化合物 T11896
化合物 T11896 性质
| 沸点 | 718.4±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.317±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：135 mg/mL（259.56 mM；需要超声波） |
| 酸度系数(pKa) | 4.28±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
化合物 T11896 用途与合成方法
IC50: 24.5 µM (ATG4B); Kd: 16 μM (ATG4B)
LV-320 (0-120 µM; SKBR3, MCF7, JIMT1, and MDA-MB-231 cells) treatment results in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines.
LV-320 (120 µM; 48 hours; MDA-MB-231 cells) treatment results in an increase in LC3B-II, indicating that LV-320 blocks autophagic flux.
Western Blot Analysis
| Cell Line: | SKBR3, MCF7, JIMT1, and MDA-MB-231 cells |
| Concentration: | 0 µM, 25 µM, 50 µM, 75 µM, 100 µM, or 120 µM |
| Incubation Time: | |
| Result: | Resulted in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines. |
Cell Autophagy Assay
| Cell Line: | MDA-MB-231 cells |
| Concentration: | 120 µM |
| Incubation Time: | 48 hours |
| Result: | Blocked autophagic flux. |
LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) treatment results in a terminal blood level of 169 µM and a liver level of 104 µM. The expression of GFP-LC3 puncta is significantly greater accumulation in LV-320 treated animals compared to controls. LC3B-II protein is also increased in LV-320-treated animals. The treatment do not cause significant toxicity in mice at either dose.
| Animal Model: | GFP-LC3 mice (females, 9-14 weeks) |
| Dosage: | 100 mg/kg or 200 mg/kg |
| Administration: | Oral gavage; three times over two days (Pharmacokinetic study) |
| Result: | Terminal blood levels were 169 µM and liver levels were 104 µM. LC3B-II protein level was also increased. |
