Uses
Novel inhibitor of tubulin polymerization
Definition
ChEBI: (5-methoxy-1H-indol-2-yl)-phenylmethanone is a N-acylindole.
Biological Activity
Novel inhibitor of tubulin polymerization; cytotoxic and inhibits tumor cell proliferation in vitro (IC 50 = 74 nM). Prevents growth of tumor models in mice following oral administration in vivo .
in vivo
D-64131 (200-400 mg/kg; p.o.; daily; days 1-5, 8-9, and 15-18) significantly inhibits tumor growth in the human amelanoic melanoma MEXF 989 tumor xenograft mice model[1].
D-64131 has oral bioavailability and is well tolerated at efficacious doses[1].
| Animal Model: | Outbred nude mice (6-8 weeks), human amelanoic melanoma MEXF 989 tumor xenograft model[1] |
| Dosage: | 200 mg/kg, 400 mg/kg |
| Administration: | Oral administration, daily, on days 1-5, 8-9, and 15-18 after xenograft |
| Result: | Resulted in significant tumor growth inhibition during treatment. |
References
1. beckers t, reissmann t, schmidt m et al. 2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors. cancer res. 2002 jun 1;62(11):3113-9.
