半岛bd体育手机客户端 说明
生化/生理作用
SAR405838 (MI-77301) is an orally available (F = 67%/mouse, 48%/rat; 10 mg/kg p.o.), highly potent and selective Mdm2 (Hdm2) inhibitor (human Mdm2 Ki= 0.88 nM; no binding at 10 μM to Bcl-2, Bcl-xL, Mcl-1, Mdmx; no inhibition against >200 receptors/enzymes) that upregulates wild-type p53 activity (EC50= 300-600 nM; SJSA-1) by blocking Mdm2-p53 interaction and Mdm2-mediated p53 degradation with 5-10-times higher potency than MI-219 and nutlin-3a. SAR405838 inhibits cancer growth in a wild-type p53-dependent manner both in cultures (IC50= 89 nM/RS4;11, 92 nM/SJSA-1, 200 nM/HCT-116, 270 nM/LANCaP) and in xenograft modelsin vivo(50-200 mg/kg single or daily p.o. dosing).
基本信息
| 经验(实验)分子式 | C29H34Cl2FN3O3 |
| 分子量 | 562.50 |
| MDL编号 | MFCD28976052 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 储存条件 | desiccated |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | ?20℃ |
| SMILES string | O=C([C@@H]1N[C@@H](CC(C)(C)C)[C@@]2(C(NC3=C2C=CC(Cl)=C3)=O)[C@H]1C4=CC=CC(Cl)=C4F)N[C@@H]5CC[C@H](CC5)O |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
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