| Bioactivity | FLT3D835Y/F691L-IN-1 (compd 8v) is an orally active inhibitor of FLT3 3-tyrosine kinase domain D835Y/F691L secondary mutations with IC50s of 1.5 and 9.7 nM. FLT3D835Y/F691L-IN-1 can be used for acute myeloid leukemia research[1]. |
| Invitro | FLT3D835Y/F691L-IN-1 (0.16-100 nM, 4 h) 抑制 p-FLT3 和细胞周期相关蛋白 CDK4/6 和 Cyclin D3，也抑制转染了 FLT3-ITD、FLT3-ITD-D835Y、FLT3-ITD-F691L、FLT3-ITD-D835Y-F691L 的 Ba/F3 细胞和 MV4-11 急性髓系白血病细胞系 (IC50 值分别为 12.2、10.5、24.6、16.9 和 6.8 nM) 的增殖[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> FLT3D835Y/F691L-IN-1 相关抗体: |
| In Vivo | FLT3D835Y/F691L-IN-1 (30 mg/kg, 口服, 每日一次共 28 天) 抑制 Ba/F3-FLT3-ITD-D835Y 异种移植模型小鼠的肿瘤体积[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| Formula | C26H37N7O4 |
| Molar Mass | 511.62 |
| 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]. Zheng X, et al. Structure-Based Optimization of Pyrazinamide-Containing Macrocyclic Derivatives as Fms-like Tyrosine Kinase 3 (FLT3) Inhibitors to Overcome Clinical Mutations. ACS Pharmacol Transl Sci. 2024 Apr 11;7(5):1485-1506. |