 value for the inhibition of DNA relaxation by topoIIα is 2 μM, the value for inhibition of DNA relaxation by topoIIβ is 120 μM[1].ARN-21934 exhibits a small panel of human cancer cell lines. It against melanoma (A375 and G-361), breast (MCF7), endometrial (HeLa), lung (A549), and androgen-independent prostate (DU145) cancer cells with IC50 values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively[1].
ARN-21934 (intraperitoneal injection; 10 mg/kg; single dose) reaches a maximal plasma concentration of 0.68 μg/mL after 15 min. The half-life is 149 min in circulation, still being present in plasma 360 min after injection. The compound also exhibits good clearance values (0.116 L/(min kg)). Besides, ARN-21934 is able to reach the brain, with a maximum concentration of compound at 60 min, and is still present in the brain 360 min after injection[1]
[1]. Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.
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