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硫酸长春新碱

硫酸长春新碱用途

Vincristine sulfate是一种抗肿瘤长春花生物碱,抑制有丝分裂纺锤体中的 microtubule 形成,导致中期阶段的分裂细胞停滞。它与 microtubule 结合的 Ki 为85 nM。

硫酸长春新碱名称

[ CAS 号 ]:
2068-78-2

[ 中文名 ]:
硫酸长春新碱

[ 英文名 ]:
Vincristine Sulfate

[中文别名 ]:

[英文别名 ]:

oncovin
VCR
Vincrisul
(2'b)-22-oxovincaleukoblastine sulfate (1:1)
NovopharM
V5 PEPTIDE
kyocristine
(2'β)-22-Oxovincaleukoblastine sulfate (1:1)
22-Oxovincaleukoblastine Sulfate (1:1) (salt)
22-oxovincaleukoblastine sulfate

硫酸长春新碱生物活性

[ 描述 ]:

Vincristine sulfate是一种抗肿瘤长春花生物碱,抑制有丝分裂纺锤体中的 microtubule 形成,导致中期阶段的分裂细胞停滞。它与 microtubule 结合的 Ki 为85 nM。

[ 相关类别 ]:

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

[体外研究]

长春新碱抑制稳态微管组装末端微管蛋白二聚体的净添加,Ki为85 nM [1]。长春新碱稳定心轴装置,导致染色体不能分离,导致中期停滞和低浓度的有丝分裂抑制。在较高浓度下,长春新碱可能会破坏并诱导微管的完全解聚[2]。长春新碱诱导肿瘤细胞凋亡,抑制SH-SY5Y细胞增殖,IC50为0.1μM。长春新碱诱导有丝分裂停滞并促进caspase-3和-9和cyclin B的表达,同时降低cyclin D的表达[3]。长春新碱诱导的神经毒性是由于干扰微管功能引起的,导致轴突运输受阻,从而导致轴突变性[4]。

[体内研究]

长春新碱(3mg/kg,ip)诱导平均生长延迟> 120和> 52天,并且重新填充0.06％和5％的组分,分别在携带双侧皮下异种移植物Rh12或Rh18的小鼠中给药[5]。

[细胞实验]

将细胞以约5×10 4个细胞/ mL的浓度接种在35mm板中的2mL培养基中，并在37℃，5％CO 2和95％空气的气氛中生长24小时。然后用缺乏或含有4nM药物的新鲜培养基替换培养基，并继续增殖3天。在用胰蛋白酶和EDTA分离细胞后，每天在库尔特计数器中进行细胞计数。

[参考文献]

[1]. Jordan, M.A., et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res, 1985. 45(6): p. 2741-7.

[2]. Gidding, C.E., et al, Vincristine revisited. Crit Rev Oncol Hematol, 1999. 29(3): p. 267-87.

[3]. Donoso, J.A., et al, Action of the vinca alkaloids vincristine, vinblastine, and desacetyl vinblastine amide on axonal fibrillar organelles in vitro. Cancer Res, 1977. 37(5): p. 1401-7.

[4]. Horton, J.K., et al. Relationships between tumor responsiveness, vincristine pharmacokinetics and arrest of mitosis in human tumor xenografts. Biochem Pharmacol, 1988. 37(20): p. 3995-4000.

[5]. Baguley, B.C., et al, Inhibition of growth of colon 38 adenocarcinoma by vinblastine and colchicine: evidence for a vascular mechanism. Eur J Cancer, 1991. 27(4): p. 482-7.

[6]. Zhang D, et al. Co-delivery nanoparticles with characteristics of intracellular precision release drugs for overcoming multidrug resistance. Int J Nanomedicine. 2017 Mar 16;12:2081-2108.

[相关活性小分子]

硫酸长春新碱物理化学性质

[ 沸点 ]:
273-281 °C

[ 熔点 ]:
300 °C

[ 分子式 ]:
C₄₆H₅₈N₄O₁₄S

[ 分子量 ]:
923.036

[ 精确质量 ]:
922.367004

[ PSA ]:
254.15000

[ LogP ]:
4.52220

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
>=1 G/100 ML AT 24 ºC

硫酸长春新碱MSDS

详细MSDS(安全技术说明书)

硫酸长春新碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OH6340000

CAS REGISTRY NUMBER :: 2068-78-2

LAST UPDATED :: 199801

DATA ITEMS CITED :: 49

MOLECULAR FORMULA :: C46-H56-N4-O10.H2-O4-S

MOLECULAR WEIGHT :: 923.14

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 :: 1900 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 :: 1010 ug/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - urine volume increased Blood - normocytic anemia

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3 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 :: 1700 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >4 mg/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Gastrointestinal - hypermotility, diarrhea Blood - changes in bone marrow (not otherwise specified)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 4 mg/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Gastrointestinal - hypermotility, diarrhea Blood - changes in bone marrow (not otherwise specified)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Bird - chicken

DOSE/DURATION :: 4 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4500 ug/kg/21D-I

TOXIC EFFECTS :: Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1500 ug/kg/3D-I

TOXIC EFFECTS :: Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1250 ug/kg/33D-I

TOXIC EFFECTS :: Endocrine - other changes Blood - changes in bone marrow (not otherwise specified) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4 mg/kg/4D-I

TOXIC EFFECTS :: Gastrointestinal - alteration in gastric secretion Endocrine - other changes Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 1450 ug/kg/16W-I

TOXIC EFFECTS :: Peripheral Nerve and Sensation - recording from afferent nerve Peripheral Nerve and Sensation - recording from peripheral motor nerve

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 600 ug/kg

SEX/DURATION :: male 15 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands Reproductive - Paternal Effects - other effects on male

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 1250 ug/kg

SEX/DURATION :: male 10 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 250 ug/kg

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

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 300 ug/kg

SEX/DURATION :: female 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

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 - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

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 - Specific Developmental Abnormalities - body wall Reproductive - Specific Developmental Abnormalities - musculoskeletal system 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 :: 250 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 :: 250 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 :: Intravenous

DOSE :: 750 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) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: Sperm Morphology

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Dominant lethal test

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Sex chromosome loss and nondisjunction

MUTATION DATA

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 125 ug/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 379,83,1997 *** 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: 26,365,1981 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: 26,365,1981 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: 7,372,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - M2867 No. of Facilities: 33 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 1452 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M2867 No. of Facilities: 476 (estimated) No. of Industries: 1 No. of Occupations: 8 No. of Employees: 18880 (estimated) No. of Female Employees: 13761 (estimated)

硫酸长春新碱安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H341-H361fd

[ 警示性声明 ]:
Missing Phrase - N15.00950417-P280

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R36/37/38;R61

[ 安全声明 (欧洲) ]:
22-24/25-53-45-37/39-26-36/37/39

[ 危险品运输编码 ]:
UN 2811 6.1/PG 2

[ WGK德国 ]:
3

[ RTECS号 ]:
OH6340000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2942000000

硫酸长春新碱上下游产品

硫酸长春新碱上游产品

硫酸长春新碱下游产品

硫酸长春新碱海关

[ 海关编码 ]: 2942000000

硫酸长春新碱文献

Synergism of arsenic trioxide and MG132 in Raji cells attained by targeting BNIP3, autophagy, and mitochondria with low doses of valproic acid and vincristine.

Eur. J. Cancer 50(18) , 3243-61, (2014)

We previously demonstrated that arsenic trioxide (ATO) and proteasome inhibitor MG132 synergistically induced cell death in promonocytic leukaemia cell line U937 but were antagonistic in Burkitt's lym...

OCT4 mutations in human erythroleukemic cells: implications for multiple drug resistance (MDR) phenotype.

Mol. Cell Biochem. 400(1-2) , 41-50, (2015)

The OCT4 transcription factor is a crucial stem cells marker and it has been related to the cancer stem cells concept. Moreover, it has also been associated to the multiple drug resistance (MDR) pheno...

Curcumin induces apoptosis of multidrug-resistant human leukemia HL60 cells by complex pathways leading to ceramide accumulation.

Biochim. Biophys. Acta 1841(12) , 1672-82, (2015)

Most anti-cancer agents induce apoptosis, however, a development of multidrug resistance in cancer cells and defects in apoptosis contribute often to treatment failure. Here, the mechanism of curcumin...

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