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ARN-21934

Chemical Structure : ARN-21934

CAS No.: 2230854-93-8

ARN-21934 (ARN 21934)

Catalog No.: PC-38577Not For Human Use, Lab Use Only.

ARN-21934 is a potent, highly selective human topoisomerase II α (Topo IIα) with IC50 of 2 μM for inhibition of DNA relaxation, 100-fold selectivity for topo IIα over Topo β.

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Biological Activity

ARN-21934 is a potent, highly selective human topoisomerase II α (Topo IIα) with IC50 of 2 μM for inhibition of DNA relaxation, 100-fold selectivity for topo IIα over Topo β.
ARN-21934 is more potent than the anticancer drug etoposide (IC50=120 uM).
ARN-21934 displays a broad antiproliferative activity toward cultured human cancer cells (DU145, IC50=11.5 uM).
ARN-21934 also exhibits a favorable in vivo pharmacokinetic profile, and the ability to penetrate the blood-brain barrier.

Physicochemical Properties

M.Wt 360.46
Formula C21H24N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N4-[4-(Dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-4,6-quinazolinediamine

References

1. Jose Antonio Ortega, et al. J Med Chem. 2020 Nov 12;63(21):12873-12886.

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