甲哌啶嗪

甲哌啶嗪用途

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。

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甲哌啶嗪名称

[ CAS 号 ]:
60-89-9

[ 中文名 ]:
哌卡嗪

[ 英文名 ]:
Mepazine

[英文别名 ]:

Lacumin
Pecazine
MEPAZINE
mepasin
Pacatal
Nothiazine
Meprazine
Mepazin
Pecatal
Pakatal

甲哌啶嗪生物活性

[ 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

[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.

甲哌啶嗪物理化学性质

[ 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

甲哌啶嗪毒性和生态

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

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甲哌啶嗪安全信息

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2934300000

甲哌啶嗪海关

[ 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%