| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
In breast cancer cells, FR054 (0.5–1 mM, 24-48 h) causes an early growth arrest, which is followed by a marked rise in cell death and the induction of apoptosis. Instead of having additional off-target effects, FR054 inhibits PGM3 [1]. N- and O-glycosylation levels in MDA-MB-231 cells are effectively impacted by FR054 (250 μM, 24 hours) treatment [1]. Endoplasmic reticulum (ER) stress and ROS-dependent apoptosis are induced by FR054 [1].
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|---|---|
| ln Vivo |
In MDA-MB-231 xenograft mice, FR054 (1000 mg/kg, i.p.) suppresses the growth of cancer [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MDA-MB-231 cells. Tested Concentrations: 0.5-1 mM. Incubation Duration: 48 h. Experimental Results: decreased viability and a significant increase of the apoptosis as compared to the control clone. |
| Animal Protocol |
Animal/Disease Models: Mice were subcutaneously (sc) injected with MDA-MB-231 cells[1].
Doses: 1000 mg/kg. Route of Administration: IP, single or fractionated dose (twice a day 500 mg/kg/dose). Experimental Results: Appears to have an in vivo antitumor efficacy that is higher when administered twice a day compared to single administration. |
| References |
[1]. Francesca Ricciardiello, et al. Inhibition of the Hexosamine Biosynthetic Pathway by Targeting PGM3 Causes Breast Cancer Growth Arrest and Apoptosis. Cell Death Dis. 2018 Mar 7;9(3):377.
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| Molecular Formula |
C14H19NO8
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|---|---|
| Molecular Weight |
329.3026
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| Exact Mass |
329.11
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| Elemental Analysis |
C, 51.06; H, 5.82; N, 4.25; O, 38.87
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| CAS # |
10378-06-0
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| Related CAS # |
FR054;35954-65-5
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| Appearance |
semi-solid or waxy solid or viscous solid
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| SMILES |
O1[C@@]2([H])[C@@]([H])(C([H])(C([H])(C1([H])C([H])([H])OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)N=C(C([H])([H])[H])O2
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| Synonyms |
6R-FR054; 6R-FR-054; 6R-FR 054;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~303.67 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0367 mL | 15.1837 mL | 30.3674 mL | |
| 5 mM | 0.6073 mL | 3.0367 mL | 6.0735 mL | |
| 10 mM | 0.3037 mL | 1.5184 mL | 3.0367 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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