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4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- manufacturers
- ARN-21934
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- $56.00
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2026-07-14
- CAS:2230854-93-8
- Purity: 99.95%
- Supply Ability: 10g
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| | 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Basic information |
| Product Name: | 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- | | Synonyms: | 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-;DNA relaxation,ARN-21934,Inhibitor,Topoisomerase,anticancer,topoisomerase IIα,ARN 21934,inhibit,ARN21934;N4-(4-(Dimethylamino)phenyl)-2-(pyridin-4-yl)-5,6,7,8-tetrahydroquinazoline-4,6-diamine;ARN-21934, 10 mM in DMSO | | CAS: | 2230854-93-8 | | MF: | C21H24N6 | | MW: | 360.46 | | EINECS: | | | Product Categories: | | | Mol File: | 2230854-93-8.mol | ![4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Structure](CAS/20210305/GIF/2230854-93-8.gif) |
| | 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Chemical Properties |
| Boiling point | 500.4±50.0 °C(Predicted) | | density | 1.230±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 8.33 mg/mL (23.11 mM; ultrasonic and warming and heat to 80°C) | | form | Solid | | pka | 9.01±0.20(Predicted) | | color | Light yellow to green yellow |
| | 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Usage And Synthesis |
| Uses | 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]. | | Biological Activity | 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] | | 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[1] | | IC 50 | topoisomerase II alpha; topoisomerase II beta | | References | [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. |
| | 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Preparation Products And Raw materials |
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