MFDCH016
MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer.
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- Fòrmula: C27H34N8O4
- Peso molecular:534.61
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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
MFDCH016 (1 μM, 10 μM, 72 h) shows a proliferation inhibition rate of 55% and 86% against MCF-7 cells at concentrations of 1 μM and 10 μM, respectively[1].
MFDCH016 (1 μM, 10 μM) dose-dependently inhibits the cell activity of a range of cancer cell lines, including MCF-7, T47D, A549, NCI-H460, NCI-H1299, FaDu, UDSCC-2, MC38, and CT26[1].
MFDCH016 (0.001-100 μM) has a good inhibitory effect on MCF-7 breast cancer cells (GI50 = 2.476 μM) [1].
MFDCH016 (12-72 h) effectively inhibits tumor cell proliferation in MCF-7 cells, characterized by G0/G1 phase cell cycle arrest, a significant reduction in S-phase and G2/M populations, and culminating in apoptosis, alongside significantly upregulating acetyl-H3 and p21 protein levels and downregulating cyclin D1 expression, effects which increased over time and peaked at 72 hours[1].
MFDCH016 (10 μM) shows low cardiotoxicity to all hERG channels in the hERG-HEK Stable cell line, with an average inhibition rate of 22.8% at a concentration of 10 μM[1].
MFDCH016 exhibits negligible activity against other CDKs (IC50 > 5000 nM for most isoforms, and >10,000 nM for CDK1, CDK2, CDK7, and CDK10), yielding selectivity folds exceeding 700-fold over non-target CDKs[1].
MFDCH016 demonstrates moderate inhibition of CYP1A2 (20.7 %), CYP2C9 (29.2 %), and CYP2C19 (26.5 %), while exhibiting lesser inhibition of CYP2D6 (14.8 %)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 human breast cancer cell line
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Concentration:1 μM, 10 μM
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Incubation Time:72 h
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Result:Showed a proliferation inhibition rate of 55% and 86% against MCF-7 cells at concentrations of 1 μM and 10 μM, respectively.
| Species | Dose | Route | T1/2 | AUC0-t | AUC0-∞ | CL | Vss | Cmax | Tmax |
|---|---|---|---|---|---|---|---|---|---|
| Mice | 2.5 mg/kg | i.v. | 0.45 h | 306 ng·h/mL | 313 ng·h/mL | 8.2 L/h/kg | 2.8 L/kg | / | / |
| Mice | 30 mg/kg | p.o. | 2.7 h | 378 ng·h/mL | 407 ng·h/mL | / | / | 411 ng/mL | 0.21 h |
| Mice | 5 mg/kg | i.p. | 0.49 h | 84 ng·h/mL | 89 ng·h/mL | / | / | 147 ng/mL | 0.13 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MCF-7 xenograft model using BALB/c female mice (n = 4/6 per group)[1].
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Dosage:40 mg/kg
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Administration:I.p., once daily for 14 days
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Result:Exhibited a strong antitumor effect, with a low average tumor weight.
Body weight remained stable, with no evidence of toxicity or weight loss.
Chemical Information
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Peso molecular 534.61
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Fòrmula C27H34N8O4
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SMILES
CC(C1=C(C2=CN=C(N=C2N(C1=O)C3CCCC3)NCCC4CCN(CC4)C5=NC=C(C=N5)C(NO)=O)C)=O
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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)
MFDCH016 Related Classifications
HY-178350 Related Classifications
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