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激动素核苷

激动素核苷用途

Kinetin riboside是细胞分裂素类似物，可诱导癌症细胞死亡。抑制HCT-15细胞增殖的IC₅₀值为2.5 μM。

激动素核苷名称

[ CAS 号 ]:
4338-47-0

[ 中文名 ]:
激动素核苷

[ 英文名 ]:
Kinetin riboside

[中文别名 ]:

[英文别名 ]:

furfuryladenosine
EINECS 224-389-3
Kinetin-9-riboside
MFCD00037987
n-furfuryl-adenosin
Ribosylkinetin
N-Furfuryladenosine

激动素核苷生物活性

[ 描述 ]:

Kinetin riboside是细胞分裂素类似物,可诱导癌症细胞死亡。抑制HCT-15细胞增殖的IC50值为2.5 μM。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

[ 靶点 ]

IC50: 2.5 μM (HCT-15 cells)[1]

[体外研究]

激动素核苷显示针对各种人癌细胞系的抗增殖和凋亡活性。激动素核苷能够以剂量依赖的方式抑制HCT-15人结肠癌细胞的增殖(IC50 =2.5μM)[1]。激动素核苷诱导HeLa和小鼠黑色素瘤B16F-10细胞凋亡。激动素核苷可破坏线粒体膜电位并诱导细胞色素c的释放和胱天蛋白酶-3的活化。坏的是上调,而Bcl-2在激动素核苷暴露下下调[2]。

[体内研究]

激动素核苷显着抑制肿瘤生长。最有效的抗黑色素瘤反应是以40 mg/kg引起的[2]。

[细胞实验]

用5,10,20μM激动素核糖苷处理HeLa和小鼠黑素瘤B16F-10细胞48小时。向每个孔中加入15μLMTT溶液（5mg / mL），并将细胞在37℃下保持4小时。然后加入100微升增溶溶液。在室温下孵育过夜后，测量490nm处的吸光度[2]。

[动物实验]

小鼠：雄性C57BL / 6小鼠注射B16F-10细胞。在肿瘤生长5天后，将激动素核苷（10,20,40mg / kg）直接注射到肿瘤块中。药物注射每3天进行一次，持续三次。在第三次注射药物后，将小鼠保持3天而不注射，并从每只小鼠中取出肿瘤块并称重[2]。

[参考文献]

[1]. Rajabi M, et al. Antiproliferative activity of kinetin riboside on HCT-15 colon cancer cell line. Nucleosides Nucleotides Nucleic Acids. 2012;31(6):474-81.

[2]. Choi BH, et al. Kinetin riboside preferentially induces apoptosis by modulating Bcl-2 family proteins and caspase-3 in cancer cells. Cancer Lett. 2008 Mar 8;261(1):37-45.

[相关活性小分子]

激动素核苷物理化学性质

[ 密度 ]:
1.8±0.1 g/cm3

[ 沸点 ]:
683.7±65.0 °C at 760 mmHg

[ 熔点 ]:
152-154ºC

[ 分子式 ]:
C₁₅H₁₇N₅O₅

[ 分子量 ]:
347.326

[ 闪点 ]:
367.3±34.3 °C

[ 精确质量 ]:
347.122955

[ PSA ]:
138.69000

[ LogP ]:
0.20

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.798

[ 储存条件 ]:
2-8°C

激动素核苷MSDS

激动素核苷毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AU7400200

CHEMICAL NAME :: Adenosine, N-furfuryl-

CAS REGISTRY NUMBER :: 4338-47-0

BEILSTEIN REFERENCE NO. :: 0059588

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C15-H17-N5-O5

MOLECULAR WEIGHT :: 347.37

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

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

TEST SYSTEM :: Human Leukocyte

DOSE/DURATION :: 100 umol/L

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 32,29,1976

激动素核苷安全信息

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

[ 安全声明 (欧洲) ]:
S24/25

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

[ WGK德国 ]:
3

[ RTECS号 ]:
AU7400200

[ 海关编码 ]:
29349990

激动素核苷合成路线

激动素核苷上下游产品

激动素核苷上游产品

激动素核苷下游产品

激动素核苷文献

High-internal-phase-emulsion polymeric monolith coupled with liquid chromatography-electrospray tandem mass spectrometry for enrichment and sensitive detection of trace cytokinins in plant samples.

Anal. Bioanal. Chem 407 , 6071-9, (2015)

High-internal-phase-emulsion polymers (polyHIPEs) show great promise as solid-phase-extraction (SPE) materials because of the tremendous porosity and highly interconnected framework afforded by the hi...

Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity.

Bioorg. Med. Chem. 16 , 3848-65, (2008)

Conformationally constrained analogue synthesis was undertaken to aid in pharmacophore mapping and 3D-QSAR analysis of nitrobenzylmercaptopurine riboside (NBMPR) congeners as equilibriative nucleoside...

Ribose-modified purine nucleosides as ribonucleotide reductase inhibitors. Synthesis, antitumor activity, and molecular modeling of N6-substituted 3'-C-methyladenosine derivatives.

J. Med. Chem. 51 , 4260-9, (2008)

A series of cycloalkyl, bicycloalkyl, aryl, and heteroaryl N (6)-substituted derivatives of the antitumor agent 3'- C-methyladenosine (3'-Me-Ado), an inhibitor of the alpha Rnr1 subunit of mammalian r...

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