MFDCH016 

MFDCH016 is a potent HDAC1/6 (IC₅₀ = 38/59 nM) and CDK4/6 (IC₅₀ = 680/720nM) 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^[1].

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.

MFDCH016 (40 mg/kg, i.p., once daily for 14 days) is an effective in vivo antitumor drug that has a significant antitumor effect in MCF-7 xenograft mice and no significant toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

534.61

C₂₇H₃₄N₈O₄

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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• [1]. Kim B, et al. Design and synthesis of novel cyclin-dependent kinase 4/6(CDK4/6) and histone deacetylase (HDAC) dual inhibitors: In vitro and in vivo anticancer activity. Eur J Med Chem. 2025 Sep 21;301:118192.  [Content Brief]