Chemical Property of Chidamide
Chemical Property:
- Melting Point:>145°C (dec.)
- Boiling Point:600.2±55.0 °C(Predicted)
- PKA:12.30±0.70(Predicted)
- PSA:97.11000
- Density:1.336±0.06 g/cm3(Predicted)
- LogP:4.42990
- Storage Temp.:2-8°C(protect from light)
- Solubility.:DMSO (Slightly), Methanol (Slightly, Sonicated)
- XLogP3:2.3
- Hydrogen Bond Donor Count:3
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:6
- Exact Mass:390.14920402
- Heavy Atom Count:29
- Complexity:577
- Purity/Quality:
-
99%, *data from raw suppliers
De-4-fluoro 5-Fluoro Chidamide *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Canonical SMILES:C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=CC(=C3)F)N
- Isomeric SMILES:C1=CC(=CN=C1)/C=C/C(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=CC(=C3)F)N
- Recent ClinicalTrials:Treatment of Chidamide and Venetoclax for Retinoic Acid and Arsenic Resistant Acute Promyelocytic Leukemia
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Description
Chidamide (Epidaza?), a class I HDAC inhibitor, was discovered
and developed by ChipScreen and approved by the CFDA in
December 2014 for the treatment of recurrent of refractory peripheral
T-cell lymphoma. Chidamide, also known as CS055 and HBI-
8000, is an orally bioavailable benzamide type inhibitor of HDAC
isoenzymes class I 1–3, as well as class IIb 10, with potential antineoplastic
activity. It selectively binds to and inhibits HDAC, leading
to an increase in acetylation levels of histone protein H3.74 This
agent also inhibits the expression of signaling kinases in the PI3K/
Akt and MAPK/Ras pathways and may result in cell cycle arrest and
the induction of tumor cell apoptosis. Currently, phases I and II
clinical trials are underway for the treatment of non-small cell lung
cancer and for the treatment of breast cancer, respectively.
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Uses
De-5-fluoro 4-Fluorochidamide is an analogue of Chidamide (CAS 743420-02-0), a hitsone deacetylase inhibitor (HDACI) that enhances gemcitabine (G305000) cytotoxicity in pancreatic cancer cells.