| Bioactivity | Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. Anti-tumor activity[1][2][3]. |
| Invitro | Nedisertib (化合物 136) 是一种有效的选择性 DNA-PK 抑制剂，对 DNA-PK 的 IC50 为 0 --> Nedisertib 相关抗体: |
| In Vivo | 结合 IR，Nedisertib 在所有 6 种人类癌症小鼠模型中均显示出疗效。在所有模型中，与单独使用 IR 相比，每天 2 Gy 的剂量与 Nedisertib 联合使用可诱导静态显著的肿瘤生长抑制。在任何研究中，单独使用或与 IR 联合使用的 Nedisertib 都不会在小鼠中引起显著的体重减轻或视觉毒性迹象[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 1637542-33-6 |
| Formula | C24H21ClFN5O3 |
| Molar Mass | 481.91 |
| Appearance | 固体 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
| Reference | [1]. L. Damstrup, et al. M3814, a DNA-dependent Protein Kinase Inhibitor (DNA-PKi), Potentiates the Effect of Ionizing Radiation (IR) in Xenotransplanted Tumors in Nude Mice. IJROBP. 2016; 94, 940-941. [2]. Frank T. Zenke, et al. Abstract 1658: M3814, a novel investigational DNA-PK inhibitor: enhancing the effect of fractionated radiotherapy leading to complete regression of tumors in mice. AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1658. [3]. Thomas Fuchss, et al. Arylchinazoline. WO2014183850A1. |