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Procarbazine hydrochloride (NSC-77213 HCl) 是一种烷化剂,是甲基肼衍生物的盐酸盐,具有抗肿瘤和诱变活性。
Procarbazine hydrochloride (NSC-77213 HCl) 是一种烷化剂,是甲基肼衍生物的盐酸盐,具有抗肿瘤和诱变活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 123 | 现货 | |
10 mg | ¥ 165 | 现货 | |
25 mg | ¥ 253 | 现货 | |
50 mg | ¥ 359 | 现货 | |
100 mg | ¥ 519 | 现货 | |
500 mg | ¥ 1,260 | 现货 | |
1 g | ¥ 1,860 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 283 | 现货 |
产品描述 | Procarbazine hydrochloride (NSC-77213 HCl) is the hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction. |
体外活性 | Procarbazine与Cu(II)共同作用,诱导在5'-ACG-3'序列(与p53基因的一个热点互补)和5'-TG-3'序列处产生piperidine敏感性损伤和formamidopyrimidine-DNA糖苷酶敏感性损伤。Procarbazine通过非酶方式生成Cu(I)-过氧化物复合物和甲基自由基来导致DNA损伤。[1] 在血液细胞中,Procarbazine表现出强烈的染色体断裂效应,并且在高剂量治疗后在多种器官中表现为突变原性。[2] |
体内活性 | Procarbazine在黄金仓鼠中显著降低了睾丸和附睾的重量,并且极大地减少了单倍体细胞数量和精子生成停滞,显示出在测试中的差异性。[3] Procarbazine在褐色脂肪组织中对MAO A的增效作用呈剂量依赖性,经单甲基肼处理后,其增效作用更为显著,活性可达对照组匀浆的350%。在大鼠中,Procarbazine或单甲基肼以与之前在血管匀浆中外源性确定的相同程度降低了该胺的代谢。[4] Procarbazine在多种复杂测试系统中均表现出致突变、致染色体断裂和致畸性,且是一种广谱致癌物,在啮齿类动物和猴子中引发造血系统、乳腺、肺和神经系统的肿瘤。体内,Procarbazine经历一系列复杂的代谢变化,生成包括甲基化剂和自由基在内的多种化学活性物种。[5] |
别名 | NSC-77213 HCl, Procarbazine HCl, 盐酸甲基苄肼 |
分子量 | 257.76 |
分子式 | C12H19N3O·HCl |
CAS No. | 366-70-1 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 48 mg/mL (186.2 mM) DMSO: 45 mg/mL (174.58 mM) Ethanol: 22 mg/mL (85.4 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO/H2O
DMSO/H2O
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