泼尼莫司汀

泼尼莫司汀用途

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]。

泼尼莫司汀名称

[ 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

[英文别名 ]:

precorrin-6y

泼尼莫司汀生物活性

[ 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。

泼尼莫司汀物理化学性质

[ 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

泼尼莫司汀毒性和生态

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