Cayman AV-412

AV-412 is a dual inhibitor of EGFR and HER2 (IC₅₀s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFR^L858R, EGFR^T790M, EGFR^L858R,T790M, and HER2 recombinant intracellular kinase domains, respectively). It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC₅₀s = >10 μM) but also inhibits Abl, FLT1, and Src (IC₅₀s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 μM) induces ubiquitination and degradation of HER2 in SK-BR-3 cells. It decreases levels of HER2 and estrogen receptor α (ERα) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 μM. AV-412 inhibits EGF-stimulated growth of A431 cells (IC₅₀ = 0.1 μM). It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.

WARNING This product is not for human or veterinary use.