Chidamide
- Product Name
- Chidamide
- CAS No.
- 743420-02-2
- Chemical Name
- Chidamide
- Synonyms
- CS-1764;Chidamide;HBI-8000);HDAC-IN-7;Chidamide D4;Chidamide(CS055;chidamide analog;Chidamide impurity;Chidamide USP/EP/BP;Tucidinostat (Chidamide)
- CBNumber
- CB42590631
- Molecular Formula
- C22H19FN4O2
- Formula Weight
- 390.41
- MOL File
- 743420-02-2.mol
Chidamide Property
- Melting point:
- >145°C (dec.)
- Boiling point:
- 600.2±55.0 °C(Predicted)
- Density
- 1.336±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C(protect from light)
- solubility
- DMSO (Slightly), Methanol (Slightly, Sonicated)
- form
- Solid
- pka
- 12.30±0.70(Predicted)
- color
- Off-White to Pale Beige
- InChI
- InChI=1S/C22H19FN4O2/c23-18-8-9-19(24)20(12-18)27-22(29)17-6-3-16(4-7-17)14-26-21(28)10-5-15-2-1-11-25-13-15/h1-13H,14,24H2,(H,26,28)(H,27,29)
- InChIKey
- WXHHICFWKXDFOW-UHFFFAOYSA-N
- SMILES
- C(NC1=CC(F)=CC=C1N)(=O)C1=CC=C(CNC(=O)C=CC2=CC=CN=C2)C=C1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 13686
- Product name
- Chidamide
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $39
- Updated
- 2021/12/16
- Product number
- 13686
- Product name
- Chidamide
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $166
- Updated
- 2021/12/16
- Product number
- 13686
- Product name
- Chidamide
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $293
- Updated
- 2021/12/16
- Product number
- 13686
- Product name
- Chidamide
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $634
- Updated
- 2021/12/16
- Product number
- 445836
- Product name
- De-4-fluoro 5-Fluoro Chidamide
- Packaging
- 25mg
- Price
- $460
- Updated
- 2021/12/16
Chidamide Chemical Properties,Usage,Production
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.
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.
Synthesis
The scalable synthetic approach to chidamide very closely follows the discovery route. The sequence began with the condensation of commercial nicotinaldehyde (52) and malonic acid (53) in a mixture of pyridine and piperidine. Next, activation of acid 54 with N,N0-carbonyldiimidazole (CDI) and subsequent reaction with 4-aminomethyl benzoic acid (55) under basic conditions afforded amide 56 in 82% yield. Finally, activation of 56 with CDI prior to treatment with 4-fluorobenzene- 1,2-diamine (57) and subsequent treatment with TFA and THF yielded chidamide (VIII) in 38% overall yield from 52. However, no publication reported that mono-N-Boc-protected bis-aniline was used to approach Chidamide.
References
[1] gong k, xie j, yi h, li w. cs055 (chidamide/hbi-8000), a novel histone deacetylase inhibitor, induces g1 arrest, ros-dependent apoptosisand differentiation in human leukaemia cells. biochem j. 2012 may 1;443(3):735-46.
[2] wang h1, guo y, fu m, liang x, etal. , antitumor activity of chidamide in hepatocellular carcinoma cell lines. mol med rep. 2012 jun;5(6):1503-8.
Chidamide Preparation Products And Raw materials
Raw materials
Preparation Products
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- 0755-84533301
- Fax
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- China
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- 18149758185
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View Lastest Price from Chidamide manufacturers
- Product
- Chidamide 743420-02-2
- Price
- US $1.10/g
- Min. Order
- 1g
- Purity
- 99.9%
- Supply Ability
- 100 Tons min
- Release date
- 2021-08-17
- Product
- Chidamide 743420-02-2
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 20kg
- Release date
- 2019-09-05