哌卡嗪

生物活性靶点体外研究体内研究哌卡嗪试剂级价格

哌卡嗪

CAS号:60-89-9
英文名:pecazine
中文名:哌卡嗪
CBNumber:CB5876419
分子式:C19H22N2S
分子量:310.46
MOL File:60-89-9.mol

哌卡嗪化学性质

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
溶解度 :DMSO : 130 mg/mL (418.73 mM; Need ultrasonic)
形态 :Oil
颜色 :Light yellow to light brown
水溶解性 :5.588mg/L(24 ºC)

哌卡嗪性质、用途与生产工艺

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.