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ChemicalBook--->CAS DataBase List--->1186222-89-8

1186222-89-8

1186222-89-8 Structure

1186222-89-8 Structure
IdentificationBack Directory
[Name]

4SC-202
[CAS]

1186222-89-8
[Synonyms]

4SC-202
CS-1272
4SC-202 tosylate
Domatinostat tosylate
4SC-202;4SC202;4SC 202
(E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide 4-methylbenzenesulfonate
4SC-202 2-Propenamide, N-(2-aminophenyl)-3-[1-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]sulfonyl]-1H-pyrrol-3-yl]-, (2E)-, 4-methylbenzenesul
[Molecular Formula]

C30H29N5O6S2
[MDL Number]

MFCD25976779
[MOL File]

1186222-89-8.mol
[Molecular Weight]

619.711
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

insoluble in H2O; ≥2.4 mg/mL in EtOH with gentle warming and ultrasonic; ≥62 mg/mL in DMSO
[form ]

Powder
[color ]

Light yellow to brown
Safety DataBack Directory
[Symbol(GHS) ]


GHS07,GHS08,GHS09,GHS06
[Signal word ]

Danger
[Hazard statements ]

H341-H411-H315-H331-H317-H301-H311
[Precautionary statements ]

P261-P272-P280-P302+P352-P333+P313-P321-P363-P501-P201-P202-P281-P308+P313-P405-P501-P261-P271-P304+P340-P311-P321-P403+P233-P405-P501-P264-P270-P301+P310-P321-P330-P405-P501-P280-P302+P352-P312-P322-P361-P363-P405-P501-P264-P280-P302+P352-P321-P332+P313-P362
Hazard InformationBack Directory
[Description]

4SC-202 is an inhibitor of the class I histone deacetylases (HDACs) HDAC1-3 and the histone demethylase KDM1A. It reduces cell viability in a panel of colorectal cancer (CRC) cell lines when used at concentrations ranging from 1 to 10 μM and in patient-derived CRC cell lines when used at a concentration of 5 μM. 4SC-202 (5 μM) induces cell cycle arrest at the G2/M phase in HT-29 cells and primary human CRC cells and increases apoptosis in HT-29 cells in a concentration-dependent manner, an effect that is enhanced by the Akt inhibitors perifosine and MK-2206 . 4SC-202 (100 mg/kg, p.o., every other day) reduces tumor growth in an HT-29 mouse xenograft model when administered alone and to an enhanced degree when co-administered with oxaliplatin (Item No. 13106).
[in vivo]

studies, 4sc-202 has shown a good tolerability and dose-dependent effect on anti-tumour activity compared with other inhibitors in the a549nsclc xenograft model and the rko27 colon carcinoma model [1].
[References]

[1] henning s w, doblhofer r, kohlhof h, et al. 178 preclinical characterization of 4sc-202, a novel isotype specific hdac inhibitor[j]. european journal of cancer supplements, 2010, 8(7): 61.
Spectrum DetailBack Directory
[Spectrum Detail]

4SC-202(1186222-89-8)MS
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