| Bioactivity | AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity[1]. |
| Invitro | AD57 (0.2 nM) 显著抑制了 ptc > dRetMEN2B 在果蝇幼虫中的致死率[1]。AD57 (0.1 nM) 通过减少 erk 基因剂量提高 ptc > dRetMEN2B 在果蝇中的存活率[1]。 |
| In Vivo | AD57 抑制 RETMEN2 模型中 MEN2B (MZ-CRC-1) 和 MEN2A (TT) 患者来源细胞系的生存能力[1]。AD57 (20 mg/kg) 在常规小鼠异种移植模型中显著抑制基于 TT 的肿瘤生长，无明显细胞毒性[1]。 |
| Name | AD57 |
| CAS | 1093380-42-7 |
| Formula | C22H20F3N7O |
| Molar Mass | 455.44 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Dar AC, et al. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature. 2012 Jun 6;486(7401):80-4. |