UCM05 (Synonyms: G28UCM) |
| Catalog No.GC15091 |
UCM05(G28UCM)는 FASN(지방산 합성효소)의 강력한 억제제로 HER2+ 유방암 이종이식에 대한 활성을 나타내며 항-HER2 약물 내성 세포주에서 활성입니다.
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Cas No.: 1094451-90-7
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 1094451-90-7 | SDF | |
| Synonyms | 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 |
| Solubility | ≤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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 ddH2O, 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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