AZM475271

AZM475271 is an inhibitor of c-Src kinase (IC₅₀ = 0.01 µM).¹ It inhibits phosphorylation of c-Src kinase, Lck, c-Yes, and VEGFR2 (IC₅₀s = 0.01, 0.03, 0.08, and 0.7 µM, respectively).² AZM475271 inhibits proliferation of NIH3T3 fibroblasts, as well as PC3 and DU145 prostate and A549 lung cancer cells (IC₅₀s = 0.5, 32, 16, and 17 µM, respectively). It reduces tumor cell proliferation and microvessel density and increases apoptosis in an L3.6pl pancreatic cancer mouse xenograft model when administered at a dose of 50 mg/kg per day. AZM475271 inhibits tumor growth and metastasis in the same mouse xenograft model when administered in combination with gemcitabine (Item Nos. 11690 | 9003096).

WARNING This product is not for human or veterinary use.

1. Plé, P.A., Green, T.P., Hennequin, L.F., et al. Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src. J. Med. Chem. 47(4), 871-887 (2004).

2. Yezhelyev, M.V., Koehl, G., Guba, M., et al. Inhibition of SRC tyrosine kinase as treatment for human pancreatic cancer growing orthotopically in nude mice. Clin. Cancer Res. 10(23), 8028-8036 (2004).