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。
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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 ]:
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 ]:
[ 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]
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
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Mepazine hydrochloride安全信息
[ 危害码 (欧洲) ]:
Xi
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相关化合物
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