Bioactivity:

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II _ over _. ARN-21934 inhibits DNA relaxation with an IC50 of 2 _M as compared to the anticancer agent Etoposide (IC50=120 _M). 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 topoII_ and topoII_. ARN-21934 is more potent against the _ isoform, the IC50 value for the inhibition of DNA relaxation by topoII_ is 2 _M, the value for inhibition of DNA relaxation by topoII_ is 120 _M[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 _M, 8.1 _M, 15.8 _M, 38.2 _M, 17.1 _M, and 11.5 _M, respectively[1]. ARN-21934 (intraperitoneal injection; 10 mg/kg; single dose) reaches a maximal plasma concentration of 0.68 _g/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 _ over _. J Med Chem. 2020 Nov 12;63(21):12873-12886.

CAS nr:

2230854-93-8

Purity:

98%

Molecular Weight:

360,46

SMILES:

N/A

Formula:

C21H24N6

Pathway:

DNA Damage/DNA Repair

Target:

Topoisomerase