米帕林盐酸盐
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- CAS号:
- 6151-30-0
- 英文名:
- Mepacrine hydrochloride
- 英文别名:
- mepacrinehcl;hloride2h2-o;QuinacrineHCl;AtabrineMepacnine;ochloride,dihydrate;Mipalin hydrochloride;Quinacrinehydrochlorid;Mepacrine hydrochloride;QUINACRINE,ATABRINE MEPACNINE;atabrinehydrochloridedihydrate
- 中文名:
- 米帕林盐酸盐
- 中文别名:
- 米帕林;盐酸阿伯平;米帕林盐酸盐;奎纳克林盐酸盐;奎纳克林二盐酸盐二水合物;N4-(6-氯-2-甲氧基-9-吖啶基)-N1,N1-二乙基-1,4-戊二胺二盐酸盐二水合物
- CBNumber:
- CB4138653
- 分子式:
- C23H36Cl3N3O3
- 分子量:
- 508.91
- MOL File:
- 6151-30-0.mol
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米帕林盐酸盐性质、用途与生产工艺
Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) 是一种抗疟剂 (antimalarial)，在体内外均具有抗肿瘤作用。Quinacrine hydrochloride hydrate 抑制 NF-κB 并激活 p53 信号转导，诱导肿瘤细胞发生凋亡 (apoptosis)。
Quinacrine (5-20 μM; 24 hours) inhibits the growth of SGC-7901 cells.
Quinacrine (7.5 and 15 μM; 24 hours) induces apoptosis in SGC-7901 cells, which is associated with mitochondria-dependent signal pathway and involves p53 upregulation and caspase-3 activation pathway.
Quinacrine (15 μM; 24 hours) treatment significantly increased the levels of proapoptotic proteins, including cytochrome c, Bax, and p53, and decreased the levels of antiapoptotic protein Bcl-2, thus shifting the ratio of Bax/Bcl-2 in favor of apoptosis .
Cell Viability Assay
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Cell Line:
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SGC-7901 cells
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Concentration:
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0, 5, 10, 15, and 20 μM
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Incubation Time:
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24 hours
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Result:
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Cell viability was inhibited in a dose-dependent manner, and the mean IC
50
value is 16.18 μM.
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Apoptosis Analysis
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Cell Line:
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SGC-7901 cells
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Concentration:
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7.5 and 15 μM
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Incubation Time:
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24 hours
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Result:
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The percentage of apoptotic cells, including the early phase and late phase apoptosis, increased to 26.30%, compared with control group of 3.37%.
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Western Blot Analysis
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Cell Line:
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SGC-7901 cells
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Concentration:
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15 μM
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Incubation Time:
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24 hours
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Result:
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The relative quantity of cytochrome c protein was upregulated, increased from 0.10 to 0.24.
The relative quantity of p53 protein was dramatically increased, from 0.06 to 0.19.
The Bax/Bcl-2 ratio was dramatically elevated from 1.21 to 2.59.
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Quinacrine (100 mg/kg three times per week for two consecutive weeks) significantly suppresses circulating blast cells at days 30/31 and increases the median survival time (MST). Quinacrine does not decrease the body weight of treated animals at the tested dose.
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Animal Model:
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Female SCID mice with acute myeloid leukemia (AML)-PS model
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Dosage:
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100 mg/kg
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Administration:
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Administered by oral gavage (po); three times a week for two consecutive weeks
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Result:
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In the first AML mouse in vivo study, evaluation of circulating leukemic cells detected in blood samples (in percent of white blood cells (WBC)) at day 30/31 showed 72% human tumor cells in the control mice, whereas in mice treated with Quinacrine, this was only 2.2%.
The MST of control mice was 34 days whereas it was 46 days in Quinacrine-treated mice.
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米帕林盐酸盐
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/16 | S5435 | 米帕林盐酸盐
Quinacrine Dihydrochloride Dihydrate | 6151-30-0 | 25mg | 794.67元 |
6151-30-0, 米帕林盐酸盐 相关搜索:
- 药靶配体
- 化学试剂
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- 医药原料药-科研原料
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- Mipalin hydrochloride
- Mepacrine hydrochloride USP/EP/BP
- Mepacrine Dihydrochloride Dihydrate
- 1,4-PentanediaMine,N4-(6-chloro-2-Methoxy-9-acridinyl)-N1,N1-diethyl-, hydrochloride, hydrate(1:2:2)
- Quinacrine Hydrochloride (200 mg)
- Quinacrine dihydrochloride dihydrate,97%
- N4-(6-Chloro-2-methoxy-9-acridinyl)-N1,N1-diethyl-1,4-pentanediamine dihydrochloride dihydrate
- Mepacrine hydrochloride
- QUINACRINE,ATABRINE MEPACNINE
- Quinacrinehydrochlorid
- QuinacrineHCl
- AtabrineMepacnine
- ochloride,dihydrate
- mepacrinehydrochloridedihydrate
- mepacrinehcl
- hloride2h2-o
- atabrinehydrochloridedihydrate
- 6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2-methoxyacridinedihydroc
- 6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2-methoxy-acridindihydr
- QUINACRINE HYDROCHLORIDE, DIHYDRATE
- QUINACRINE DIHYDROCHLORIDE DIHYDRATE