| Bioactivity | Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min[1]. |
| Invitro | Anticancer agent 98 抑制黑色素瘤、乳腺癌和胰腺癌的癌症增殖，IC50 范围为 0.6-3 nM[1]。Anticancer agent 98 (300 nM、1 μM 或 3 μM；2 小时) 剂量依赖性地增加 PC-3 细胞中的 β-微管蛋白加合物[1]。Anticancer agent 98 (3.125、6.25、12.5、25 和 50 μM) 对微管蛋白具有高结合亲和力，SPR 光谱分析的 Kd 值为 16.9 μM[1]。Anticancer agent 98 (10 μM、50 μM；0-60 分钟) 在 60 分钟内强烈抑制微管蛋白聚合[1]。Anticancer agent 98 (100 nM; 4 h) 在体外对 COS-7 细胞具有抗增殖和抗血管生成作用[1]。体外代谢稳定性[1]human microsomes |
| In Vivo | Anticancer agent 98 (2.5 mg/kg；静脉注射；每周两次，持续 2 周) 耐受性良好，在雄性 NSG 小鼠的 PC3/TxR 异种移植肿瘤中没有显着的体重减轻。相对于 Paclitaxel (HY-B0015；10 mg/kg，每周一次) 和对照组，Anticancer agent 98 还显着减缓了前列腺癌肿瘤的进展[1]。NSG 小鼠中的药代动力学分析[1]Route |
| Name | Anticancer agent 98 |
| CAS | 2857070-72-3 |
| Formula | C17H19N5O2 |
| Molar Mass | 325.37 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Pochampally S, et al. Design, Synthesis, and Biological Evaluation of Pyrimidine Dihydroquinoxalinone Derivatives as Tubulin Colchicine Site-Binding Agents That Displayed Potent Anticancer Activity Both In Vitro and In Vivo[J]. ACS Pharmacology & Translational Science, 2023. |
Anticancer agent 98
CAS: 2857070-72-3 F: C17H19N5O2 W: 325.37
Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98
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