CS-1

Names

[ Name ]:
CS-1

[Synonym ]:
1,2-Benzenediol, 4-(6-hydroxy-2-naphthalenyl)-
4-(6-Hydroxy-2-naphthyl)-1,2-benzenediol

Biological Activity

[Description]:

CS1 is a potent DNA Topo II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

[Target]

topoisomerase II alpha

[In Vitro]

CS1 shows cytotoxicity with IC50 values of 16.92 and 18.88 µM for MCF-7 and MCF7/ADR cells, respectively[1] . CS1 (10, 50, 100 µM) inhibits the activity of topoisomerase II α (Topo IIα)[1]. CS1 (0-20 µM) shows antiproliferation activity in cancer cells[1]. CS1 (2.5, 5, 10 µM) induces cell cycle arrest at the G2/M phase[1]. CS1 (2.5, 5, 10 µM) induces cell apoptosis[1]. CS1 (5, 10, 15 µM; 24 h) induces DNA breaks in MDA-MB-231 cells[1]. Cell Cycle Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 2.5, 5, 10 µM Incubation Time: Result: Cells were arrest at the G2/M phase. Apoptosis Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 2.5, 5, 10 µM Incubation Time: Result: Induced apoptosis

[In Vivo]

CS1 (20 mg/kg; i.v.; every other day for two weeks) shows antitumor effects[1]. Animal Model: Five-week-old female athymic nude mice (BALB/c-nu)[1] Dosage: 20 mg/kg Administration: i.v., every other day for two weeks Result: Showed antitumor effects.

[References]

[1]. Shen Y, et al. CS1 is a novel topoisomerase IIα inhibitor with favorable drug resistance profiles. Biochem Biophys Res Commun. 2014; 453(3):302-8.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
508.8±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₆H₁₂O₃

[ Molecular Weight ]:
252.265

[ Flash Point ]:
251.3±23.3 °C

[ Exact Mass ]:
252.078644

[ LogP ]:
3.08

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.741

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335-H400

[ Precautionary Statements ]:
P305 + P351 + P338

[ RIDADR ]:
UN 3077 9 / PGIII

Related Compounds

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