Chemical Structure : EP102
CAS No.:
3050818-07-7
EP102
(EP-102)
Catalog No.: PC-26542Not For Human Use, Lab Use Only.
EP102 is a potent, selective METTL3 inhibitor with IC50 of 2 nM in SPA primary assay.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
EP102 is a potent, selective METTL3 inhibitor with IC50 of 2 nM in SPA primary assay.
EP102 showed nanomolar potency across a broad panel of cancer cell lines (Kasumi-1 (IC50=61 nM) and MV-4-11 (AML), Calu-6 and A549 (lung), FaDu (head and neck), and Caov-3 and SK-OV-3 (ovarian)).
EP102 potently inhibits intracellular m6A in SK-OV-3 cells with IC50 of 6 nM,.
EP102 selectively inhibits METTL3/14 among a panel of 40 methyl transferases.
EP102 demonstrated a dose-dependent inhibition of m6A up to a maximum reduction (79%) following a single dose of 3 mg/kg (oral) in PBMCs from rats.
EP102 (20 mg/kg, po, QD) inhibited tumor growth in AML xenograft model (MV-4-11-Luc-mCh-Puro CDX model).
Physicochemical Properties
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M.Wt
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488.65
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Formula
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C27H32N6OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-N-(Cyclopropylmethyl)-1-(6-(3-(5-(5-cyclopropylpyridin-3-yl)-1,3,4-thiadiazol-2-yl)oxetan-3-yl)pyridin-3-yl)piperidin-3-amine
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References
1. Dutheuil G, et al. J Med Chem. 2026 Apr 13. doi: 10.1021/acs.jmedchem.6c00474.
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