Chemical Structure : ML234
CAS No.:
ML234
(ML-234)
Catalog No.: PC-22960Not For Human Use, Lab Use Only.
ML234 is a potent EZH2/LSD1 dual inhibitor with IC50 of 0.09/0.12 uM respectively, shows excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3, and 22RV1.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ML234 is a potent EZH2/LSD1 dual inhibitor with IC50 of 0.09/0.12 uM respectively, shows excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3, and 22RV1.
ML234 accumulates H3K4me2 and H3K9me2 and decreases H3K27me3 in prostate cancer cells.
ML234 weakly inhibits LSD2 and MAO-A.
ML234 shows anticancer activity in all three prostate cancer cell lines (GI50s at 3.96, 1.04, and 1.63 μM).
ML234 inhibits cell migration in prostate cancer cells via a potential EMT intervention.
ML234 (80 mg/kg) daily significantly suppressed tumor volume by a tumor growth inhibitory rate (TGI) of 52.2% in 22RV1 tumor xenograft model.
Physicochemical Properties
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M.Wt
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726.96
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Formula
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C43H58N4O6
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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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(±)-trans-tert-Butyl(2-(3'-(((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-5'-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4'-methyl-[1,1'-biphenyl]-4-yl)cyclopropyl)((tetrahydro-2H-pyran-4-yl)methyl)carbamate
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References
1. Meiling Le, et al. Journal of Medicinal Chemistry, August 28, 2024
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