2. Epigenetics Metabolic Enzyme/Protease
  3. METTL3 Cytochrome P450
  4. 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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EP102

EP102 Chemical Structure

CAS No. : 3050818-07-7

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EP102 Related Antibodies

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View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Description

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[1].

IC50 & Target[1]

CYP3A4

0.9 nM (IC50)

CYP3A5

16 nM (IC50)

In Vitro

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.

EP102 Related Antibodies

Real Time qPCR[1]

Cell Line: Kasumi-1, MV-4-11, Calu-6, A549, FaDu, and SK-OV-3 human cancer cell lines
Concentration: IC50
Incubation Time: /
Result: Downregulated the intracellular m6A levels in with IC50 values ranging from 6 nM to 19 nM.
In Vivo

EP102 (20-47 mg/kg; p.o.; QD, TIW; 4 weeks) inhibits AML tumor growth in a disseminated mouse xenograft model, with superior efficacy observed with a 47 mg/kg oral three-times-weekly dose compared to a 20 mg/kg oral daily dose[1].
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.

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]
Dosage: 20 mg/kg; 47 mg/kg
Administration: p.o.; QD (20 mg/kg), TIW (47 mg/kg); 4 weeks
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.
Animal Model: Balb/c mice with Ovarian cancer (female; intraovarian xenograft model via implant of SK-OV-3-Luc cells)[1]
Dosage: 47 mg/kg
Administration: p.o.; TIW; 32 days
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.
Molecular Weight

488.65

Formula

C27H32N6OS
CAS No.
SMILES

C1(C2(COC2)C3=NN=C(C4=CC(C5CC5)=CN=C4)S3)=NC=C(N6CCC[C@@H](NCC7CC7)C6)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EP102 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EP1023050818-07-7EP 102EP-102METTL3Cytochrome P450Methyltransferase-like 3CYPsMETTL3/METTL14 complexadvanced solid tumorsN6-methyladenosineMV-4-11ovarian solid tumorsKasumi-1acute myeloid leukemiaA549FaDuCalu-6Inhibitorinhibitorinhibit

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