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UCM05 (Synonyms: G28UCM)

Katalog-Nr.GC15091 Copy One-Click Copy Product Info

UCM05 (G28UCM) ist ein potenter Inhibitor der FettsÄuresynthase (FASN), zeigt AktivitÄt gegen HER2+-Brustkrebs-Xenotransplantate und ist in gegen HER2-Medikamente resistenten Zelllinien aktiv.

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UCM05 Chemische Struktur

Cas No.: 1094451-90-7

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1mg
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5mg
179,00 $
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10mg
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Sample solution is provided at 25 µL, 10mM.



Description of UCM05

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 of UCM05

Cas No. 1094451-90-7 SDF
Überlieferungen G28UCM
Chemical Name 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
Formula C24H16O10 M.Wt 464.4
Löslichkeit ≤12mg/ml in ethanol;5mg/ml in DMSO;10mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of UCM05

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1533 mL 10.7666 mL 21.5332 mL
5 mM 430.7 μL 2.1533 mL 4.3066 mL
10 mM 215.3 μL 1.0767 mL 2.1533 mL
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In vivo Formulation Calculator (Clear solution) of UCM05

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 4 reference(s) in Google Scholar.)

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