29069-24-7

• 常用中文名：泼尼莫司汀
• 常用英文名：[2-(11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl)-2-oxo-ethyl] 4-[4-[bis(2-chloroethyl)amino]phenyl]butanoate
• CAS号：29069-24-7
• 分子式：C₃₅H₄₅Cl₂NO₆
• 分子量：646.64100
• 相关类别： 原料药 抗肿瘤药 烷化剂类抗肿瘤药
• 发布时间：2018-07-03 17:03:18
• 更新时间：2024-01-08 20:33:07
• 泼尼莫司汀(Leo 1031；NSC 134087)是由泼尼松龙(HY-17463)和氯霉素(HY-13593)形成的酯。普尼莫司汀可用于白血病和淋巴瘤研究[1]。

名称

• 中文名: 泼尼莫司汀
• 英文名: prednimustine
• 英文别名: precorrin-6y; 3,7,12,17-Corrintetrapropanoic acid,2,8,13,18-tetrakis(carboxymethyl)-7,8,11,12-tetradehydro-9,10,11,22-tetrahydro-3,9,13,18,19-pentamethyl-,(1R-(1alpha,2alpha,3beta,9beta,13alpha,17beta,18alpha,19beta))

物化性质

• 密度: 1.3g/cm3
• 沸点: 791.5ºC at 760 mmHg
• 熔点: 163-164ºC
• 分子式: C₃₅H₄₅Cl₂NO₆
• 分子量: 646.64100
• 闪点: 432.5ºC
• 精确质量: 645.26200
• PSA: 104.14000
• LogP: 5.41540
• 蒸汽压: 2.08E-26mmHg at 25°C
• 折射率: 1.606

生物活性

• 描述: 泼尼莫司汀(Leo 1031；NSC 134087)是由泼尼松龙(HY-17463)和氯霉素(HY-13593)形成的酯。普尼莫司汀可用于白血病和淋巴瘤研究[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> DNA烷基化剂/交联剂
• 体内研究: 由于烷基化剂药代动力学的差异,在非荷瘤大鼠模型中,普瑞尼莫司汀(120 mg/kg；皮下注射；单剂量)的毒性远低于等摩尔剂量的氯霉素(HY-13593)(60 mg/kg；单剂量；皮下注射)[1]。普瑞尼莫司汀(40 mg/kg；皮下注射；单次剂量)产生低血浆浓度(小于5μM)的烷基化代谢物氯丁嘧啶和苯乙酸芥,在携带Walker 256癌肉瘤敏感菌株的腹水大鼠中维持48小时[1]。普瑞尼莫司汀(40 mg/kg；皮下注射；单剂量；72小时测量)在吉田肉瘤抗烷基化剂菌株的大鼠模型中显示出抗肿瘤作用[1]。动物模型：非荷瘤雌性Wistar大鼠(150-200g)[1]剂量：120 mg/kg给药：皮下注射；单剂量；结果：大鼠存活率仍为100%,氯霉素治疗组存活率为0%。动物模型：携带吉田肉瘤烷基化剂抗性菌株(150-200g)的雌性Wistar大鼠[1]剂量：40 mg/kg给药：皮下注射；单剂量结果：杀死57%的耐药肿瘤细胞。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TU4153000 CHEMICAL NAME : Pregna-1,4-diene-3,20-dione, 11-beta,17,21-trihydroxy-, 21-(4-(p-(bis(2-chloroethyl)amino) phenyl)butyrate) CAS REGISTRY NUMBER : 29069-24-7 LAST UPDATED : 199612 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C35-H45-Cl2-N-O6 MOLECULAR WEIGHT : 646.71 WISWESSER LINE NOTATION : L E5 B666 OV AHTTT&J A1 CQ E1 FV1OV3R DN2G2G& FQ HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human DOSE/DURATION : 16 mg/kg/4W TOXIC EFFECTS : Behavioral - euphoria Blood - leukopenia Blood - thrombocytopenia REFERENCE : JNMDBO Journal of Medicine (Westbury, NY). (PJD Pub., Ltd., POB 966, Westbury, NY 11590) V.1- 1970- Volume(issue)/page/year: 8,115,1977 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 530 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 1,137,1976 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 128 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EJCAAH European Journal of Cancer. (Oxford, UK) V.1-17(6), 1965-1981. For publisher information, see EJCODS. Volume(issue)/page/year: 13,873,1977 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 128 mg/kg TOXIC EFFECTS : Tumorigenic - active as anti-cancer agent REFERENCE : EJCAAH European Journal of Cancer. (Oxford, UK) V.1-17(6), 1965-1981. For publisher information, see EJCODS. Volume(issue)/page/year: 13,873,1977 *** REVIEWS *** IARC Cancer Review:Animal Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 50,115,1990 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 50,115,1990 IARC Cancer Review:Group 3 IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 50,115,1990