2894121-83-4

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]

Administration	t_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_0-t (h?ng/mL)	AUC_0-∞ (h?ng/mL)	MRT_0-∞ (h)
p.o.	5.2	0.5	71.8	257	272	5.5
Administration	t_1/2 (h)	AUC_0-t (h?ng/mL)	AUC_0-∞ (h?ng/mL)	V_ss (L/kg)	CL (mL/min/kg)	MRT_0-∞ (h)	F (%)
i.v.	4.0	8290	8690	0.8	9.6	1.3	0.5

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

Hazard Information

Uses

in vivo

IC 50

References

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