Description
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.
Product information
CAS Number: 2230854-93-8
Molecular Weight: 360.46
Formula: C21H24N6
Chemical Name: N4-[4-(dimethylamino)phenyl]-2-(pyridin-4-yl)-5,6,7,8-tetrahydroquinazoline-4,6-diamine
Smiles: CN(C)C1C=CC(=CC=1)NC1=NC(=NC2CCC(N)CC=21)C1C=CN=CC=1
InChiKey: CKXSRLUXTFDZCF-UHFFFAOYSA-N
InChi: InChI=1S/C21H24N6/c1-27(2)17-6-4-16(5-7-17)24-21-18-13-15(22)3-8-19(18)25-20(26-21)14-9-11-23-12-10-14/h4-7,9-12,15H,3,8,13,22H2,1-2H3,(H,24,25,26)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 8.33 mg/mL (23.11 mM; ultrasonic and warming and heat to 80°C).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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. 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.
In Vivo:
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
Products are for research use only. Not for human use.
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