| Identification | Back Directory | [Name]
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- | [CAS]
2230854-93-8 | [Synonyms]
4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- | [Molecular Formula]
C21H24N6 | [MDL Number]
MFCD34179494 | [MOL File]
2230854-93-8.mol | [Molecular Weight]
360.46 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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. |
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cjbscvictory
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| Telephone: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
| Company Name: |
Bide Pharmatech Ltd.
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| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
| Company Name: |
nanjing
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| Telephone: |
13376084917 13376082704 |
| Website: |
www.linye-e.com/ |
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