AF9/ENL-DOT1L PPI-IN-1
AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent AF9/ENL and histone methyltransferase DOT1L/AF4 protein-protein interactions (PPI) inhibitor. AF9/ENL-DOT1L/AF4 PPI-IN-1 can inhibit the AF9-DOT1L (IC50 = 1.5 μM), AF9-AF4 (IC50 = 1 μM), ENL-AF4 (IC50 = 1.2 μM) interactions. AF9/ENL-DOT1L/AF4 PPI-IN-1 can suppress the expression of Mixed lineage leukemia (MLL) target genes Myc and Meis1 and selectively block the proliferation of MLL-r and several other leukemia cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 exhibits significant antitumor activities in a mouse model of MLL-r leukemia without overt toxicities. AF9/ENL-DOT1L/AF4 PPI-IN-1 can be used for the study of MLL-r leukemia.
For research use only. We do not sell to patients.
- Formula: C26H26ClFN4O2
- Molecular Weight:480.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
AF9/ENL-DOT1L/AF4 PPI-IN-1 (0-1μM, 3 days) significantly decreases the mRNA levels of Myc and Meis1 in a generally concentration-dependent manner in Molm-13 cells[1].
AF9/ENL-DOT1L/AF4 PPI-IN-1 can effectively and selectively inhibit a panel of cancer cells, including MV4-11 (EC50 = 0.96 μM), Molm-13 (EC50 = 1.6 μM), NB4 (EC50 = 2.7 μM), HL-60 (EC50 = 0.66 μM), Kasumi (EC50 = 0.92 μM), Jurkat (EC50 = 0.77 μM), and shows negligible antiproliferative activities against solid tumor HeLa cells(EC50 ＞ 30 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Molm-13 cells
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Concentration:0 μM, 0.3 μM, 1μM
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Incubation Time:72 h
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Result:Significantly decreased the mRNA levels of Myc and Meis1 in a generally concentration-dependent manner in Molm-13 cells.
AF9/ENL-DOT1L/AF4 PPI-IN-1 (50 mg/kg, i.p., 0.5-24 h) has a favorable PK with a satisfactory plasma drug exposure and a long half-life of > 40 h in NOD-SCID mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:106 Molm-13 cells were injected subcutaneously into 6−8 weeks old NOD-SCID mice[1].
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Dosage:1-3 days, 50 mg/kg, twice daily
4-14 days, 25 mg/kg, twice daily -
Administration:I.p.
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Result:Significantly inhibited tumor growth in mice by 65%.
After 24 h, its plasma concentration was 1.7 μM, which is well above the EC50 values of AF9/ENL-DOT1L/AF4 PPI-IN-1 against the two MLL-r leukemia cells.
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Animal Model:NOD-SCID mice.
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Dosage:50 mg/kg
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Administration:I.p.
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Result:Exhibited a favorable PK profile with the maximal plasma concentration of 3.1 μM and a half-life of > 40 h.
Chemical Information
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Molecular Weight 480.96
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Formula C26H26ClFN4O2
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SMILES
FC1=CC=C(OC2=CC=C(NC3=CC=C4N=CC(OCC5CCNCC5)=NC4=C3)C=C2)C=C1.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AF9/ENL-DOT1L PPI-IN-1 Related Classifications
HY-178172 Related Classifications
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