FTO-IN-16
FTO-IN-16 (Compound 8a-1), a FTO-IN-15 (HY-179266) prodrug, is a potent FTO inhibitor. FTO-IN-16 suppresses acute myeloid leukemia (AML) cell viability, increases m6A levels, downregulates c-Myc and CEBPA, and upregulates ASB2 and RARA. FTO-IN-16 induces apoptosis. FTO-IN-16 demonstrates strong in vivo efficacy in AML mouse xenografts. FTO-IN-16 can be used for the research of AML.
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- Formule: C23H23Cl2N3O6
- Masse moléculaire:508.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
FTO-IN-16 (0-8 μM; 48 h) downregulates c-Myc and CEBPA (protein and mRNA), and upregulates ASB2 and RARA in multiple AML cells (NB4, MOLM13, MV4-11, HEL, OCI-AML3, NOMO-1, KG-1)[1].
FTO-IN-16 (0-20 μM; 48 h) induces dose-dependent apoptosis in NB4 cells[1].
FTO-IN-16 (0-8 μM; 48 h) downregulates c-Myc and CEBPA (protein and mRNA), and upregulates ASB2 and RARA in multiple AML cells (NB4, MOLM13, MV4-11, HEL, OCI-AML3, NOMO-1, KG-1)[1].
FTO-IN-16 (72 h) exhibits potent antileukemic activity across a panel of AML cell lines, with IC50 values of 5.5 (NB4), 2.3 (MOLM13), 4.4 (KG-1), 3.6 (MV4-11), 4.6 (HEL), 5.2 (OCI-AML3), and 4.7 μM (NOMO-1), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM13
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Concentration:0, 2, 4, 8 μM
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Incubation Time:24, 48, 72 h
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Result:Induced time-dependent growth inhibition. Significantly inhibited cell growth after 72 h treatment at 8 μM compared to the control.
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Cell Line:NB4
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Concentration:0, 1, 2, 4 μM
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Incubation Time:7 days
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Result:Induced dose-dependent suppression of colony formation.
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Cell Line:NB4
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Concentration:0, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Induced dose-dependent apoptosis.
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Cell Line:NB4, MOLM13, MV4-11, HEL, OCI-AML3, NOMO-1, KG-1
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Concentration:0, 2, 4, 8 μM
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Incubation Time:48 h
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Result:Upregulated tumor suppressors RARA and ASB2. Reduced protein levels of the oncoproteins CEBPA and c-Myc. The downregulation of c-Myc protein was consistently observed across 7 tested AML cell lines. Did not alter the protein levels of FTO itself or other major m6A regulators, including ALKBH5 and METTL3.
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Cell Line:NB4
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Concentration:0, 4, 8 μM
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Incubation Time:48 h
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Result:Increased ASB2 expression accompanied by decreased c-Myc and CEBPA transcripts.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice subcutaneously injected with NB4 AML cells[1]
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Dosage:30 and 60 mg/kg
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Administration:i.p.; daily for 9 days
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Result:Significantly suppressed tumor growth in a dose-dependent manner. Showed no significant body weight loss or organ toxicity. Resulted in upregulation of tumor suppressors (RARA, ASB2) and downregulation of oncoproteins (CEBPA, c-Myc). Showed a marked increase in global RNA m6A modifications.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- CCK-8/WST-8 Cell Proliferation Assay
- MTT Cell Proliferation Assay
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Masse moléculaire 508.35
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Formule C23H23Cl2N3O6
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SMILES
O=C(C1=CC=CC=C1NC2=C(C=C(C=C2Cl)C(NCCNC(/C=C/C(OCC)=O)=O)=O)Cl)OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FTO-IN-16 Related Classifications
HY-179267 Related Classifications
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