哌卡嗪
| 中文名称 | 哌卡嗪 |
|---|---|
| 中文同义词 | 哌卡嗪;甲哌啶嗪;化合物 T16040 |
| 英文名称 | pecazine |
| 英文同义词 | MEPAZINE;10-[(1-Methyl-3-piperidinyl)methyl]-10H-phenothiazine;Nothiazine;Paxital;pecazine;Pacazine;Pecatal;(N-Methyl-3-piperidyl)methylphenothiazine |
| CAS号 | 60-89-9 |
| 分子式 | C19H22N2S |
| 分子量 | 310.46 |
| EINECS号 | 200-490-8 |
| 相关类别 | |
| Mol文件 | 60-89-9.mol |
| 结构式 |  |
哌卡嗪 性质
| 熔点 | 80°C |
|---|---|
| 沸点 | bp4 230-235° |
| 密度 | 1.1252 (rough estimate) |
| 折射率 | 1.6270 (estimate) |
| 储存条件 | Hygroscopic, Refrigerator, under inert atmosphere |
| 溶解度 | DMSO：130 mg/mL（418.73 mM；需要超声波） |
| 水溶解性 | 5.588mg/L(24 ºC) |
Mepazine (Pecazine) 是一种有效的选择性 MALT1 蛋白酶抑制剂。Mepazine 抑制全长 GSTMALT1 和 GSTMALT1 325-760 段的 IC50 分别为 0.83 和 0.42 μM。Mepazine 通过增强细胞凋亡 (apoptosis) 来影响 ABC-DLBCL 细胞的生存能力。
MALT1
Mepazine (5-20 μM; 4 days) causes a decrease of cell viability in the activated B cell subtype of diffuse large B cell lymphoma (ABCDLBCL) cells, without significantly affecting GCB-DLBCL cells.
Cell Viability Assay
| Cell Line: | ABC-DLBCL cell lines (HBL1, OCI-Ly3, U2932, TMD8, OCI-Ly10) and GCB-DLBCL cell lines (BJAB, Su-DHL-6, Su-DHL-4) |
| Concentration: | 5, 10, and 20 μM |
| Incubation Time: | 4 days |
| Result: | Caused a decrease of cell viability in the ABC-DLBCL cells HBL1, OCI-Ly3, U2932, and TMD8, without significantly affecting GCB-DLBCL cells. |
Mepazine (16 mg/kg; intraperitoneal administration) interferes with growth and induces apoptosis of ABC-DLBCL cell line OCI-Ly10 in NOD/scid IL-2Rg null (NSG) mice with a murine DLBCL xenogeneic tumor model. Daily administration of Mepazine strongly impairs the expansion of the ABC-DLBCL cell line OCI-Ly10.
| Animal Model: | 6- to 8-week-old female NOD.Cg- Prkdc scid Il2rg tm1Wjl /SzJ (NSG) mice with a murine DLBCL xenogeneic tumor model |
| Dosage: | 400 μg per animal (25 g), corresponding to approximately 16 mg/kg. |
| Administration: | Intraperitoneal administration; started 1 or 12 days after transplantation and given continuously every 24 hr; daily application |
| Result: | Daily administration strongly impaired the expansion of the ABC-DLBCL cell line OCI-Ly10. |