| Bioactivity | Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth[1]. |
| Invitro | Tubulin degrader 1 (0.2-25 μM, 24 h) 通过直接结合 Hela 细胞中的秋水仙碱位点发挥抗增殖活性[1]。Tubulin degrader 1 (0-300 nM, 24 h) 可导致 A2780S 和 A2780T 细胞明显的 G2/M 期细胞周期停滞和细胞凋亡[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Tubulin degrader 1 相关抗体: |
| In Vivo | Tubulin degrader 1 (10-30 mg/kg, 静脉注射, 两天一次, 6-9 次) 在 A2780S 和 A2780T 异种移植模型中具有抗肿瘤活性[1]。药代动力学分析[1]Route |
| Formula | C20H19N5O |
| Molar Mass | 345.40 |
| 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]. Zhang C, et al. Structure-based design and synthesis of BML284 derivatives: A novel class of colchicine-site noncovalent tubulin degradation agents. Eur J Med Chem. 2024 Feb 27;268:116265. |