


| 货号 | 包装规格 | 操作 |
|---|---|---|
| 5.08053.0001 | 10 mg |
A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM142-161 for Mcl-1, but not Bcl-xL, binding (IC50 = 310 nM vs >40 µM; [Mcl-1] & [Bcl-xL] = 6.25 nM), displaying little inhibitory potency toward CYP450 isoforms 1A2/2D6/3A4/2C9 (IC50 = >10 µM). Antiproliferation potencies against 2 murine lymphoma cell lines (GI50 = 300 nM/ MCl1-1780 & 1.1 µM/Bcl2-1863) and 11 human cancer lines of various origins (GI50 from 1.6 to 25 µM) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment. Stability studies using murine and human liver microsome preparations reveal t1/2 values of 40 min and 55 min, respectively.
细胞渗透性:是
一级靶点Mcl-1
是否可逆:是
惰性气体包装
Richard,D.J.等人,2013年。生物有机医学化学,21,6642。
| 英文名称 | Mcl-1 Inhibitor II |
| CAS 号 | 315698-17-0 |
| 经验分子式 | C23H24F3N3O |
| 分子量 | 415.45 |
| MDL 号 | MFCD02330695 |
| UNSPSC | 12352200 |
| NACRES | NA.77 |
| InChI key | 乌夫法奥萨-N |
| SMILES字符串 | 碳四氯化碳 |
| 含量测定 | ≥95%(HPLC) |
| 形态 | 粉末 |
| 制造商/商标 | 钙生化® |
| 储存条件 | 可冷冻;避光保存 |
| 颜色 | 白色 |
| 溶解性 | DMSO:25 mg/mL |
| 质量等级 | 100 |
| 网页元数据关键词.default | 7-4-乙基哌嗪-1-基(4-(三氟甲基)苯基)甲基)喹啉-8-醇化学品; 7-4-乙基哌嗪-1-基(4-(三氟甲基)苯基)甲基)喹啉-8-醇; Mcl-1BH3-结合沟抑制剂; Mcl-1抑制剂II 315698 - 17 - 0; Mcl-1抑制剂II IC50 310nM;用于细胞测定的Mcl-1抑制剂II;用于药物开发应用的Mcl-1抑制剂II;实验室用Mcl-1抑制剂II; Mcl-1抑制剂II实验室级产品; Mcl-1选择性抑制剂1.1 µ M;髓细胞白血病-1抑制剂II M |
| 储存温度 | 2-8°C |
| 包装规格(货号 5.08053.0001) | 10 mg |