EED-IN-3
EED-IN-3 is an orally active EED inhibitor. EED-IN-3 effectively inhibits PRC2 by binding to EED (IC50 = 0.62 μM for EED) and downregulates H3K27me3. EED-IN-3 can efficiently and selectively inhibit PC3 cells with the IC50 of 3.69 μΜ and could significantly suppress colony formation and migration. EED-IN-3 can be used for research on prostate cancer.
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- CAS No.: 3051817-48-9
- Formule: C25H29N3O5
- Masse moléculaire:451.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
EED-IN-3 (Compound 39) (7 days) exhibits highly selective anticancer activity against PC3 cells and low toxicity against normal cells, including PC3 (IC50 = 3.69 μM), EC109 (IC50 = 26.8 μM), KYSE150 (IC50 = 24.53 μM) and PC9 (IC50 = 18.43 μM)[1].
EED-IN-3 (0-16 μM) significantly reduce the level of H3K27me3 in PC3 cells[1].
EED-IN-3 (0-16 μM, 24 or 48 h) can inhibit PC3 cell migration and invasion in a time-and concentration dependent manner[1].
EED-IN-3 (8-16 μM, 12 days) significantly inhibits the formation of cell colonies in PC3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 cells
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Concentration:3 μM or 6 μM
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Incubation Time:4 days
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Result:Effectively upregulated the expression of E-Cadherin and downregulated the expression of N-Cadherin.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 2.23 h | 1.50 h | 20.0 ng/mL | 73.8 ng·h/mL | 81.3 ng·h/mL | 2.66 h | 3.42 h |
EED-IN-3 (50 mg/kg-100 mg/kg; i.g.; once daily; for 14 days) has a significant inhibitory effect on tumor growth in the PC3 cells injected BALB/C-nu mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 wild-type mice (8-12 weeks)[1]
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Dosage:Single dose 2 g/kg
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Administration:Oral gavage (i.g.)
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Result:Did not cause any abnormal weight changes and did not cause histopathological changes in important organs.
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Animal Model:1×107 PC3 cells injected the BALB/C-nu mice[1]
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Dosage:50 mg/kg or 100 mg/kg
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Administration:Oral gavage (i.g.); once daily for 14 days
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Result:Inhibited tumor growth by nearly 50% in the 50 mg/kg/day group and nearly 80 % in the 100 mg/kg/day group, steadily increased body weight.
Chemical Information
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CAS No. 3051817-48-9
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Masse moléculaire 451.51
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Formule C25H29N3O5
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SMILES
COC1=CC=C(C=C1)C2=NN(C(C(C(NCCCOC(C)C)=O)=C2)=O)C3=CC=C(C=C3)OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EED-IN-3 Related Classifications
HY-174397 Related Classifications
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