EP102
EP102 is an orally active, selective inhibitor of the METTL3/METTL14 complex with an IC50 of 2 nM. EP102 reduces intracellular N6-methyladenosine levels, inhibits cancer cell proliferation, and thereby suppresses tumor growth in mouse models. EP102 is applicable for the research of acute myeloid leukemia, ovarian solid tumors and advanced solid tumors.
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- No. CAS: 3050818-07-7
- Fòrmula: C27H32N6OS
- Peso molecular:488.65
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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CYP3A4 0.9 nM (IC50) |
CYP3A5 16 nM (IC50) |
EP102 (72 h) inhibits the viability of Kasumi-1, MV-4-11, Calu-6, A549, FaDu, SK-OV-3, and Caov-3 human cancer cell lines with IC50 values ranging from 31 nM to 225 nM[1].
EP102 inhibits intracellular m6A levels in Kasumi-1, MV-4-11, Calu-6, A549, FaDu, and SK-OV-3 human cancer cell lines with IC50 values ranging from 6 nM to 19 nM[1].
EP102 exhibits metabolic stability in rat, minipig, and human liver microsomes with half-lives of 149 min, 44 min, and 53 min, respectively[1].
EP102 selectively inhibits human CYP3A4 with an IC50 of 0.9 μM and CYP3A5 with an IC50 of 16 μM, while not significantly inhibiting the other 8 tested major human CYPs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Kasumi-1, MV-4-11, Calu-6, A549, FaDu, and SK-OV-3 human cancer cell lines
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Concentration:IC50
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Incubation Time:/
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Result:Downregulated the intracellular m6A levels in with IC50 values ranging from 6 nM to 19 nM.
EP102 (47 mg/kg; p.o.; TIW; 32 days) achieves >90% tumor growth inhibition and reduces metastasis in an intraovarian mouse xenograft model of ovarian cancer when dosed orally at 47 mg/kg three times weekly[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice with Acute myeloid leukemia (AML) (female; disseminated xenograft model via intravenous injection of 2 × 10^6 MV-4-11-Luc-mCh-Puro cells)[1]
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Dosage:20 mg/kg; 47 mg/kg
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Administration:p.o.; QD (20 mg/kg), TIW (47 mg/kg); 4 weeks
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Result:Restricted AML tumor spread as shown by bioluminescence imaging with both dosing regimens.
Reduced levels of hCD45+ human AML cells in bone marrow with both dosing regimens.
Showed no depletion of mouse mCD45+ cells.
Demonstrated superior efficacy with the 47 mg/kg TIW regimen compared to the 20 mg/kg QD regimen.
Maintained stable body weights in treated mice, indicating well-tolerated treatment.
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Animal Model:Balb/c mice with Ovarian cancer (female; intraovarian xenograft model via implant of SK-OV-3-Luc cells)[1]
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Dosage:47 mg/kg
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Administration:p.o.; TIW; 32 days
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Result:Achieved >90% tumor growth inhibition (TGI) relative to vehicle controls over the 32-day treatment period via bioluminescence measurement.
Reduced metastasis in the intestines, an effect not observed with the positive control Olaparib.
Maintained stable body weights in treated mice and showed no macroscopic adverse events, indicating well-tolerated treatment.
Chemical Information
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No. CAS 3050818-07-7
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Peso molecular 488.65
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Fòrmula C27H32N6OS
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SMILES
C1(C2(COC2)C3=NN=C(C4=CC(C5CC5)=CN=C4)S3)=NC=C(N6CCC[C@@H](NCC7CC7)C6)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EP102 Related Classifications
HY-183186 Related Classifications
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