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硝呋酚酰肼

硝呋酚酰肼用途

Nifuroxazide 是 STAT3 的有效抑制剂,且具有抗癌和抗转移活性。

硝呋酚酰肼名称

[ CAS 号 ]:
965-52-6

[ 中文名 ]:
硝呋酚酰肼

[ 英文名 ]:
Nifuroxazide

[中文别名 ]:

[英文别名 ]:

Nifuroxazide
Ercefuryl
Diarlidan
Dicoferin
EINECS 213-522-0
Nifuroxazid
Nifuroxazidum
Nifuroxazida
p-hydroxy-N'-(5-nitrofurfurylidene)benzhydrazide
MFCD00079482

硝呋酚酰肼生物活性

[ 描述 ]:

Nifuroxazide 是 STAT3 的有效抑制剂,且具有抗癌和抗转移活性。

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

[ 靶点 ]

STAT3

[体外研究]

当U266细胞与Nifuroxazide一起孵育时,观察到STAT3酪氨酸磷酸化的显着剂量依赖性降低。这种对STAT3酪氨酸磷酸化的抑制是快速的,早在治疗后1小时就发生,并且持续至少24小时。用Nifuroxazide处理U266或INA6细胞48小时导致细胞活力的剂量依赖性丧失,在两种细胞类型中EC50为约4.5μM。值得注意的是,缺乏组成型STAT3活化的MM细胞对Nifuroxazide几乎没有毒性[1]。

[体内研究]

与赋形剂组相比,Nifuroxazide处理可以剂量依赖性地抑制肿瘤生长和肿瘤重量,25mg/kg和50mg/kg时肿瘤体积抑制率分别为43.0％和62.1％。还显示Nifuroxazide显着抑制核Ki-67阳性细胞的增殖并诱导裂解的caspase-3阳性细胞的凋亡细胞。此外,发现用Nifuroxazide治疗可抑制A375肿瘤组织中MMP-2,MMP-9和p-Stat3的表达。此外,Nifuroxazide抑制MDSCs向肺内的浸润,这可能与抑制B16-F10黑色素瘤转移模型中肿瘤细胞的远端定植有关[2]。

[动物实验]

小鼠[2]当肿瘤体积约为100mm 3时，将1×107个A375细胞皮下移植的小鼠随机分成组，并且每天腹膜内注射Nifuroxazide 25mg / kg，50mg / kg或载体一次。每3天测量肿瘤大小和体重。通过尾静脉静脉内注射2×105个B16-F10细胞来植入C57Bl / 6J小鼠，以产生实验性肺转移。在第6天将它们随机分配到组，并且每天一次腹膜内注射Nifuroxazide 50mg / kg或载体。对肺表面的黑点进行计数并确认为黑素瘤转移[2]。

[参考文献]

[1]. Nelson EA, et al. Nifuroxazide inhibits survival of multiple myeloma cells by directly inhibiting STAT3. Blood. 2008 Dec 15;112(13):5095-102.

[2]. Zhu Y, et al. Nifuroxazide exerts potent anti-tumor and anti-metastasis activity in melanoma. Sci Rep. 2016 Feb 2;6:20253.

[相关活性小分子]

硝呋酚酰肼物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 熔点 ]:
281-283°C

[ 分子式 ]:
C₁₂H₉N₃O₅

[ 分子量 ]:
275.217

[ 精确质量 ]:
275.054230

[ PSA ]:
120.65000

[ LogP ]:
0.59

[ 外观性状 ]:
黄色固体

[ 折射率 ]:
1.653

[ 储存条件 ]:
Refrigerator, Under Inert Atmosphere

硝呋酚酰肼毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DH2528300

CHEMICAL NAME :: Benzoic acid, p-hydroxy-, (5-nitrofurfurylidene)hydrazide

CAS REGISTRY NUMBER :: 965-52-6

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C12-H9-N3-O5

MOLECULAR WEIGHT :: 275.24

WISWESSER LINE NOTATION :: T5OJ BNW E1UNMVR DQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6 gm/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 :: 100 mg/kg

TOXIC EFFECTS :: Behavioral - antipsychotic Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - other changes in urine composition

MUTATION DATA

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

TEST SYSTEM :: Bacteria - Escherichia coli

DOSE/DURATION :: 250 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 187,55,1987

硝呋酚酰肼安全信息

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

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
DH2528300

[ 海关编码 ]:
2928000090

硝呋酚酰肼合成路线

详细合成路线

硝呋酚酰肼上下游产品

硝呋酚酰肼上游产品

硝呋酚酰肼下游产品

硝呋酚酰肼海关

[ 海关编码 ]: 2932190090

[ 中文概述 ]:
2932190090 其他结构上有非稠合呋喃环化合物. 增值税率:17.0% 退税率:9.0% 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 ]:
2932190090 other compounds containing an unfused furan ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

硝呋酚酰肼文献

Determination of nitrofuran and chloramphenicol residues by high resolution mass spectrometry versus tandem quadrupole mass spectrometry.

Anal. Chim. Acta 862 , 41-52, (2015)

An ultra-high performance liquid chromatography based method, coupled to high resolution mass spectrometry (UHPLC-HRMS), was developed to permit the detection and quantification of various nitrofuran ...

The transcriptional modulator BCL6 as a molecular target for breast cancer therapy.

Oncogene 34(9) , 1073-82, (2015)

Inappropriate expression or activation of transcription factors can drive patterns of gene expression, leading to the malignant behavior of breast cancer cells. We have found that the transcriptional ...

Genotoxicity of 2-nitro-7-methoxy-naphtho[2,1-b]furan (R7000): a case study with some considerations on nitrofurantoin and nifuroxazide.

Res. Microbiol. 153(7) , 427-34, (2002)

Two nitrofurans present broad-spectrum antimicrobial properties and some of them are used in human and veterinary medicine. Most of these molecules are mutagens and some of them were reported as carci...

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