PB28DIHYDROCHLORIDE
PB28DIHYDROCHLORIDE 性质
| 沸点 | 501.4±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.032±0.06 g/cm3(Predicted) |
| 储存条件 | Desiccate at +4°C |
| 溶解度 | H2O：60°C 时约 10mg/mL |
| 酸度系数(pKa) | 8.32±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色 |
| 水溶解性 | H2O: ~10mg/mL at60°C |
PB28DIHYDROCHLORIDE 用途与合成方法
Ki: 0.68 nM (σ2 receptor); 0.38 nM (σ1 receptor)
PB28 (15-25 nM; 24-48 hours; MCF7 and MCF7 ADR cells) treatment shows an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that are time and concentration independent.
PB28 has a higher σ2 receptor affinity expressed as K
i
(0.28 nM and 0.17 nM in MCF7 and MCF7 ADR cells, respectively) than σ1 receptor affinity (13.0 nMand 10.0 nM, respectively).
PB28 inhibits cell growth of MCF7 and MCF7 ADR cells with IC
50
s of 25 nM and 15 nM, respectively after 2-day treatment.
PB28 induces apoptosis through a caspase-independent pathway.
PB28 also reduces P-gp expression in a concentration- and time-dependent manner (approximately 60% in MCF7 and 90% in MCF7 ADR).
PB28 displays antiproliferative and cytotoxic effects in both C6 rat glioma and SK-N-SH human neuroblastoma cell lines.
Cell Cycle Analysis
| Cell Line: | MCF7 and MCF7 ADR cells |
| Concentration: | 25 nM and 15 nM |
| Incubation Time: | 24 hours, 48 hours |
| Result: | Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent. |
PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice.
| Animal Model: | C57BL/6 female mice (10 weeks old) injected with Panc02 cells |
| Dosage: | 10.7 mg/mL |
| Administration: | Intraperitoneal injection; daily; for two weeks |
| Result: | Inhibited tumor growth in Panc02 tumor burden mice. |
