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Monastrol Sale

(Synonyms: (±)-Monastrol) 目录号 : GC14929

Reversible inhibitor of the motor protein Eg5

Monastrol Chemical Structure

Cas No.:254753-54-3;329689-23-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥357.00
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10mg
¥672.00
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50mg
¥3,045.00
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500mg
¥13,230.00
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1g
¥18,690.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

The cytotoxicity assay is performed with MTT. Cells are seeded in 96-well culture plates (5000 cells/well) and incubated for 24 h for stabilization. After this period, the following treatments are administered for 24 and 48 h: vehicle control (0.5 % DMSO); 1 μM doxorubicin and monastrol at 5, 25, 50, 75, and 100 μM. After each time of treatment, the medium is withdrawn, serum-free media containing 0.5 mg/mL MTT salt is added and incubated for 4 h, and formazan crystal products are diluted[2].

References:

[1]. Cochran JC, et al. Monastrol inhibition of the mitotic kinesin Eg5. J BiolChem. 2005 Apr 1;280(13):12658-67.
[2]. Mayer TU, et al. Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science. 1999 Oct 29;286(5441):971-4.
[3]. Marques LA, et al. Antiproliferative activity of monastrol in human adenocarcinoma (MCF-7) and non-tumor (HB4a) breast cells. Naunyn Schmiedebergs Arch Pharmacol. 2016 Dec;389(12):1279-1288.

产品描述

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.

References:
[1] Kapoor TM,Mayer TU,Coughlin ML,Mitchison TJ.  Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5. J Cell Biol.2000 Sep 4;150(5):975-88.
[2] Torres BG,Ucha Fde T,Pigatto MC,Azeredo FJ,Haas SE,Dallegrave E,Canto RF,Eifler-Lima VL,Dalla Costa T.  Pre-clinical pharmacokinetics and acute toxicological evaluation of a monastrol derivative anticancer candidate LaSOM 65 in rats. Xenobiotica.2014 Mar;44(3):254-63.

Chemical Properties

Cas No. 254753-54-3;329689-23-8 SDF
别名 (±)-Monastrol
化学名 ethyl 6-(3-hydroxyphenyl)-2-mercapto-4-methyl-1,6-dihydropyrimidine-5-carboxylate
Canonical SMILES CCOC(C(C1C2=CC(O)=CC=C2)=C(N=C(S)N1)C)=O
分子式 C14H16N2O3S 分子量 292.35
溶解度 ≥ 29.2mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.4206 mL 17.1028 mL 34.2056 mL
5 mM 0.6841 mL 3.4206 mL 6.8411 mL
10 mM 0.3421 mL 1.7103 mL 3.4206 mL
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