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2894121-83-4

2894121-83-4 Structure

2894121-83-4 Structure
IdentificationBack Directory
[Name]

Eleven-Nineteen-Leukemia Protein IN-3
[CAS]

2894121-83-4
[Synonyms]

Eleven-Nineteen-Leukemia Protein IN-3
Hazard InformationBack Directory
[Uses]

Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro[1].
[in vivo]

Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) (30 mg/kg; p.o.; single dose) shows oral exposure characteristics[1].
Eleven-Nineteen-Leukemia Protein IN-3 (5 mg/kg; i.v.; single dose) highly exposes in vivo[1].
Pharmacokinetic (PK) study in Male BALB/c mice[1]

Administrationt1/2 (h)Tmax (h)Cmax (ng/mL)AUC0-t (h?ng/mL) AUC0-∞ (h?ng/mL)MRT0-∞ (h)
p.o.5.20.571.82572725.5
Administrationt1/2 (h) AUC0-t (h?ng/mL) AUC0-∞ (h?ng/mL)Vss (L/kg) CL (mL/min/kg)MRT0-∞ (h)F (%)
i.v.4.0829086900.89.61.30.5
Animal Model:Male BALB/c mice[1].
Dosage:30 mg/kg.
Administration:Oral gavage; single dose.
Result:Showed an oral activity.
Animal Model:Male BALB/c mice[1].
Dosage:5 mg/kg.
Administration:Intravenous injection; single dose.
Result:Exhibited efficacy.
[IC 50]

Eleven-Nineteen-Leukemia YEATS domain: 15.4 nM (IC50)
[References]

[1] Guo S, et al. Design, synthesis of novel benzimidazole derivatives as ENL inhibitors suppressing leukemia cells viability via downregulating the expression of MYC. Eur J Med Chem. 2023 Feb 15;248:115093. DOI:10.1016/j.ejmech.2023.115093
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