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Product details

名称

ARN-21934

分子类型

未知

英文名称

ARN-21934

货号

A651864-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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

生化机理

ARN-21934 是一种强效、高选择性、血脑屏障 (BBB) 穿透性抑制剂，可抑制人类拓扑异构酶 II α 和 β。ARN-21934还能

CAS号

2230854-93-8

分子式

C21H24N6

分子量

360.46 g/mol

PubChem编号

135150944

Isomeric SMILES

CN(C)C1=CC=C(C=C1)NC2=NC(=NC3=C2CC(CC3)N)C4=CC=NC=C4

IIUPAC Name

4-N-[4-(dimethylamino)phenyl]-2-pyridin-4-yl-5,6,7,8-tetrahydroquinazoline-4,6-diamine

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)

InChi Key

CKXSRLUXTFDZCF-UHFFFAOYSA-N

Smiles

CN(C)C1=CC=C(C=C1)NC2=NC(=NC3=C2CC(CC3)N)C4=CC=NC=C4

PubChem CID

135150944

溶解性

DMSO : 8.33 mg/mL (23.11 mM; ultrasonic and warming and heat to 80°C)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

360.206 Da

单同位素质量Monoisotopic Mass

360.206 Da

拓扑极表面积Topological Polar Surface Area

80.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

458

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

2.6

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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