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喜树碱

喜树碱用途

【用途一】
用于治疗胃癌、肠癌、慢性粒细胞型和急性白血病等

【用途二】
抗癌药。用于胃癌、结肠癌、直肠癌、头颈部圆柱瘤型癌和膀胱癌

【用途三】
抗癌药。用于胃癌、结肠癌、直肠癌、头颈部圆柱瘤型癌和膀胱癌

喜树碱名称

[ CAS 号 ]:
7689-03-4

[ 中文名 ]:
喜树碱

[ 英文名 ]:
Campathecin

[中文别名 ]:

[英文别名 ]:

EINECS 444-280-6
Camptothecin
d-Camptothecin
CaMpathecin
(S)-(+)-Camptothecin
Camptohecin
MFCD00081076
Baicalin std.
CAMPTOTHECINE
(+)-Camptothecin

喜树碱生物活性

[ 描述 ]:

Campathecin 是有效的 DNA拓扑异构酶 I 抑制剂,IC50 值为 679 nM。

[ 相关类别 ]:

信号通路 >> 抗体- 药物偶联物 >> ADC细胞毒素

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

研究领域 >> 癌症

[ 靶点 ]

Topoisomerase I:679 nM (IC50)

[体外研究]

[3H]拓扑异构酶I的BrCPT标记由于DNA的存在而大大增强;很少标记分离的拓扑异构酶I或分离的DNA发生者。即使在DNA存在下,拓扑异构酶I的[3H] BrCPT标记也被喜树碱抑制,这表明CPT和BrCPT都与DNA拓扑异构酶I二元复合物上的相同位点结合[1]。随着喜树碱浓度的增加,闭合的环状pRR322 DNA(形式I)被转化为带切口的环状DNA(形式11)。喜树碱的这种明显的切口活性需要DNA拓扑异构酶I [2]。

[激酶实验]

每种反应混合物（200μL，总体积）含有2μg超螺旋pDPT2789 DNA（2.4nM质粒浓度），50mM Tris-HCl，pH 7.5,120mM KCl，10mM MgCl 2,0.5mM EDTA，0.05％二甲基亚砜， 1％甲醇，100μg/ mL BSA，4.3ng小牛胸腺拓扑异构酶I（0.26nM）和CPT衍生物。将反应混合物在37℃温育，并在指定的时间取出20-μL等分试样并通过加入5μLSDS/ Ficoll终止混合物终止（终浓度，0.5％SDS，2％Ficoll，0.025％溴酚）蓝色）。将样品上样到1％琼脂糖凝胶上并通过电泳分析。

[参考文献]

[1]. Hertzberg RP, et al. Irreversible trapping of the DNA-topoisomerase I covalent complex. Affinity labeling of the camptothecin binding site. J Biol Chem. 1990 Nov 5;265(31):19287-95.

[2]. Hsiang YH, et al. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. J Biol Chem. 1985 Nov 25;260(27):14873-8.

[3]. Luzzio MJ, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.

[相关活性小分子]

喜树碱物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
757.0±60.0 °C at 760 mmHg

[ 熔点 ]:
260 °C (dec.)(lit.)

[ 分子式 ]:
C₂₀H₁₆N₂O₄

[ 分子量 ]:
348.352

[ 闪点 ]:
411.6±32.9 °C

[ 精确质量 ]:
348.110992

[ PSA ]:
81.42000

[ LogP ]:
1.60

[ 外观性状 ]:
淡黄色晶体粉末

[ 蒸汽压 ]:
0.0±2.7 mmHg at 25°C

[ 折射率 ]:
1.746

[ 储存条件 ]:
库房低温通风干燥,与食品原料分开存放

[ 水溶解性 ]:
insoluble

喜树碱MSDS

详细MSDS(安全技术说明书)

喜树碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ0492000

CAS REGISTRY NUMBER :: 7689-03-4

LAST UPDATED :: 199706

DATA ITEMS CITED :: 29

MOLECULAR FORMULA :: C20-H16-N2-O4

MOLECULAR WEIGHT :: 348.38

WISWESSER LINE NOTATION :: T F6 D6 C566 BN HVO LVN NHT&&&&J GQ G2

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 :: 50100 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 64 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 38 mg/kg

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

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Primate - monkey Kidney

DOSE/DURATION :: 25 umol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 48,1722,1988

喜树碱安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
Missing Phrase - N15.00950417

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
S45-S36/37/39-S26

[ 危险品运输编码 ]:
UN 1544 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
UQ0492000

喜树碱合成路线

详细合成路线

喜树碱上下游产品

喜树碱上游产品

喜树碱下游产品

喜树碱制备

本品是由珙桐科旱莲属植物喜树的根、皮、果实提取制得的生物碱。也可合成生产。将喜树果粗粉用10倍量80%乙醇浸泡24小时，收集渗漉液，减压浓缩回收乙醇。浓缩液静置取清液，用氯仿提取，提取液蒸馏回收氯仿至干，再加甲醇溶液，冷却过滤，滤饼为喜树碱粗品，粗品用甲醇-氯仿混合溶剂重结晶，得喜树碱。对生药喜树果汁，总收率0.03-0.04%.

喜树碱文献

TAp73 promotes cell survival upon genotoxic stress by inhibiting p53 activity.

Oncotarget 5(18) , 8107-22, (2014)

p53 plays a key role in regulating DNA damage response by suppressing cell cycle progression or inducing apoptosis depending on extent of DNA damage. However, it is not clear why mild genotoxic stress...

DNA damage-specific deubiquitination regulates Rad18 functions to suppress mutagenesis.

J. Cell Biol. 206(2) , 183-97, (2014)

Deoxyribonucleic acid (DNA) lesions encountered during replication are often bypassed using DNA damage tolerance (DDT) pathways to avoid prolonged fork stalling and allow for completion of DNA replica...

A dihydroselenoquinazoline inhibits S6 ribosomal protein signalling, induces apoptosis and inhibits autophagy in MCF-7 cells.

Eur. J. Pharm. Sci. 63 , 87-95, (2014)

The PI3K/Akt/mTOR/S6 ribosomal protein signalling pathway is a key potential target in breast cancer therapy, playing a central role in proliferation and cell survival. In this study, we found that th...

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喜树碱