(+-)-A-甲基-4-羧基苯糖胶
(+-)-A-甲基-4-羧基苯糖胶用途
为烷化剂类抗肿瘤药,用于多发性骨髓瘤、乳腺癌、卵巢癌、慢性淋巴细胞和粒细胞型白血病、恶性淋巴瘤、多发性骨髓瘤有效。对动脉灌注治疗肢体恶性肿瘤如恶性黑色素瘤、软组织肉瘤和骨肉瘤有较好的疗效。消旋体对睾丸精原细胞瘤疗效较好。制剂有片剂、注射剂。
(+-)-A-甲基-4-羧基苯糖胶名称
[ CAS 号 ]:
148-82-3
[ 中文名 ]:
美法仑
[ 英文名 ]:
melphalan
[中文别名 ]:
[英文别名 ]:
- 4-[Bis(2-chloroethyl)amino]-L-phenylalanine
- L-3-[p-[Bis(2-chloroethyl)amino]phenyl]alanine
- melphalan
- L-Phenylalanine, 4-(bis(2-chloroethyl)amino)-
- MFCD00057717
- L-Phenylalanine, 4-[bis(2-chloroethyl)amino]-
- Sarcoclorin
- 3025 C.B.
- L-Phenylalanine mustard
- EINECS 205-726-3
(+-)-A-甲基-4-羧基苯糖胶生物活性
[ 描述 ]:
[ 相关类别 ]:
[ 靶点 ]
DNA Alkylator/Crosslinker[1]
[体外研究]
[体内研究]
[细胞实验]
[动物实验]
[参考文献]
[相关活性小分子]
(+-)-A-甲基-4-羧基苯糖胶物理化学性质
[ 密度 ]:
1.3±0.1 g/cm3
[ 沸点 ]:
473.1±45.0 °C at 760 mmHg
[ 熔点 ]:
~180 °C
[ 分子式 ]:
C13H18Cl2N2O2
[ 分子量 ]:
305.200
[ 闪点 ]:
239.9±28.7 °C
[ 精确质量 ]:
304.074524
[ PSA ]:
66.56000
[ LogP ]:
1.79
[ 外观性状 ]:
结晶固体
[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C
[ 折射率 ]:
1.597
[ 储存条件 ]:
-20?C Freezer
[ 水溶解性 ]:
95% ethanol and 1 drop 6 N HCl: 0.05 g/mL, clear | <0.1 g/100 mL at 22 ºC
(+-)-A-甲基-4-羧基苯糖胶毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- AY3675000
- CHEMICAL NAME :
- Alanine, 3-(p-(bis(2-chloroethyl)amino)phenyl)-, L-
- CAS REGISTRY NUMBER :
- 148-82-3
- BEILSTEIN REFERENCE NO. :
- 2816456
- LAST UPDATED :
- 199712
- DATA ITEMS CITED :
- 95
- MOLECULAR FORMULA :
- C13-H18-Cl2-N2-O2
- MOLECULAR WEIGHT :
- 305.23
- WISWESSER LINE NOTATION :
- QVYZ1R DN2G2G -L
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- Rinsed with water
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Rodent - rabbit
- TYPE OF TEST :
- Standard Draize test
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Rodent - rabbit
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 700 mg/kg/7D
- TOXIC EFFECTS :
- Gastrointestinal - nausea or vomiting
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 1200 ug/kg/5D-I
- TOXIC EFFECTS :
- Gastrointestinal - nausea or vomiting
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - child
- DOSE/DURATION :
- 4500 mg/kg
- TOXIC EFFECTS :
- Behavioral - anorexia (human) Gastrointestinal - hypermotility, diarrhea Blood - agranulocytosis
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 8140 mg/kg
- TOXIC EFFECTS :
- Behavioral - anorexia (human) Gastrointestinal - hypermotility, diarrhea Blood - agranulocytosis
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - infant
- DOSE/DURATION :
- 28 mg/kg
- TOXIC EFFECTS :
- Gastrointestinal - hypermotility, diarrhea Blood - agranulocytosis Blood - thrombocytopenia
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 11200 ug/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 - rat
- DOSE/DURATION :
- 4484 ug/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 :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 4100 ug/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 :
- Intracerebral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 200 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD10 - Lethal Dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 32 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 :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 20800 ug/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Blood - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Parenteral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 6 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 - mouse
- DOSE/DURATION :
- 29600 ug/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 3 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Blood - normocytic anemia
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 14 mg/kg/7D-I
- TOXIC EFFECTS :
- Endocrine - changes in spleen weight Immunological Including Allergic - decrease in humoral immune response Nutritional and Gross Metabolic - weight loss or decreased weight gain
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 80 ug/kg/D-C
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - other changes Blood - lymphoma, including Hodgkin's disease
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 57 ug/kg/D-C
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - other changes Blood - lymphoma, including Hodgkin's disease
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 26 mg/kg/2Y-C
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - tumors
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 70 mg/kg/26W-I
- TOXIC EFFECTS :
- Tumorigenic - neoplastic by RTECS criteria Tumorigenic - tumors at site of application
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 58 mg/kg/9W-I
- TOXIC EFFECTS :
- Tumorigenic - equivocal tumorigenic agent by RTECS criteria Lungs, Thorax, or Respiration - tumors Skin and Appendages - tumors
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 60 mg/kg/26W-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Lungs, Thorax, or Respiration - tumors Blood - lymphoma, including Hodgkin's disease
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 15 mg/kg/6W-I
- TOXIC EFFECTS :
- Tumorigenic - neoplastic by RTECS criteria Skin and Appendages - tumors
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 66 mg/kg/4Y-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - leukemia
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 34 mg/kg/2Y-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - leukemia
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 12 mg/kg/3Y-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - leukemia
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 23 mg/kg/2Y-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - leukemia
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 17 mg/kg/4Y-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - leukemia
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 3750 ug/kg
- SEX/DURATION :
- female 25 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - menstrual cycle changes or disorders
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Unreported
- DOSE :
- 8800 ug/kg
- SEX/DURATION :
- female 1 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - other effects
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Unreported
- DOSE :
- 5946 ug/kg
- SEX/DURATION :
- female 1 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - menstrual cycle changes or disorders
- TYPE OF TEST :
- Specific locus test
- TYPE OF TEST :
- Specific locus test
- TYPE OF TEST :
- Sex chromosome loss and nondisjunction
- TYPE OF TEST :
- Micronucleus test
- TYPE OF TEST :
- Specific locus test
- TYPE OF TEST :
- DNA damage
- TYPE OF TEST :
- Unscheduled DNA synthesis
- TYPE OF TEST :
- DNA inhibition
- TYPE OF TEST :
- Sister chromatid exchange
- TYPE OF TEST :
- Dominant lethal test
- TYPE OF TEST :
- Heritable translocation test
MUTATION DATA
- TYPE OF TEST :
- DNA damage
- TEST SYSTEM :
- Mammal - species unspecified Lymphocyte
- DOSE/DURATION :
- 2500 nmol/L
- REFERENCE :
- MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 368,235,1996 *** REVIEWS *** IARC Cancer Review:Human Sufficient Evidence IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,239,1987 IARC Cancer Review:Animal Sufficient 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: 9,167,1975 IARC Cancer Review:Group 1 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,239,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4742 No. of Facilities: 140 (estimated) No. of Industries: 1 No. of Occupations: 4 No. of Employees: 2418 (estimated) No. of Female Employees: 974 (estimated)
(+-)-A-甲基-4-羧基苯糖胶安全信息
[ 符号 ]:
GHS06, GHS08
[ 信号词 ]:
Danger
[ 危害声明 ]:
H300-H310-H330-H350-H361
[ 警示性声明 ]:
P201-P260-P264-P280-P284-P302 + P350
[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
[ 危害码 (欧洲) ]:
T+:Verytoxic;
[ 风险声明 (欧洲) ]:
R45;R46;R26/27/28;R63
[ 安全声明 (欧洲) ]:
S53-S22-S36/37/39-S45
[ 危险品运输编码 ]:
UN 2811 6.1/PG 2
[ WGK德国 ]:
3
[ RTECS号 ]:
AY3675000
[ 包装等级 ]:
II
[ 危险类别 ]:
6.1(a)
[ 海关编码 ]:
2922499990
(+-)-A-甲基-4-羧基苯糖胶合成路线
(+-)-A-甲基-4-羧基苯糖胶上下游产品
(+-)-A-甲基-4-羧基苯糖胶上游产品
(+-)-A-甲基-4-羧基苯糖胶下游产品
(+-)-A-甲基-4-羧基苯糖胶制备
以对硝基溴苄为原料制得。
(+-)-A-甲基-4-羧基苯糖胶海关
[ 海关编码 ]: 2922499990
[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐(含有一种以上含氧基的除外). 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%
[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装
[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单
[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验
[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%
(+-)-A-甲基-4-羧基苯糖胶文献
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Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...
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