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盐酸柔红霉素

盐酸柔红霉素用途

Daunorubicin hydrochloride是具有有效抗肿瘤活性的DNA拓扑异构酶II抑制剂。

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盐酸柔红霉素名称

[ CAS 号 ]:
23541-50-6

[ 中文名 ]:
柔红霉素盐酸盐

[ 英文名 ]:
Daunorubicin HCl

[中文别名 ]:

[英文别名 ]:

DAUNOBLASTINE
Daunorubicin hydrochloride
daunoblastin
Daunorubicin HCl
Daunorubicin (Hydrochloride)
Daunoblastina
Rubidomycin hydrochloride
Cerubidine
ndc0082-4155
Daunomycin, monohydrochloride

盐酸柔红霉素生物活性

[ 描述 ]:

Daunorubicin hydrochloride是具有有效抗肿瘤活性的DNA拓扑异构酶II抑制剂。

[ 相关类别 ]:

信号通路 >> 抗体- 药物偶联物 >> ADC细胞毒素

信号通路 >> 自噬 >> 自噬

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

天然产物 >> 醌类

研究领域 >> 癌症

[ 靶点 ]

Topoisomerase II

[体外研究]

Molt-4细胞中柔红霉素(Dnr)的平均IC50值为0.04μM。柔红霉素属于蒽环霉素,一组细胞毒性化学治疗剂。蒽环霉素的细胞毒性作用是由DNA插入和通过抑制拓扑异构酶II以及产生活性氧来干扰DNA转录和复制的能力引起的[2]柔红霉素抑制HeLa细胞中DNA和RNA合成的浓度范围0.2至2μM。对于人胰腺细胞系L3.6中的柔红霉素(Dnr),IC50值为0.4μM[3]。

[体内研究]

与对照组相比,柔红霉素组(3mg/kg,iv)中尿蛋白排泄,血清肌酐和血尿素氮(BUN)水平显着增加。与对照组相比,柔红霉素(DNR)的施用导致肾组织中丙二醛(MDA)水平显着增加[4]。

[细胞实验]

使用MTT测定评估对柔红霉素的化学敏感性。简而言之，96孔板设置有初始密度为2×105个细胞/ mL的细胞，并在不存在和存在9种不同浓度的不同浓度的存在下，在5％CO 2的气氛中在37℃下孵育72小时。柔红霉素（Dnr）或Dox的范围为1.90至0.007μM，一式三份。温育后，向每个孔中加入10μLMTT溶液（5mg / mL四唑盐），并将板在37℃下再温育4小时。通过在10mM HCl溶液中加入100μL10％SDS溶解甲crystals盐晶体并在37℃下温育过夜。通过96孔酶联免疫吸附测定（ELISA）读板仪在540nm处用参比在650nm处测量吸光度。化学敏感性表示为IC 50，其是与没有药物生长的对照细胞相比引起50％细胞存活的药物浓度。使用Microsoft Excel [2]进行计算。

[动物实验]

大鼠[4]使用8周龄雄性Sprague-Dawley大鼠。在开始实验之前，将动物隔离并使其适应另外2周。在第0天，每只动物以3mg / kg的剂量接受单次静脉内注射柔红霉素（iv）。柔红霉素以48小时的间隔以三次相等的注射给药，持续一周，以达到9mg / kg的累积剂量，这充分证明产生心脏毒性和肾毒性。向年龄匹配的大鼠注射相应体积的0.9％NaCl并用作对照（组对照; n = 5）。将22只DNR处理的大鼠随机分成两组，口服替米沙坦（10mg / kg /天;柔红霉素+替米沙坦组; n = 10）或载体（柔红霉素组; n = 12）。替米沙坦的剂量是根据之前的报告选择的。替米沙坦的给药在与柔红霉素给药的同一天开始，并在停止使用柔红霉素后持续另外5周（总共6周）。该研究期限是根据以前的报告选择的。在第41天，将大鼠单独置于代谢笼中以进行24小时尿液收集以测量蛋白质浓度并测量体重（BW）。在研究期结束后（6周），处死大鼠并收获肾组织用于半定量免疫印迹和免疫组织化学研究。

[参考文献]

[1]. Lehmann M, et al. Activity of topoisomerase inhibitors daunorubicin, idarubicin, and aclarubicin in the Drosophila Somatic Mutation and Recombination Test. Environ Mol Mutagen. 2004;43(4):250-7.

[2]. Svensson SP, et al. Melanin inhibits cytotoxic effects of Doxorubicin and Daunorubicin in MOLT 4 cells. Pigment Cell Res. 2003 Aug;16(4):351-4

[3]. Gervasoni JE Jr, et al. An effective in vitro antitumor response against human pancreatic carcinoma with paclitaxel and Daunorubicin by induction of both necrosis and apoptosis. Anticancer Res. 2004 Sep-Oct;24(5A):2617-26

[4]. Arozal W, et al. Telmisartan prevents the progression of renal injury in daunorubicin rats with the alteration of angiotensin II and endothelin-1 receptor expression associated with its PPAR-γ agonist actions. Toxicology. 2011 Jan 11;279(1-3):91-9.

[相关活性小分子]

盐酸柔红霉素物理化学性质

[ 沸点 ]:
770ºC at 760 mmHg

[ 熔点 ]:
188 - 190ºC

[ 分子式 ]:
C₂₇H₃₀ClNO₁₀

[ 分子量 ]:
563.981

[ 闪点 ]:
419.5ºC

[ 精确质量 ]:
563.155823

[ PSA ]:
185.84000

[ LogP ]:
2.53120

[ 外观性状 ]:
橙色-红色粉末

[ 蒸汽压 ]:
6.99E-26mmHg at 25°C

[ 储存条件 ]:
0-10°C;存放于惰性气体之中;避免湿气 (吸湿),加热

[ 水溶解性 ]:
水溶性：可溶；可溶于：甲醇；不溶：苯,氯仿,乙醚

盐酸柔红霉素MSDS

详细MSDS(安全技术说明书)

盐酸柔红霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HB7878000

CHEMICAL NAME :: Daunomycin, hydrochloride

CAS REGISTRY NUMBER :: 23541-50-6

LAST UPDATED :: 199806

DATA ITEMS CITED :: 27

MOLECULAR FORMULA :: C27-H29-N-O10.Cl-H

MOLECULAR WEIGHT :: 564.03

WISWESSER LINE NOTATION :: L E6 C666 BV MVT&&&J DQ HV1 HQ KQ RO1 FO- FT6OTJ B1 CQ DZ &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 290 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 :: 14300 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 - rat

DOSE/DURATION :: 33200 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 :: 14300 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 :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 27900 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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 205 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 :: 3050 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 :: 28800 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 :: 50 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 :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 23300 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 :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 375 mg/kg/5D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 11500 ug/kg/5D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg/5D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 43500 ug/kg/5D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: Specific locus test

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Rodent - mouse Liver

DOSE/DURATION :: 17 mg/L

REFERENCE :: AMOKAG Acta Medicia Okayama. (Okayama Univ. Medical School, Okayama, Japan) V.27 1973- Volume(issue)/page/year: 33,149,1979 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4586 No. of Facilities: 49 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 881 (estimated) No. of Female Employees: 459 (estimated)

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盐酸柔红霉素安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H334-H351

[ 警示性声明 ]:
P261-P281-P301 + P310-P342 + P311

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R40;R42/43

[ 安全声明 (欧洲) ]:
S22-S36/37-S45

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

[ RTECS号 ]:
HB7878000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2932999099

盐酸柔红霉素合成路线

详细合成路线

盐酸柔红霉素上下游产品

盐酸柔红霉素上游产品

盐酸柔红霉素下游产品

盐酸柔红霉素海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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