60-89-9

• 常用中文名：甲哌啶嗪
• 常用英文名：Mepazine
• CAS号：60-89-9
• 分子式：C₁₉H₂₂N₂S
• 分子量：310.45600
• 相关类别： 信号通路 细胞凋亡 细胞凋亡
• 发布时间：2018-08-25 12:35:19
• 更新时间：2024-01-14 20:03:47
• Mepazine (Pecazine) 是一种有效的选择性 MALT1 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。

名称

• 中文名: 哌卡嗪
• 英文名: 10-[(1-methylpiperidin-3-yl)methyl]phenothiazine
• 英文别名: Lacumin; 10-[(1-methyl-3-piperidinyl)methyl]-10H-phenothiazine; Pecazine; MEPAZINE; 10-(1-methyl-piperidin-3-ylmethyl)-10H-phenothiazine; mepasin; Pacatal; Nothiazine; Meprazine; Mepazin; Pecatal; Pakatal; 10-(1-methyl-[3]piperidylmethyl)-phenothiazine

物化性质

• 密度: 1.159 g/cm3
• 沸点: 444.4ºC at 760 mmHg
• 分子式: C₁₉H₂₂N₂S
• 分子量: 310.45600
• 闪点: 222.6ºC
• 精确质量: 310.15000
• PSA: 31.78000
• LogP: 4.63400
• 折射率: 1.627
• 储存条件: 2-8°C，干燥，密封

生物活性

• 描述: Mepazine (Pecazine) 是一种有效的选择性 MALT1 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。
• 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
• 体外研究: 美帕嗪(5-20μM；4天)导致弥漫性大B细胞淋巴瘤(ABCDLBCL)细胞活化B细胞亚型的细胞活性降低,但对GCB-DLBCL细胞无明显影响[1]。细胞活力测定[1]细胞株：ABC-DLBCL细胞株(HBL1,OCI-Ly3,U2932,TMD8,OCI-Ly10)和GCB-DLBCL细胞株(BJAB,Su-DHL-6,Su-DHL-4)浓度：5,10,20μM培养时间：4天结果：导致ABC-DLBCL细胞株HBL1,OCI-Ly3,U2932,TMD8细胞活力下降,对GCB-DLBCL细胞无明显影响。
• 体内研究: 美帕嗪(16mg/kg；腹腔给药)干预NOD/scid-IL-2Rgnull(NSG)荷瘤小鼠ABC-DLBCL细胞系OCI-Ly10的生长并诱导其凋亡。每天服用美帕嗪会严重损害ABC-DLBCL细胞系OCI-Ly10的增殖[1]。动物模型：6-8周龄雌性NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ(NSG)小鼠,小鼠DLBCL异种肿瘤模型[1]剂量：400μg/只(25g),相当于约16mg/kg。给药：腹腔给药；移植后1或12天开始,每24小时连续给药；每日给药结果：每日给药严重损害ABC-DLBCL细胞系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 : SP2625000 CHEMICAL NAME : Phenothiazine, 10-((1-methyl-3-piperidyl)methyl)- CAS REGISTRY NUMBER : 60-89-9 LAST UPDATED : 199707 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C19-H22-N2-S MOLECULAR WEIGHT : 310.49 WISWESSER LINE NOTATION : T C666 BN ISJ B1- CT6NTJ A1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 200 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 24,136,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 140 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 8,489,1958 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 : CANJAE Canadian Anaesthetists' Society Journal. (Toronto, Ont., Canada) V.1-33, 1954-86. Volume(issue)/page/year: 3,224,1956 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 70 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 4,232,1954 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 : CANJAE Canadian Anaesthetists' Society Journal. (Toronto, Ont., Canada) V.1-33, 1954-86. Volume(issue)/page/year: 3,224,1956 *** REVIEWS *** TOXICOLOGY REVIEW JMSCA9 Journal of Mental Science. (London, UK) V.4-108, 1857-1962. For publisher information, see BJPYAJ. Volume(issue)/page/year: 106,755,1960

安全

• 危害码 (欧洲): Xi
• 海关编码: 2934300000

海关

海关编码	2934300000
中文概述	2934300000. 含一个吩噻嗪环系的化合物(吩噻嗪环系不论是否氢化,化合物未经进一步稠合的 ). 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途
Summary	2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%