Mepazine hydrochloride

Mepazine hydrochloride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。

Mepazine hydrochloride名称

[ CAS 号 ]:
2975-36-2

[ 中文名 ]:
甲哌啶嗪盐酸盐

[ 英文名 ]:
Mepazine hydrochloride

[英文别名 ]:

mepazine hydrochloride

Mepazine hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> NF-κB信号通路 >> MALT1

[ 靶点 ]

MALT1[1]

[体外研究]

甲哌嗪(5-20μM；4天)可导致弥漫性大B细胞淋巴瘤(ABCDLBCL)活化B细胞亚型的细胞活力下降,而对GCB-DLBCL细胞无明显影响[1]。细胞活力测定[1]细胞系：ABC-DLBCL细胞系(HBL1、OCI-Ly3、U2932、TMD8、OCI-Ly10)和GCB-DLBCL细胞系(BJAB、Su-DHL-6、Su-DHL-4)浓度：5、10、20μM孵育时间：4天结果：导致ABC-DLBCL细胞HBL1、OCI-Ly3、U2932和TMD8的细胞活力下降,对GCB-DLBCL细胞无明显影响。

[体内研究]

甲哌嗪(16mg/kg；腹腔给药)干预NOD/scid IL-2Rgnull(NSG)小鼠DLBCL异种肿瘤模型的生长并诱导凋亡。每天服用美帕嗪会严重损害ABC-DLBCL细胞系OCI-Ly10的扩张[1]。动物模型：6～8周龄雌性点头Cg-小鼠腹腔注射prkdg/kg,连续给药,每24天注射1μg/kg的小鼠；每日应用结果：每日给药可明显抑制ABC-DLBCL细胞株OCI-Ly10的增殖。

[参考文献]

[1]. Nagel D, et al. Pharmacologic inhibition of MALT1 protease by phenothiazines as a therapeutic approach for the treatment of aggressive ABC-DLBCL. Cancer Cell. 2012 Dec 11;22(6):825-37.

Mepazine hydrochloride物理化学性质

[ 沸点 ]:
444.4ºC at 760 mmHg

[ 分子式 ]:
C₁₉H₂₃ClN₂S

[ 分子量 ]:
346.91700

[ 闪点 ]:
222.6ºC

[ 精确质量 ]:
346.12700

[ PSA ]:
31.78000

[ LogP ]:
5.43600

[ 蒸汽压 ]:
4.29E-08mmHg at 25°C

[ 储存条件 ]:
2-8°C，干燥，密封

Mepazine hydrochloride毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SP2800000

CHEMICAL NAME :: Phenothiazine, 10-((1-methyl-3-piperidyl)methyl)-, monohydrochloride

CAS REGISTRY NUMBER :: 2975-36-2

LAST UPDATED :: 199510

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C19-H22-N2-S.Cl-H

MOLECULAR WEIGHT :: 346.95

WISWESSER LINE NOTATION :: T C666 BN ISJ B1- CT6NTJ A1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,28,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,28,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 155 mg/kg

TOXIC EFFECTS :: Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: CKFRAY Ceskoslovenska Farmacie. (PNS-Ustredni Expedice a Dovoz Tisku, Kafkova 19, 160 00 Prague 6, Czechoslovakia) V.1- 1952- Volume(issue)/page/year: 6,365,1957

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,28,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 750 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,28,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 62 mg/kg

TOXIC EFFECTS :: Behavioral - sleep

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 19,87,1962

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,28,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,28,1972

Mepazine hydrochloride安全信息

[ 危害码 (欧洲) ]:
Xi