671-16-9

• 常用中文名：甲基苄肼
• 常用英文名：Procarbazine
• CAS号：671-16-9
• 分子式：C₁₂H₁₉N₃O
• 分子量：221.299
• 相关类别： 原料药 抗肿瘤药 抗肿瘤辅助用药
• 发布时间：2018-03-19 08:00:00
• 更新时间：2024-01-04 20:09:35
• 丙卡巴嗪是一种口服活性烷基化剂,具有抗癌活性。丙卡巴嗪可用于霍奇金病的研究[1][2]。

名称

• 中文名: 甲基苄肼
• 英文名: procarbazine
• 中文别名: 甲肼苄甲酰异丙胺; N-异丙基-4-((2-甲基肼)甲基)苯甲酰胺
• 英文别名: 4-[(2-methylhydrazinyl)methyl]-N-(propan-2-yl)benzamide; Natulan; Procarbazine; N-(1-methylethyl)-4-[(2-methylhydrazino)methyl]benzamide; Benzamide, N-(1-methylethyl)-4-((2-methylhydrazino)methyl)-; N-Isopropyl-4-[(2-methylhydrazino)methyl]benzamide; Procarbazina; [4-(2-methyl-hydrazino)-methyl-benzoic acid-isopropylamide]; Procarbazinum; Ibenzmethyzin; EINECS 211-582-2; MFCD00866411; N-Isopropyl-4-((2-methylhydrazinyl)methyl)benzamide; Benzamide, N-(1-methylethyl)-4-[(2-methylhydrazino)methyl]-; Benzamide, N-(1-methylethyl)-4-[(2-methylhydrazinyl)methyl]-; 4-[(2-methylhydrazinyl)methyl]-N-propan-2-ylbenzamide; Procarbazin; N-isopropyl-4-[(N'-methylhydrazino)methyl]benzamide

物化性质

• 密度: 1.0±0.1 g/cm3
• 沸点: 384.6±35.0 °C at 760 mmHg
• 分子式: C₁₂H₁₉N₃O
• 分子量: 221.299
• 闪点: 148.9±26.1 °C
• 精确质量: 221.152817
• PSA: 53.16000
• LogP: 0.77
• 外观性状: 固体
• 蒸汽压: 0.0±0.9 mmHg at 25°C
• 折射率: 1.529
• 储存条件: 20°C，惰性气体，避光

生物活性

• 描述: 丙卡巴嗪是一种口服活性烷基化剂,具有抗癌活性。丙卡巴嗪可用于霍奇金病的研究[1][2]。
• 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
• 体外研究: 丙卡巴嗪(5和20 nM；1小时)治疗显示不同浓度的细胞存活[1]。细胞活力测定[1]细胞系：L1210细胞浓度：5和20 nM培养时间：1小时结果：细胞在5 mM和20 mM下分别存活99.3%和99.9%。
• 体内研究: 丙卡巴嗪(腹腔注射；50和150 mg/kg；每天一次；5天)可诱导造血细胞微核,但不会增加骨髓中的lacZ突变频率[2]。动物模型：雄性突变小鼠(7-8周龄)[2]剂量：50和150 mg/kg给药：腹腔注射；50和150 mg/kg；每天一次；5天结果：MN频率明显增加,并在50 mg/kg时观察到外周血微核诱导。
• 参考文献:

  [1]. J M Erikson, et al. Cytotoxicity and DNA damage caused by the azoxy metabolites of procarbazine in L1210 tumor cells. Cancer Res. 1989 Jan 1;49(1):127-33.

  [2]. T Suzuki, et al. Procarbazine genotoxicity in the MutaMouse; strong clastogenicity and organ-specific induction of lacZ mutations. Mutat Res. 1999 Aug 18;444(2):269-81.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : XS4550000 CHEMICAL NAME : p-Toluamide, N-isopropyl-alpha-(2-methylhydrazino)- CAS REGISTRY NUMBER : 671-16-9 LAST UPDATED : 199706 DATA ITEMS CITED : 84 MOLECULAR FORMULA : C12-H19-N3-O MOLECULAR WEIGHT : 221.34 WISWESSER LINE NOTATION : 1Y1&MVR D1MM1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >400 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 350 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 614 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1250 mg/kg/1Y-I TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Gastrointestinal - tumors Kidney, Ureter, Bladder - Kidney tumors TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 125 mg/kg female 22 day(s) after conception TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Reproductive - Tumorigenic effects - transplacental tumorigenesis Brain and Coverings - tumors TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1200 mg/kg/4W-I TOXIC EFFECTS : Tumorigenic - neoplastic by RTECS criteria Lungs, Thorax, or Respiration - tumors TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Primate - monkey DOSE/DURATION : 7 gm/kg/7Y-I TOXIC EFFECTS : Tumorigenic - equivocal tumorigenic agent by RTECS criteria Blood - leukemia TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 540 mg/kg SEX/DURATION : female 13 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 960 mg/kg SEX/DURATION : female 12 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - gastrointestinal system Reproductive - Specific Developmental Abnormalities - homeostasis TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 540 mg/kg SEX/DURATION : female 12 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - urogenital system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 60 mg/kg SEX/DURATION : female 3 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 50 mg/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 200 mg/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 1050 mg/kg SEX/DURATION : male 1-5 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - other effects on male Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 600 mg/kg SEX/DURATION : male 14 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - other effects on male TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intratesticular DOSE : 20 mg/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 53 mg/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 10 mg/kg SEX/DURATION : female 16 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 400 mg/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 200 mg/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 20 mg/kg SEX/DURATION : female 12 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - delayed effects TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 100 mg/kg SEX/DURATION : male 5 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 500 mg/kg SEX/DURATION : male 5 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct TYPE OF TEST : Specific locus test TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Sex chromosome loss and nondisjunction TYPE OF TEST : Sex chromosome loss and nondisjunction TYPE OF TEST : Dominant lethal test TYPE OF TEST : Specific locus test TYPE OF TEST : Morphological transformation TYPE OF TEST : DNA damage TYPE OF TEST : DNA damage TYPE OF TEST : DNA damage TYPE OF TEST : DNA inhibition TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Sperm Morphology TYPE OF TEST : Micronucleus test TYPE OF TEST : Micronucleus test TYPE OF TEST : Micronucleus test TYPE OF TEST : Specific locus test TYPE OF TEST : Specific locus test TYPE OF TEST : Specific locus test TYPE OF TEST : Specific locus test TYPE OF TEST : Specific locus test TYPE OF TEST : Unscheduled DNA synthesis TYPE OF TEST : Mutation test systems - not otherwise specified TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Sister chromatid exchange TYPE OF TEST : Dominant lethal test TYPE OF TEST : Dominant lethal test TYPE OF TEST : Dominant lethal test TYPE OF TEST : Sperm Morphology TYPE OF TEST : Sperm Morphology TYPE OF TEST : Sister chromatid exchange TYPE OF TEST : Sister chromatid exchange TYPE OF TEST : Sister chromatid exchange MUTATION DATA TEST SYSTEM : Rodent - rabbit DOSE/DURATION : 5 mg/kg REFERENCE : ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 46,139,1980 *** REVIEWS *** TOXICOLOGY REVIEW MIMDAL Minnesota Medicine. (Minnesota Medical Assoc., 2221 University Ave., SE, Suite 400, Minneapolis, MN 55414) V.1- 1918- Volume(issue)/page/year: 57,19,1974 TOXICOLOGY REVIEW 32XPAD "Teratology," Berry, C.L., and D.E. Poswillo, eds., New York, Springer, 1975 Volume(issue)/page/year: -,49,1975 TOXICOLOGY REVIEW MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 39,111,1977 TOXICOLOGY REVIEW MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 55,1,1978 TOXICOLOGY REVIEW CRTXB2 CRC Critical Reviews in Toxicology. (CRC Press, Inc., 2000 Corporate Blvd., NW, Boca Raton, FL 33431) V.1- 1971- Volume(issue)/page/year: 2,159,1973 TOXICOLOGY REVIEW BLFSBY Basic Life Sciences. (Plenum Pub. Corp., 223 Spring St., New York, NY 10003) V.1- 1973- Volume(issue)/page/year: 24,129,1983

安全

• 危害码 (欧洲): Xn
• 海关编码: 2928000090

合成路线

58914-41-3 ~% 671-16-9

文献：CH441366 , ; Chem.Abstr., , vol. 69, # 35691

99-75-2 ~% 671-16-9

文献：CH441366 , ; Chem.Abstr., , vol. 69, # 35691

18969-60-3 ~% 671-16-9

文献：CH441366 , ; Chem.Abstr., , vol. 69, # 35691

2417-72-3 ~% 671-16-9

文献：CH441366 , ; Chem.Abstr., , vol. 69, # 35691

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海关

海关编码	2928000090
中文概述	2928000090 其他肼（联氨）及胲（羟胺）的有机衍生物。监管条件:无。增值税率:17.0%。退税率:9.0%。最惠国关税:6.5%。普通关税:20.0%
申报要素	品名, 成分含量, 用途
Summary	2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%