A2073
A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways. A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.
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- No. CAS: 2834742-70-8
- Fòrmula: C33H37NO7
- Peso molecular:559.65
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
A2073 (25-100 nM, 24-72 h) significantly inhibites the proliferation of HEL and K562 cells in a dose- and time-dependent manner, with IC50 values of 55.02 nM (HEL) and 77.07 nM (K562)[1].
A2073 (25-100 nM, 24-72 h) reduces HEL cell numbers without significantly increasing apoptosis, induces erythroid differentiation in HEL cells as evidenced by increased CD71 expression, and causes cell cycle arrest while downregulating key cell cycle regulatory proteins[1].
A2073 (25-100 nM, 48 h) downregulates key proteins in the MAPK (RAS, RAF, MAPK, MEK), PI3K-AKT (PI3K, AKT), and NF-κB (p-NF-κB, p-IκBα) pathways[1].
A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEL cells
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Concentration:/
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Incubation Time:72 h
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Result:Reduced HEL cell numbers more effectively than Cytarabine (Ara-C) (HY-13605), with a lower IC50 (55.02 nM vs. 73.36 nM)
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Cell Line:HEL cells
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Concentration:100 nM
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Incubation Time:48 h
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Result:Increased the expression levels of erythroid differentiation markers GATA1, EKLF, SHIP1, and NFE2.
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Cell Line:HEL cells
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Concentration:25, 50, 100 nM
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Incubation Time:24, 48, 72 h
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Result:Caused cell cycle arrest in the G0 and G2 phases, reduces the proportion of cells in the S phase.
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Cell Line:HEL cells
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Concentration:25, 50, 100 nM
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Incubation Time:48 h
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Result:Downregulatesd key cell cycle regulatory proteins including CMYC, CDK1, CDK2, CCNB1, and CCNA2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CM-Dil dye-labeled HEL cells into zebrafish embryos at 48 h post-fertilizations[1]
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Dosage:25, 50, 100 nM
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Administration:1, 3, 5 days
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Result:Showed no significant morphological abnormalities (morphology, survival, body length, and heart rate) at any examined time points (1, 3, 5 days) compared to the control group.
Did not induce significant in vivo toxicity in zebrafish embryos.Reduced HEL cell proliferation and migration.
Inhibited the proliferation of HEL cells in the zebrafish xenograft tumor model.
Chemical Information
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No. CAS 2834742-70-8
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Peso molecular 559.65
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Fòrmula C33H37NO7
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SMILES
O=C(CN1CCCCC1)O[C@@H]2C[C@@H](C3=CC=CC=C3)[C@@]4(C5=CC=C(OC)C=C5)[C@]2(O)C6=C(OC)C=C(OC)C=C6O4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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