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占托西林

占托西林用途

Xanthocillin 是从青霉中提取的一种海洋药剂,通过抑制 MEK/ERK 途径诱导自噬。

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占托西林名称

[ CAS 号 ]:
580-74-5

[ 中文名 ]:
占托西林

[ 英文名 ]:
Xantocillin

[中文别名 ]:

[英文别名 ]:

XANTHOCILLINX
XANTHOCILINX
Brevicide-x
Ophthocillin
Xanthocillin
Xantocillin
Brevicid
Brevicide
Ethylene isocyanide,bis(p-hydroxybenzylidene)
Trianthil

占托西林生物活性

[ 描述 ]:

Xanthocillin 是从青霉中提取的一种海洋药剂,通过抑制 MEK/ERK 途径诱导自噬。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> MAPK/ERK信号通路 >> MEK

信号通路 >> MAPK/ERK信号通路 >> ERK

信号通路 >> 干细胞及 Wnt 通路 >> ERK

[体外研究]

Xantocillin(SD118-xanthocillin X(1))(6.9-55.56μM; 48小时)对HepG2细胞的增殖具有显着的抑制作用,IC50为22.88±4.76μM[1]。 Xantocillin(SD118-xanthocillin X(1))(24.3μM; 12-48小时)增加自噬相关基因LC3和Beclin 1的表达[1]。细胞增殖测定[1]细胞系：HepG2细胞浓度：6.9μM,13.89μM,27.78μM,55.56μM孵育时间：48小时结果：HepG2细胞对细胞生长的浓度依赖性抑制作用,IC50为22.88± 4.76μM。蛋白质印迹分析[1]细胞系：HepG2细胞浓度：24.3μM孵育时间：12小时,24小时,48小时结果：增加自噬相关基因,LC3和Beclin 1的表达。

[参考文献]

[1]. Zhao Y,et al. SD118-xanthocillin X (1), a novel marine agent extracted from Penicillium commune, induces autophagy through the inhibition of the MEK/ERK pathway. Mar Drugs. 2012 Jun;10(6):1345-59.

占托西林物理化学性质

[ 分子式 ]:
C₁₈H₁₂N₂O₂

[ 分子量 ]:
288.30

[ 精确质量 ]:
288.09000

[ PSA ]:
40.46000

[ LogP ]:
2.77980

占托西林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KX1625000

CHEMICAL NAME :: Ethylene isocyanide, bis(p-hydroxybenzylidene)-

CAS REGISTRY NUMBER :: 580-74-5

BEILSTEIN REFERENCE NO. :: 3700094

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C18-H12-N2-O2

MOLECULAR WEIGHT :: 288.32

WISWESSER LINE NOTATION :: QR D1UYNU1&YNU1&U1R DQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 45 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 7,98,1957

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 13500 ug/kg

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

REFERENCE :: PHARAT Pharmazie. (VEB Verlag Volk und Gesundheit, Neue Gruenstr. 18, Berlin DDR-1020, Ger. Dem. Rep.) V.1- 1946- Volume(issue)/page/year: 21,217,1966

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >600 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 7,98,1957

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 9500 ug/kg

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

REFERENCE :: PHARAT Pharmazie. (VEB Verlag Volk und Gesundheit, Neue Gruenstr. 18, Berlin DDR-1020, Ger. Dem. Rep.) V.1- 1946- Volume(issue)/page/year: 21,217,1966