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.
For research use only. We do not sell to patients.
- Formula: C27H34N8O4
- Molecular Weight:534.61
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Histamine Receptor Isoforms
More
Biological Activity
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.
-
Cell Line:MCF-7 human breast cancer cell line
-
Concentration:1 μM, 10 μM
-
Incubation Time:72 h
-
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.
-
Animal Model:MCF-7 xenograft model using BALB/c female mice (n = 4/6 per group)[1].
-
Dosage:40 mg/kg
-
Administration:I.p., once daily for 14 days
-
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
-
Molecular Weight 534.61
-
Formula C27H34N8O4
-
SMILES
CC(C1=C(C2=CN=C(N=C2N(C1=O)C3CCCC3)NCCC4CCN(CC4)C5=NC=C(C=N5)C(NO)=O)C)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)
MFDCH016 Related Classifications
HY-178350 Related Classifications
Powered by Bioz