60-89-9

中文名称哌卡嗪

英文名称 pecazine

CAS 60-89-9

分子式 C19H22N2S

分子量 310.46

MOL 文件 60-89-9.mol

更新日期 2023/03/20 15:41:21

60-89-9 结构式

基本信息物理化学性质图谱信息常见问题列表

基本信息

中文别名

哌卡嗪
甲哌啶嗪

英文别名

Paxital
Pecatal
Lacumin
Mepazin
MEPAZINE
Pacazine
pecazine
Ai3-50131
Nothiazine
Einecs 200-490-8

物理化学性质

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

水溶解性5.588mg/L(24 ºC)

图谱信息

哌卡嗪(60-89-9)核磁图(¹HNMR)

常见问题列表

生物活性

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。

靶点

MALT1

体外研究

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.

体内研究

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.