FR054

Research use only, not for human use.

FR054 is an inhibitor of the Hexosamine Biosynthetic Pathway (HBP) enzyme PGM3, with a remarkable anti-breast cancer effect. FR054 induces in different breast cancer cells a dramatic decrease in cell proliferation and survival.

FR054 is an inhibitor of the Hexosamine Biosynthetic Pathway (HBP) enzyme PGM3, with a remarkable anti-breast cancer effect. FR054 induces in different breast cancer cells a dramatic decrease in cell proliferation and survival.(In Vivo):The effect of FR054 occurs through PGM3 inhibition instead of other off-target effects. FR054 (0.5-1 mM, 24-48 h) induces an early proliferation arrest followed by a marked cell death increase in breast cancer cells and induces apoptosis. FR054 (250?μM, 24 h) treatment efficiently affects both N- and O-glycosylation levels in MDA-MB-231 cells. FR054 induces endoplasmic reticulum stress and ROS-dependent apoptotic cell death .

Cell Viability Assay Cell Line:MDA-MB-231 cells.Concentration:0.5-1?mM.Incubation Time:48 h.Result:Reduced viability and a significant increase of the apoptosis as compared to the control clone.

Animal Model:Mice were subcutaneously injected with MDA-MB-231 cells.Dosage:1000?mg/kg.Administration:IP, single or fractionated dose (twice a day 500?mg/kg/dose).Result:Appears to have an in vivo antitumor efficacy that is higher when administered twice a day compared to single administration.

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Others

Other Targets

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35954-65-5

657.6

C28H37N2O16

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (303.67 mM)

CC(OC[C@H]([C@H]1OC(C)=O)O[C@@H]2OC(C)=N[C@@H]2[C@H]1OC(C)=O)=OCC(OC[C@H]([C@H]1OC(C)=O)O[C@@H]2OC(C)=N[C@@H]2[C@H]1OC(C)=O)=O

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(-20℃)

With Ice Pack

≥ 2 years