Pironetin
Names
[ CAS No. ]:
151519-02-7
[ Name ]:
Pironetin
Biological Activity
[Description]:
Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity[1][2].
[Related Catalog]:
[Target]
Microtubule[1]
[In Vitro]
Pironetin (20-100 ng/mL; 24 hours; 3Y1 cells) treatment arrests the cell cycle progression at G2/M in 3Y1 cells[1]. Pironetin (1-10000 ng/mL; 3 days; HeLa, A2780 and K-NRK cells) treatment inhibits the cell proliferation. IC50 values against these cell lines are almost 10 ng/mL[1]. Cell Cycle Analysis[1] Cell Line: 3Y1 cells Concentration: 20 ng/mL, 50 ng/mL, 100 ng/mL Incubation Time: 24 hours Result: Arrested the cell cycle progression at G2/M in3Y1 cells. Cell Proliferation Assay[1] Cell Line: HeLa, A2780 and K-NRK cells Concentration: 1 ng/mL, 10 ng/mL, 100 ng/mL, 1000 ng/mL and 10000 ng/mL Incubation Time: 3 days Result: Inhibited the cell proliferation.
[In Vivo]
Pironetin (0.78-6.25 mg/kg; intraperitoneal injection; daily; for 5 days; female CDF1-SLC mice) treatment shows a moderate antitumor effect, however, a severe weight loss is observed as a side effect[1]. Animal Model: Female CDF1-SLC mice (10 weeks) injected with P388 murine leukemia cells[1] Dosage: 0.78 mg/kg, 1.56 mg/kg, 3.13 mg/kg, 6.25 mg/kg Administration: Intraperitoneal injection; daily; for 5 days Result: Showed a moderate antitumor effect.
[References]
Chemical & Physical Properties
[ Density]:
0.993 g/cm3
[ Boiling Point ]:
473.1ºC at 760 mmHg
[ Molecular Formula ]:
C19H32O4
[ Molecular Weight ]:
324.45500
[ Flash Point ]:
160.3ºC
[ Exact Mass ]:
324.23000
[ PSA ]:
55.76000
[ LogP ]:
3.49860
[ Vapour Pressure ]:
6.14E-11mmHg at 25°C
[ Index of Refraction ]:
1.478