Ansamitocin P-3

66584-72-3

C32H43ClN2O9

DMSO : >= 100 mg/mL (157.45 mM); H2O : < 0.1 mg/mL (insoluble)

Cell Cycle/DNA Damage; Cytoskeleton; Antibody-drug Conjugate/ADC Related

Ansamitocin P-3 is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic. IC50 & Target: Microtubule^[1] In Vitro: Ansamitocin P3 potently inhibits the proliferation of MCF-7, HeLa, EMT-6/AR1 and MDA-MB-231 cells in culture with a half-maximal inhibitory concentration of 20+/-3, 50+/-0.5, 140+/-17, and 150+/-1.1 pM, respectively. Further, Ansamitocin P3 is found to bind to purified tubulin in vitro with a dissociation constant (K_d) of 1.3+/-0.7 uM. The binding of Ansamitocin P3 induces conformational changes in tubulin. Ansamitocin P3 inhibits the proliferation of MCF-7, HeLa, EMT-6/AR1 and MDA-MB-231 cells in culture in a concentration dependent manner. Flow cytometric analysis of PI-stained cells suggests that Ansamitocin P3 inhibits the cell cycle progression of MCF-7 cells in G2/M phase. For example, 26, 50 and 70% of the cells are found to be in G2/M phase in the absence and presence of 50 and 100 pM Ansamitocin P3, respectively^[2].