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Monastrol

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产品名称: Monastrol
产品型号: GOY-Y2997
产品展商: 谷研
产品文档: 无相关文档
发布时间:2023-05-04

简单介绍

Monastrol≥ 29.2mg/mL in DMSO


Monastrol  的详细介绍

性能参数

产品名称

Monastrol

规格

10mM (in 1mL DMSO) 10mg 50mg 500mg 1g

货号

GOY-Y2997

 含量

>98.00%

CAS

254753-54-3

别名

(±)-Monastrol

 

 

化学名

ethyl 6-(3-hydroxyphenyl)-2-mercapto-4-methyl-1,6-dihydropyrimidine-5-carboxylate

分子式

C14H16N2O3S

分子量

分子量 292.35

溶解度

≥ 29.2mg/mL in DMSO

储存条件

Store at -20°C

General tips

 

用途

仅供科研

价格

电询

详细内容

IC50: 14 μM

Monastrol is a cell-permeable small molecule inhibitor of the mitotic kinesin, Eg5. Like other kinesins, Eg5 can drive the movement of microtubules in vitro.

In vitro: Previous study found that monastrol did not inhibit progression through S and G2 phases of the cell cycle or centrosome duplication. The mitotic arrest due to monastrol was also reversible rapidly. Chromosomes in monastrol-treated cells frequently had both sister kinetochores attached to microtubules extending to the center of the monoaster. Monastrol also inhibited bipolar spindle formation in Xenopus egg extracts, however, monastrol did not prevent the targeting of Eg5 to the monoastral spindles that form [1].

In vivo: Previous study investigated the rat PK and TK of LaSOM 65, a monastrol derivative. Results showed that LaSOM 65 had good bioavailability and linear PK after oral doses. LaSOM 65 distributed consistently in lung and fatty tissues. Other investigated tissues presented smaller penetration ratios. Adverse symptoms were observed only after iv administration, and regressed 3 h after dosing. No statistical differences were found for serum analysis, body weight and relative organ weight, indicating no acute toxicological effects. [2].

Clinical trial: Up to now, LaSOM 65 is still in the preclinical development stage.

 

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