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UCM05

(Synonyms: G28UCM) 目录号 : GC15091

A fatty acid synthase inhibitor

UCM05 Chemical Structure

Cas No.:1094451-90-7

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1mg
¥254.00
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5mg
¥927.00
现货
10mg
¥1,576.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 21 μmol/L for SK-Br3 cells

UCM05 is a fatty acid synthase inhibitor.

Fatty acid synthase, a lipogenic enzyme, catalyzes the de novo synthesis of long-chain fatty acids from malonyl-CoA, acetyl-CoA, and NADPH precursors.

In vitro: In SK-Br3 cells, UCM05 was the most potent derivative with an IC50 value of 21 μmol/L. SK-Br3 cells also showed inhibitary effects towards for MCF-7, and MDA-MB-231 with IC50 values of 46, and 79 μmol/L, respectively. Moreover, the cytotoxic effects of UCM05 was determined in two types of nonmalignant cells, and no significant effects in cell death or morphology was observed using doses up to 60 μmol/L. In addition, the FASN activity decreased time-dependently and the maximal inhibition at 24 hours were 90% for UCM05. Incubation of cells with 30 μmol/L of UCM05 could dramatically decrease the levels of p-HER2 [1].

In vivo: In the BT474 xenograft-bearing mice, the six informative UCM05–treated animals substantially reduced tumor growth when compared with the vehicle-treated control animals. Moreover, one of the UCM05-treated animals had no identifiable residual tumor and one of them died due to traumatic i.p. injections. In addition, no significant weight loss or anorexia was observed after 45 days of treatment [1].

Clinical trial: Up to now, UCM05 is still in the preclinical development stage.

Reference:
[1] T.  Puig, C. Turrado, B. Benhamú, et al. Novel inhibitors of fatty acid synthase with anticancer activity. Clinical Cancer Research 15(24), 7608-7615 (2009).

Chemical Properties

Cas No. 1094451-90-7 SDF
别名 G28UCM
化学名 3,4,5-trihydr3,​4,​5-​trihydroxy-benzoic acid 1,​1'-​(1,​3-​naphthalenediyl) ester
Canonical SMILES OC1=C(O)C(O)=CC(C(OC2=CC(C=CC=C3)=C3C(OC(C4=CC(O)=C(O)C(O)=C4)=O)=C2)=O)=C1
分子式 C24H16O10 分子量 464.4
溶解度 ≤12mg/ml in ethanol;5mg/ml in DMSO;10mg/ml in dimethyl formamide 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 2.1533 mL 10.7666 mL 21.5332 mL
5 mM 0.4307 mL 2.1533 mL 4.3066 mL
10 mM 0.2153 mL 1.0767 mL 2.1533 mL
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