| Bioactivity | A011 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. A011 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). A011 combines with CPT-11 shows antitumor activity[1]. |
| Invitro | A011 (compound 8d) (10, 30, 100 nM; 5 days) 增加 SW620 和 HCT116 细胞对 CPT-11 (HY-16562) (100 nM) 的敏感性[1]。A011 (0-100 nM; 24, 72 h) 与 CPT-11 联用可诱导细胞凋亡和细胞周期停滞在 G2/M 期[1]。A011 (3, 9, 27, 83, 250 nM) 在 1.5 或 3 Gy 照射条件下以剂量依赖性方式降低 SW620 细胞中 p-ATM 和 p-Chk2 的表达[1] . Cell Proliferation Assay[1] Cell Line: |
| In Vivo | A011 (5 mg/kg；腹腔注射；每天一次，持续 23 天) 与 CPT-11 (5 mg/kg，腹腔注射；每周一次) 联合用药在小鼠体内显示出抗肿瘤活性[1]。 Animal Model: |
| Name | A011 |
| Formula | C27H28N6O |
| Molar Mass | 452.55 |
| 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]. Shiyu Zhang, et al. Discovery of [1,2,3]Triazolo[4,5-c]quinoline Derivatives as a New Class of Ataxia-Telangiectasia Mutated Kinase Inhibitors. ACS Med. Chem. Lett. 2023. |