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71486-22-1生产厂家

71486-22-1价格

71486-22-1

71486-22-1结构式
71486-22-1结构式

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中文名 长春瑞宾
英文名 vinorelbine
中文别名 长春瑞滨
英文别名 Methyl (2β,3β,4β,5α,12β,19α)-4-acetoxy-15-[(12S)-16-ethyl-12-(methoxycarbonyl)-1,10-diazatetracyclo[12.3.1.0.0]octadeca-3(11),4,6,8,15-pentaen-12-yl]-3-hydroxy-16-methoxy-1-methyl-6,7-didehydroaspidospermidine-3-carboxylate
8-methylsulfanyl-5-nonylsulfanyl-quinoline
aspidospermidine-3-carboxylic acid, 4-(acetyloxy)-6,7-didehydro-15-[(8S)-4-ethyl-1,3,6,7,8,9-hexahydro-8-(methoxycarbonyl)-2,6-methano-2H-azecino[4,3-b]indol-8-yl]-3-hydroxy-16-methoxy-1-methyl-, methyl ester, (2β,3β,4β,5α,12β,19α)-
vinorebline
3',4'-didehydro-4'-desoxy-8'-norvincaleucoblastine
5-Nonylthio-8-methylthio-chinolin
5'-noranhydrovinblastine
vinorelbene
Methyl (2β,3β,4β,5α,12β,19α)-4-acetoxy-15-[(12S)-16-ethyl-12-(methoxycarbonyl)-1,10-diazatetracyclo[12.3.1.0.0]octadeca-3(11),4,6,8,15-pentaen-12-yl]-3-hydroxy-16-methox y-1-methyl-6,7-didehydroaspidospermidine-3-carboxylate
Quinoline,8-(methylthio)-5-(nonylthio)
Vinorelbine
Aspidospermidine-3-carboxylic acid, 4-(acetyloxy)-6,7-didehydro-15-[(8S)-4-ethyl-1,3,6,7,8,9-hexahydro-8-(methoxycarbonyl)-2,6-methano-2H-azecino[4,3-b]indol-8-yl]-3-hydroxy-16-methoxy-1-methyl-, meth ;yl ester, (2β,3β,4β,5α,12β,19α)-
描述 Vinorelbine(KW-2307 base)是抗有丝分裂剂,能抑制Hela细胞增殖,IC50为1.25 nM。
相关类别
体外研究 长春瑞滨(0.5-5nM)在浓度为1.25nM时抑制细胞增殖50%(IC50)。浓度为8 nM的长春瑞滨时,没有细胞处于后期[1]。长春瑞滨时间依赖性地诱导雄激素依赖性(AD)和非依赖性(AI)前列腺癌细胞系中的p53和p21WAFI/CIP1表达。长春瑞滨以浓度依赖性方式刺激报告基因[2]。
体内研究 长春瑞滨治疗后,第一次中性粒细胞过多发生在狗的第一次(4只狗),第二次(1)或第六次(1)长春瑞滨治疗后[3]。长春瑞滨在携带肿瘤的猫中每周耐受一次,MTD为11.5 mg/m2 [4]。
动物实验 根据该研究的定义,将VRL1在0.9%NaCl中稀释至1.5mg / mL的浓度,并在5分钟内进行IV。预期的治疗间隔为7天,最多4次治疗。在每周接受4次剂量后,猫有资格每2周继续接受VRL治疗,费用由所有者承担。
参考文献

[1]. Ngan VK, et al. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001 Jul;60(1):225-32.

[2]. Liu XM, et al. Unique induction of p21(WAF1/CIP1)expression by vinorelbine in androgen-independent prostate cancer cells. Br J Cancer. 2003 Oct 20;89(8):1566-73.

[3]. Poirier VJ, et al. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9.

[4]. Pierro JA, et al. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013 Jul-Aug;27(4):943-8.

密度 1.4±0.1 g/cm3
分子式 C45H54N4O8
分子量 778.932
精确质量 778.394165
PSA 133.87000
LogP 4.69
折射率 1.676
储存条件 2-8C
稳定性

二酒石酸长春瑞滨(Vinordbine Ditartrate): C45H54N4O8?2C4H6O6。黄白色无定形粉末。溶于水或乙醇。

分子结构

1、 摩尔折射率:214.24

2、 摩尔体积(cm3/mol):569.7

3、 等张比容(90.2K):1643.1

4、 表面张力(dyne/cm):69.1

5、 极化率(10-24cm3):84.93

更多

1.比旋光度:[α]D20+52.4°(C=0.3,氯仿)。

2.UV最大吸收(乙醇):215,268,282,293,310nm(ε 3700,11000,9500,7600,4400)。

CHEMICAL IDENTIFICATION

RTECS NUMBER :
RD2530000
CHEMICAL NAME :
C'-Norvincaleukoblastine, 3',4'-didehydro-4'-deoxy-
CAS REGISTRY NUMBER :
71486-22-1
LAST UPDATED :
199706
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C45-H54-N4-O8
MOLECULAR WEIGHT :
779.03

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
26 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
GTKRDX Gan to Kagaku Ryoho. Cancer and Chemotherapy. (1-8-9 Yaesu, Chuo-ku, Tokyo 103, Japan) V.1- 1974- Volume(issue)/page/year: 10,1050,1983

~79%

71486-22-1结构式

71486-22-1

文献:Gueritte; Pouilhes; Mangeney; et al. European Journal of Medicinal Chemistry, 1983 , vol. 18, # 5 p. 419 - 424

~77%

71486-22-1结构式

71486-22-1

文献:Gueritte; Pouilhes; Mangeney; et al. European Journal of Medicinal Chemistry, 1983 , vol. 18, # 5 p. 419 - 424

~76%

71486-22-1结构式

71486-22-1

文献:European Journal of Medicinal Chemistry, , vol. 18, # 5 p. 419 - 424

~%

71486-22-1结构式

71486-22-1

文献:European Journal of Medicinal Chemistry, , vol. 18, # 5 p. 419 - 424
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由脱水长春碱(Anhydmvinblastine)经1步或2步反应得到长春瑞滨,收率有所提高。71486-22-1 preparation