< 生产厂家价格 >

棘霉素

棘霉素用途

Echinomycin (Quinomycin A) 是一种有效的,细胞渗透性的低氧诱导因子-1 (HIF-1) DNA 结合活性的小分子抑制剂。Echinomycin 选择性抑制癌症干细胞,其 IC50 值为 29.4 pM。

点击显示

棘霉素名称

[ CAS 号 ]:
512-64-1

[ 中文名 ]:
棘霉素

[ 英文名 ]:
Echinomycin

[英文别名 ]:

echinomycin
quinomycin-A

棘霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

[体外研究]

棘霉素(0-10nM；16小时；U251细胞)处理以剂量依赖性方式显着抑制缺氧诱导的VEGF mRNA表达。棘霉素以剂量依赖性方式非常有效地抑制U251-HRE中荧光素酶表达的缺氧诱导,EC50为1.2 nM[1]。RT-PCR[1]细胞系：U251细胞浓度：0 nM,0.625 nM,1.25 nM,5 nM,10 nM孵育时间：16小时结果：以剂量依赖性方式显着抑制缺氧诱导的VEGF mRNA表达。

[体内研究]

棘霉素(10μg/kg；静脉注射；40天；NOD-SCID小鼠)治疗通过优先消除癌症干细胞(CSC)在异种模型中有效根除小鼠淋巴瘤和可连续移植的人急性髓性白血病(AML)。HIF1α通过抑制Notch途径中的负反馈环来维持小鼠淋巴瘤CSC[2]。动物模型：NOD-SCID小鼠接受1.8Gy照射并静脉注射来自患者AML-71和AML-150的外周血细胞[2]剂量：10μg/kg给药：静脉注射；40天结果：有效根除通过优先消除CSC在异种模型中的小鼠淋巴瘤和可连续移植的人AML。

[参考文献]

[1]. Kong D, et al. Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity. Cancer Res. 2005 Oct 1;65(19):9047-55.

[2]. Wang Y, et al. Targeting HIF1α eliminates cancer stem cells in hematological malignancies. Cell Stem Cell. 2011 Apr 8;8(4):399-411.

棘霉素物理化学性质

[ 密度 ]:
1.41 g/cm3

[ 沸点 ]:
1427.2ºC at 760 mmHg

[ 分子式 ]:
C₅₁H₆₄N₁₂O₁₂S₂

[ 分子量 ]:
1101.26000

[ 闪点 ]:
817ºC

[ 精确质量 ]:
1100.42000

[ PSA ]:
352.40000

[ LogP ]:
1.82630

[ 折射率 ]:
1.536

[ 储存条件 ]:
-20°C，干燥，密封

棘霉素MSDS

详细MSDS(安全技术说明书)

棘霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: JW5250000

CHEMICAL NAME :: Echinomycin

CAS REGISTRY NUMBER :: 512-64-1

BEILSTEIN REFERENCE NO. :: 0078671

LAST UPDATED :: 199712

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C51-H64-N12-O12-S2

MOLECULAR WEIGHT :: 1101.39

WISWESSER LINE NOTATION :: T C-16-6-16-/CE& A B C- C-- 2CP E& AS CX C-S DNV GMV KOV NNV PXNV TMV A&OV D&NVTJ D1

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 :: 280 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 :: 3800 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 :: 629 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Skin and Appendages - hair

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 89 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Gastrointestinal - nausea or vomiting

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Mammal - species unspecified Lymphocyte

DOSE/DURATION :: 27 umol/L

REFERENCE :: HXPHAU Handbuch der Experimentellen Pharmakologie. (Berlin, Ger.) New series: V.1-49, 1935-78. For publisher information, see HEPHD2. Volume(issue)/page/year: 38(Pt 2),623,1975

点击显示

棘霉素安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301 + H311 + H331-H361

[ 警示性声明 ]:
P261-P280-P301 + P310-P311

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R46

[ 安全声明 (欧洲) ]:
53-36/37/39-45

[ 危险品运输编码 ]:
UN 3462 6.1/PG 2

[ WGK德国 ]:
3

[ RTECS号 ]:
JW5250000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

棘霉素文献

Regulatory effect of hypoxia-inducible factor-1α on hCG-stimulated endothelin-2 expression in granulosa cells from the PMSG-treated rat ovary.

J. Reprod. Dev. 58(6) , 678-84, (2012)

Endothelin (ET)-2 plays a crucial role in ovarian ovulation in mammals. The present study was designed to test the hypothesis that hypoxia-inducible factor (HIF)-1α-mediated transcriptional activation...

Interaction of an echinomycin-DNA complex with manganese ions.

Acta Crystallogr. Sect. F Struct. Biol. Cryst. Commun. 65(Pt 7) , 660-4, (2009)

The crystal structure of an echinomycin-d(ACGTACGT) duplex interacting with manganese(II) was solved by Mn-SAD using in-house data and refined to 1.1 A resolution against synchrotron data. This comple...

Effects of echinomycin on endothelin-2 expression and ovulation in immature rats primed with gonadotropins.

Exp. Mol. Med. 44(10) , 615-21, (2012)

Echinomycin is a small-molecule inhibitor of hypoxia- inducible factor-1 DNA-binding activity, which plays a crucial role in ovarian ovulation in mammalians. The present study was designed to test the...

更多文献

棘霉素