021-51111890
购物车（）
sales@molnova.cn
ARN-21934
CAS No. 2230854-93-8
ARN-21934 ( —— )
产品货号. M28108 CAS No. 2230854-93-8
ARN-21934 是一种有效的、选择性的人拓扑异构酶 II α 和拓扑异构酶 II β 抑制剂。与抗癌剂依托泊苷 (IC50 = 120 μM) 相比，ARN-21934 (IC50 = 2 μM) 可抑制 DNA 松弛。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥1349 | 有现货 |
|
| 10MG | ￥2024 | 有现货 |
|
| 25MG | ￥3190 | 有现货 |
|
| 50MG | ￥4390 | 有现货 |
|
| 100MG | ￥5724 | 有现货 |
|
| 200MG | ￥7713 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥1102 | 有现货 |
|
生物学信息
-
产品名称ARN-21934
-
注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
-
产品简述ARN-21934 是一种有效的、选择性的人拓扑异构酶 II α 和拓扑异构酶 II β 抑制剂。与抗癌剂依托泊苷 (IC50 = 120 μM) 相比，ARN-21934 (IC50 = 2 μM) 可抑制 DNA 松弛。
-
产品描述ARN-21934 is a potent and selective inhibitor for human topoisomerase II α and topoisomerase II β. ARN-21934(IC50 = 2 μM) inhibits DNA relaxation as compared to the anticancer agent Etoposide (IC50=120 μM).(In Vitro):ARN-21934 is more potent against the α isoform. ARN-21934 exhibits a small panel of human cancer cell lines such as melanoma (A375, IC50 = 12.6 μM and G-361, IC50 = 8.1 μM), breast (MCF7, IC50 = 15.8 μM), endometrial (HeLa, IC50 = 38.2 μM), lung (A549, IC50 = 17.1 μM), and androgen-independent prostate (DU145, IC50 = 11.5 μM) cancer cells.(In Vivo):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. ARN-21934 (intraperitoneal injection; 10 mg/kg) reaches a maximal plasma concentration of 0.68 μg/mL after 15 min. The half-life and clearance value are 149 min in circulation and 0.116 L/(min kg).
-
体外实验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.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.
-
体内实验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
-
同义词——
-
通路Cell Cycle/DNA Damage
-
靶点Topoisomerase
-
受体——
-
研究领域——
-
适应症——
化学信息
-
CAS Number2230854-93-8
-
分子量360.46
-
分子式C21H24N6
-
纯度>98% (HPLC)
-
溶解度In Vitro:?DMSO : 8.33 mg/mL (23.11 mM)
-
SMILESN/A
-
化学全称——
运输与储存
-
储存条件(-20℃)
-
运输条件With Ice Pack
-
稳定性≥ 2 years
参考文献
1.Yang J, et al. Dimethylolurea as a Novel Slow-Release Nitrogen Source for Nitrogen Leaching Mitigation and Crop Production. J Agric Food Chem. 2019 Jul 10;67(27):7616-7625.
产品手册
关联产品
-
DRF-1042
DRF-1042 是一种具有口服活性的喜树碱类似物，具有抑制 DNA 拓扑异构酶 I (DNA topoisomerase I) 的作用。DRF-1042 对一组人癌细胞株，包括多药耐药 (MDR)表型，显示出良好的抗癌活性。
-
Voreloxin
一种一流的抗癌喹诺酮衍生物，可插入 DNA 并抑制拓扑异构酶 II。
-
Exatecan Mesylate
Exatecan Mesylate 是一种 DNA 拓扑异构酶 I 抑制剂（IC50：2.2 μM，0.975 μg/mL）。Exatecan Mesylate (DX-8951f) 显着抑制多种癌细胞系的增殖，平均 GI50 为 2.02 ng/mL、2.92 ng/mL对于乳腺癌细胞、结肠癌细胞、胃癌细胞和肺癌细胞分别为 1.53 ng/mL 和 0.877 ng/mL。
