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硫酸长春碱

硫酸长春碱用途

Vinblastine sulfate是一种针对各种癌症类型的有细胞毒性的生物碱。长春花碱可抑制微管的形成,抑制nAChR的IC50值为8.9 μM。

硫酸长春碱名称

[ CAS 号 ]:
143-67-9

[ 中文名 ]:
硫酸长春碱

[ 英文名 ]:
Vinblastine Sulfate

[中文别名 ]:

硫酸长春花碱

[英文别名 ]:

vinbalastine
Velsar
EINECS 205-606-0
Vincaleukoblastine, (2'β)-, sulfate (1:1)
VLB
velbe
velban
Vinblastine-d3
(2'β)-Vincaleukoblastine sulfate (1:1)
Periblastine

硫酸长春碱生物活性

[ 描述 ]:

Vinblastine sulfate是一种针对各种癌症类型的有细胞毒性的生物碱。长春花碱可抑制微管的形成,抑制nAChR的IC50值为8.9 μM。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白

信号通路 >> 细胞骨架 >> 微管/微管蛋白

天然产物 >> 生物碱

研究领域 >> 癌症

[ 靶点 ]

IC50: 8.9 μM(nAChR)[1]

[体外研究]

长春碱不会使纺锤体微管解聚,但它有效阻断有丝分裂(例如,HeLa细胞中IC50为0.8 nM),细胞死于细胞凋亡[2]。在NB4细胞中,长春碱产生p53和DNA片段化的改变。长春碱治疗通过诱导细胞凋亡产生Bax/Bcl-2失衡具有抗增殖作用。长春碱处理抑制NFκB表达并抑制NFκB-DNA结合活性,同时维持JNK活化,随后通过半胱天冬酶依赖性途径导致细胞凋亡反应[3]。发现长春碱诱导细胞凋亡,如线粒体膜电位的丧失,细胞色素c和细胞凋亡诱导因子的释放,caspase-9和3的激活以及Poly(ADP-核糖)聚合酶的裂解所证明[4]。

[体内研究]

长春碱是一种广泛使用的抗癌药物,具有不良副作用。它与载体分子的结合可能是减少这些副作用的有效策略[5]。

[参考文献]

[1]. McKay DB, et al. Nicotinic and nonnicotinic receptor-mediated actions of vinblastine. Proc Soc Exp Biol Med. 1993 Jul;203(3):372-6.

[2]. Pandya P, et al. Molecular recognition pattern of cytotoxic alkaloid vinblastine with multiple targets. J Mol Graph Model. 2014 Nov;54:1-9.

[3]. Calviño E, et al. JNK and NFκB dependence of apoptosis induced by vinblastine in human acute promyelocytic leukaemia cells. Cell Biochem Funct. 2015 Jun;33(4):211-9.

[4]. Selimovic D, et al. Vinblastine-induced apoptosis of melanoma cells is mediated by Ras homologous A protein (Rho A) via mitochondrial and non-mitochondrial-dependent mechanisms. Apoptosis. 2013 Aug;18(8):980-97.

[5]. Bánóczi Z, et al. Synthesis and in vitro antitumor effect of vinblastine derivative-oligoarginine conjugates. Bioconjug Chem. 2010 Nov 17;21(11):1948-55.

[相关活性小分子]

硫酸长春碱物理化学性质

[ 密度 ]:
1.37 g/cm3

[ 熔点 ]:
267 °C (dec.)(lit.)

[ 分子式 ]:
C₄₆H₆₀N₄O₁₃S

[ 分子量 ]:
909.053

[ 精确质量 ]:
908.387756

[ PSA ]:
237.08000

[ LogP ]:
4.35970

[ 外观性状 ]:
白色粉末

[ 储存条件 ]:
2~8°C

[ 水溶解性 ]:
>=1 g/100 mL at 24.5 ºC

硫酸长春碱MSDS

详细MSDS(安全技术说明书)

硫酸长春碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YY8400000

CAS REGISTRY NUMBER :: 143-67-9

LAST UPDATED :: 199806

DATA ITEMS CITED :: 52

MOLECULAR FORMULA :: C46-H58-N4-O9.H2-O4-S

MOLECULAR WEIGHT :: 909.16

WISWESSER LINE NOTATION :: T C6 B5665/BS 2AB S BX IN QN NU&&TTTJ FO1 I1 KVO1 KQ LOV1 M2 E- CT F6 D596 A EN ON&&TTJ CVO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 557 ug/kg

TOXIC EFFECTS :: Blood - leukopenia Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 305 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 - rat

DOSE/DURATION :: 1 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 355 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 - rat

DOSE/DURATION :: 37 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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 423 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 :: 2700 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 324 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 :: 9500 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 :: 500 ug/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Gastrointestinal - hypermotility, diarrhea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 4300 ug/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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3 mg/kg/15D-I

TOXIC EFFECTS :: Gastrointestinal - other changes Blood - leukopenia Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 500 ug/kg/5D-I

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 125 ug/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - body wall

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 125 ug/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 350 ug/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - body wall Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 250 ug/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 50 ug/kg

SEX/DURATION :: female 9 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 :: 350 ug/kg

SEX/DURATION :: female 9 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 :: Subcutaneous

DOSE :: 10 mg/kg

SEX/DURATION :: female 11-14 day(s) after conception

TOXIC EFFECTS :: 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 :: Intravenous

DOSE :: 500 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 1 mg/kg

SEX/DURATION :: female 1 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - other effects to embryo

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: DNA inhibition

TYPE OF TEST :: Sperm Morphology

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Sperm Morphology

MUTATION DATA

TEST SYSTEM :: Rodent - hamster

DOSE/DURATION :: 24 ug/kg

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 327,237,1995 *** 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: 26,349,1981 IARC Cancer Review:Human 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: 26,349,1981 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,371,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 83934 No. of Facilities: 33 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 1386 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 83934 No. of Facilities: 273 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 14022 (estimated) No. of Female Employees: 10067 (estimated)

硫酸长春碱安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H315-H318-H335

[ 警示性声明 ]:
P280-P301 + P312 + P330-P305 + P351 + P338 + P310

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R22;R36/37/38;R41;R61

[ 安全声明 (欧洲) ]:
26-36/39-53-45-37/39-36/37/39

[ 危险品运输编码 ]:
1544

[ WGK德国 ]:
3

[ RTECS号 ]:
YY8400000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2942000000

硫酸长春碱上下游产品

硫酸长春碱上游产品

硫酸长春碱下游产品

硫酸长春碱海关

[ 海关编码 ]: 2942000000

硫酸长春碱文献

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

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...

Developing structure-activity relationships for the prediction of hepatotoxicity.

Chem. Res. Toxicol. 23 , 1215-22, (2010)

Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals ...

A predictive ligand-based Bayesian model for human drug-induced liver injury.

Drug Metab. Dispos. 38 , 2302-8, (2010)

Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predicti...

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