≥98% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
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 IC 50 of 2 μM as compared to the anticancer agent Etoposide (IC 50 =120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research
In Vitro
ARN-21934 display a different affinity for topoIIα and topoIIβ. ARN-21934 is more potent against the α isoform, the IC 50 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 IC 50 values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:topoisomerase II alpha topoisomerase II beta
| Canonical Smiles | CN(C)C1=CC=C(C=C1)NC2=NC(=NC3=C2CC(CC3)N)C4=CC=NC=C4 |
|---|---|
| IUPAC Name | 4-N-[4-(dimethylamino)phenyl]-2-pyridin-4-yl-5,6,7,8-tetrahydroquinazoline-4,6-diamine |
| InChIKey | CKXSRLUXTFDZCF-UHFFFAOYSA-N |
| 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) |
| Isomeric SMILES | CN(C)C1=CC=C(C=C1)NC2=NC(=NC3=C2CC(CC3)N)C4=CC=NC=C4 |
| PubChem CID | 135150944 |
| Molecular Weight | 360.46 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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| Solubility | DMSO : 8.33 mg/mL (23.11 mM; ultrasonic and warming and heat to 80°C) |
|---|---|
| Molecular Weight | 360.500 g/mol |
| XLogP3 | 2.600 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 4 |
| Exact Mass | 360.206 Da |
| Monoisotopic Mass | 360.206 Da |
| Topological Polar Surface Area | 80.000 Ų |
| Heavy Atom Count | 27 |
| Formal Charge | 0 |
| Complexity | 458.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 1 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
