Eleven-Nineteen-Leukemia Protein IN-3

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Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
Email: marketing@targetmol.cn
Company Name: TargetMol Chemicals Inc.  
Tel: 13564774135
Email: marketing@targetmol.com

Eleven-Nineteen-Leukemia Protein IN-3 manufacturers
Eleven-Nineteen-Leukemia Protein IN-3 Basic information
Product Name:Eleven-Nineteen-Leukemia Protein IN-3
Synonyms:Eleven-Nineteen-Leukemia Protein IN-3;2-Phenanthridinecarboxamide, 5,6-dihydro-5-methyl-N-[2-[[(2S)-2-methyl-1-pyrrolidinyl]methyl]-1H-benzimidazol-6-yl]-6-oxo-
CAS:2894121-83-4
MF:C28H27N5O2
MW:465.55
EINECS:
Product Categories:
Mol File:2894121-83-4.mol
Eleven-Nineteen-Leukemia Protein IN-3 Structure
Eleven-Nineteen-Leukemia Protein IN-3 Chemical Properties
Boiling point 694.064±55.00 °C(Press: 760.00 Torr)(predicted)
density 1.342±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
pka10.866±0.10(predicted)
Safety Information
MSDS Information
Eleven-Nineteen-Leukemia Protein IN-3 Usage And Synthesis
UsesEleven-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 (hng/mL) AUC0-∞ (hng/mL)MRT0-∞ (h)
p.o.5.20.571.82572725.5
Administrationt1/2 (h) AUC0-t (hng/mL) AUC0-∞ (hng/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 50Eleven-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
Eleven-Nineteen-Leukemia Protein IN-3 Preparation Products And Raw materials
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