| Identification | Back Directory | [Name]
Benzamide, N-[2-(4-ethoxyphenoxy)phenyl]-4-[[(1-oxo-2-propen-1-yl)amino]methyl]- | [CAS]
1197824-15-9 | [Synonyms]
EN4 MYC inhibitor
Benzamide, N-[2-(4-ethoxyphenoxy)phenyl]-4-[[(1-oxo-2-propen-1-yl)amino]methyl]- | [Molecular Formula]
C25H24N2O4 | [MDL Number]
MFCD13582116 | [MOL File]
1197824-15-9.mol | [Molecular Weight]
416.47 |
| Chemical Properties | Back Directory | [Boiling point ]
564.1±50.0 °C(Predicted) | [density ]
1.202±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 250 mg/mL (600.28 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.82±0.70(Predicted) | [color ]
White to light yellow | [InChI]
1S/C25H24N2O4/c1-3-24(28)26-17-18-9-11-19(12-10-18)25(29)27-22-7-5-6-8-23(22)31-21-15-13-20(14-16-21)30-4-2/h3,5-16H,1,4,17H2,2H3,(H,26,28)(H,27,29) | [InChIKey]
DKOWGKKELPCHEG-UHFFFAOYSA-N | [SMILES]
O=C(C1=CC=C(CNC(C=C)=O)C=C1)NC2=C(OC3=CC=C(OCC)C=C3)C=CC=C2 |
| Hazard Information | Back Directory | [Uses]
EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis[1]. | [Biological Activity]
EN4 is a cell penetrantpotent and selective covalent c-MYC inhibitor th at targets cysteine 171 located within a predicted intrinsically disordered region of MYC. EN4 inhibits MYC transcriptional activitydownregulates multiple MYC transcriptional targetsreduces MYC and MAX thermal stabilityand impairs tumorigenesis. | [in vivo]
EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment significantly attenuated tumor growth in 231MFP breast tumor xenograft mice[1]. | Animal Model: | SCID mice injected with 231MFP breast cancer cells[1] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; daily; for 3 weeks | | Result: | Significantly attenuated tumor growth in vivo. |
| [References]
[1] Lydia Boike, et al. Discovery of a Functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC. Cell Chem Biol. 2021 Jan 21;28(1):4-13.e17. DOI:10.1016/j.chembiol.2020.09.001 |
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