SDZ281-977

SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A. In Vitro: The anticancer profile of SDZ 281-977 is investigated in nude mice bearing the human tumor cell lines A431 (vulvar carcinoma cells), MIA PaCa-2 (pancreatic tumor cells) and MDA-MB-231 (breast carcinoma cells). These cell lines are selected because of their sensitivity for SDZ 281-977. The IC₅₀ values for inhibition of growth of A431, MIA PaCa-2 and MDA-MB-231 cells are 0.21 μM, 0.29 μM and 0.43 μM, respectively^[1]. In Vivo: Nude mice bearing A431 human vulvar carcinomas receive intravenous injections of SDZ 281-977 (1-10 mg/kg) for 4 weeks. This treatment results in a dose-dependent inhibition of tumor growth. Orally administered SDZ 281-977 (30 mg/kg) induces a 54% inhibition of A431 tumor growth after 3 weeks of treatment. The above regimens are well tolerated. No significant change in body weight occurred during treatment^[1].