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硫酸长春地辛

硫酸长春地辛用途

硫酸长春地辛是一种有效的微管蛋白抑制剂,Ki为0.110µM。硫酸长春地辛在体外具有抗增殖作用。硫酸长春地辛在体内具有抗肿瘤作用[1]。

硫酸长春地辛名称

[ CAS 号 ]:
59917-39-4

[ 中文名 ]:
硫酸长春地辛

[ 英文名 ]:
Vindesine sulfate

[英文别名 ]:

Vindesine Sulfate Salt
Vindesine sulphate

硫酸长春地辛生物活性

[ 描述 ]:

硫酸长春地辛是一种有效的微管蛋白抑制剂,Ki为0.110µM。硫酸长春地辛在体外具有抗增殖作用。硫酸长春地辛在体内具有抗肿瘤作用[1]。

[ 相关类别 ]:

研究领域 >> 癌症

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

[体外研究]

硫酸长春地辛抑制L细胞生长,在40 nM处显示约25%的抑制作用【1】。

[参考文献]

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

硫酸长春地辛物理化学性质

[ 密度 ]:
1.41 g/cm3

[ 熔点 ]:
>250ºC

[ 分子式 ]:
C₄₃H₅₇N₅O₁₁S

[ 分子量 ]:
852.00

[ 精确质量 ]:
851.377502

[ PSA ]:
247.80000

[ LogP ]:
3.80150

[ 外观性状 ]:
非晶形的固体

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
deionized water: ≥50mg/mL

硫酸长春地辛毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YY8090000

CAS REGISTRY NUMBER :: 59917-39-4

LAST UPDATED :: 199706

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C43-H55-N5-O7.H2-O4-S

MOLECULAR WEIGHT :: 852.11

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 :: 1050 ug/kg

TOXIC EFFECTS :: Behavioral - ataxia Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - urine volume increased

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1790 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 :: 1920 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 :: 3500 ug/kg

TOXIC EFFECTS :: Behavioral - ataxia Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - urine volume increased

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6800 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 - mouse

DOSE/DURATION :: 6300 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 :: 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 :: 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 :: Micronucleus test

MUTATION DATA

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

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 28 nmol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 38,2886,1978

硫酸长春地辛安全信息

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R40

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
UN 1544

[ RTECS号 ]:
YY8090000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2942000000

硫酸长春地辛海关

[ 海关编码 ]: 2942000000

硫酸长春地辛文献

Validated HILIC-MS/MS assay for determination of vindesine in human plasma: Application to a population pharmacokinetic study

J. Pharm. Biomed. Anal. 96 , 31-6, (2014)

Mean plasma concentration–time profiles of intravenous injection of 3mg Vindesine Sulfate for Injection to 100 unrelated Chinese Han subjects with hematological malignant disorders.

Young patients with non-germinal center B-cell-like diffuse large B-cell lymphoma benefit from intensified chemotherapy with ACVBP plus rituximab compared with CHOP plus rituximab: analysis of data from the Groupe d'Etudes des Lymphomes de l'Adulte/lymphoma study association phase III trial LNH 03-2B.

J. Clin. Oncol. 32(35) , 3996-4003, (2014)

To determine whether any tumor biomarkers could account for the survival advantage observed in the LNH 03-2B trial among patients with diffuse large B-cell lymphoma (DLBCL) and low-intermediate risk a...

Reovirus cell entry requires functional microtubules.

MBio 4 , (2013)

Mammalian reovirus binds to cell-surface glycans and junctional adhesion molecule A and enters cells by receptor-mediated endocytosis in a process dependent on β1 integrin. Within the endocytic compar...

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