| Bioactivity | CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026)[1]. |
| Invitro | CHK1-IN-9 (compound 11) (11.11, 33.33, 100, and 300 nM, 16 h) 对肿瘤细胞具有增殖抑制作用，其中对 MV-4-11 细胞的 IC50 值为 202 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CHK1-IN-9 相关抗体: Cell Proliferation Assay [1] Cell Line: |
| In Vivo | CHK1-IN-9 (compound 11) (每天使用 30 mg/kg，连续21天，iv or po) 单独使用时对 HT-29 异种移植小鼠模型的肿瘤生长抑制 (TGI) 值为 20.6％，与 Gemcitabine (HY-17026) 联合使用时显示出更大的抗肿瘤活性 (TGI = 42.8%)[1]。HT-29异种移植小鼠模型中的药代动力学分析[1]Route |
| Formula | C19H18F2N8O |
| Molar Mass | 412.40 |
| 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]. Hu S, et al. Discovery of pyrido[3,2-d]pyrimidin-6(5H)-one derivatives as checkpoint kinase 1 (CHK1) inhibitors with potent antitumor efficacy. Eur J Med Chem. 2024 Apr 5;269:116351. |