4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-
![4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Structure](CAS/20210305/GIF/2230854-93-8.gif)
- CAS No.
- 2230854-93-8
- Chemical 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
- CBNumber:
- CB19014210
- Molecular Formula:
- C21H24N6
- Molecular Weight:
- 360.46
- MDL Number:
- MFCD34179494
- MOL File:
- 2230854-93-8.mol
| 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) |
| pka | 9.01±0.20(Predicted) |
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Chemical Properties,Uses,Production
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]
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
Raw materials
Preparation Products
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 4604 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | 024-024-88590548 18341751992 | 757984502@qq.com | China | 888 | 58 |
| ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8011 | 62 |
| Shanghai Rechem science Co., Ltd. | 21-31433387 15618786686 | sales@rechemscience.com | China | 2993 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 3689 | 58 |