2975-36-2

• 常用中文名：Mepazine hydrochloride
• 常用英文名：Mepazine hydrochloride
• CAS号：2975-36-2
• 分子式：C₁₉H₂₃ClN₂S
• 分子量：346.91700
• 相关类别： 信号通路 细胞凋亡 细胞凋亡
• 发布时间：2016-08-14 08:04:56
• 更新时间：2024-01-06 19:26:33
• 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。

名称

• 中文名: 甲哌啶嗪盐酸盐
• 英文名: 10H-Phenothiazine,10-[(1-methyl-3-piperidinyl)methyl]-, hydrochloride (1:1)
• 英文别名: mepazine hydrochloride

物化性质

• 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

生物活性

• 描述: 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。
• 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.

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

安全

• 危害码 (欧洲): Xi