1186222-89-8

Basic information

• Product Name: 4SC-202
• Synonyms: 4SC-202;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;(E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide 4-methylbenzenesulfonate;4SC-202 tosylate
• CAS NO: 1186222-89-8
• Molecular Formula: C₇H₈O₃S*C₂₃H₂₁N₅O₃S
• Molecular Weight: 619.71116
• Mol File: 1186222-89-8.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Solubility: insoluble in H2O; ≥2.4 mg/mL in EtOH with gentle warming and ultrasonic; ≥62 mg/mL in DMSO
• CAS DataBase Reference: 4SC-202(CAS DataBase Reference)
• NIST Chemistry Reference: 4SC-202(1186222-89-8)
• EPA Substance Registry System: 4SC-202(1186222-89-8)

Safety Data

• Hazardous Substances Data: 1186222-89-8(Hazardous Substances Data)

Usage

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.

Upstream product

• 104-15-4 toluene-4-sulfonic acid 

Relevant articles and documents

(E) -N -(2-Amino-phenyl) -3-{1-[4-(1-methyl-1H-pyrazol-4-yl)- benzenesulfonyl]-1H-pyrrol-3-yl} -acrylamide salts

A salt of (E)-N-(2-amino-phenyl)-3-{1-[4-(1-methyl-1H-pyrazol-4-yl)-benzenesulfonyl]-1H-pyrrol-3-yl}-acrylamide selected from the group consisting of the hydrobromide, methansulfonate, hemi ethane-1,2-disulfonate, benzenesulfonate, toluenesulfonate and 2-