60-89-9
中文名稱
哌卡嗪
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
哌卡嗪甲哌啶嗪
英文別名
PaxitalPecatal
Lacumin
Mepazin
MEPAZINE
Pacazine
pecazine
Ai3-50131
Nothiazine
Einecs 200-490-8
物理化學性質(zhì)
熔點80°C
沸點bp4 230-235°
密度1.1252 (rough estimate)
折射率1.6270 (estimate)
儲存條件Hygroscopic, Refrigerator, under inert atmosphere
溶解度DMSO : 130 mg/mL (418.73 mM; Need ultrasonic)
形態(tài)Oil
顏色Light yellow to light brown
水溶解性5.588mg/L(24 ºC)
常見問題列表
生物活性
Mepazine (Pecazine) 是一種有效的選擇性 MALT1 蛋白酶抑制劑。Mepazine 抑制全長 GSTMALT1 和 GSTMALT1 325-760 段的 IC50 分別為 0.83 和 0.42 μM。Mepazine 通過增強細胞凋亡 (apoptosis) 來影響 ABC-DLBCL 細胞的生存能力。靶點
MALT1
體外研究
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. |
體內(nèi)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. |