4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-

Product Name: 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-
CAS No.: 2230854-93-8
Chemical Name: 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-
Synonyms: ARN-21934, 10 mM in DMSO;N4-(4-(Dimethylamino)phenyl)-2-(pyridin-4-yl)-5,6,7,8-tetrahydroquinazoline-4,6-diamine;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
Formula Weight: 360.46
MOL File: 2230854-93-8.mol

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4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Property

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

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Hazard and Precautionary Statements (GHS)

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4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Chemical Properties,Usage,Production

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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4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)- Suppliers

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2230854-93-8, 4,6-Quinazolinediamine, N4-[4-(dimethylamino)phenyl]-5,6,7,8-tetrahydro-2-(4-pyridinyl)-Related Search:

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

2230854-93-8