CAS号：2975-36-2
|
英文名称：10-[(1-methyl-3-piperidyl)methyl]-10H-phenothiazine monohydrochloride
分子式
C19H23ClN2S
分子量
347
EINECS号
221-020-8
MDL
Smiles
InChIKey
哌卡嗪盐酸盐化学百科
基本信息
| 中文名称 | 哌卡嗪盐酸盐 |
| 英文名称 | 10-[(1-methyl-3-piperidyl)methyl]-10H-phenothiazine monohydrochloride |
| CAS号 | 2975-36-2 |
| 分子式 | C19H23ClN2S |
| 分子量 | 346.91732 |
| EINECS号 | 221-020-8 |
物化性质
| 熔点 | 180-181 °C |
| 沸点 | 180-183 °C(Press: 0.5 Torr) |
| 溶解度 | 二甲基亚砜：50 mg/ml（144.13 mM） |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
安全信息
生产及用途
Mepazine hydrochloride (Pecazine hydrochloride) 是一种有效的选择性 MALT1 蛋白酶抑制剂。Mepazine hydrochloride 抑制全长 GSTMALT1 和 GSTMALT1 325-760 段的IC50 分别为 0.83 和 0.42 μM。Mepazine hydrochloride 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. |
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