sklb4771

Description: SKLB4771 (also known as FLT3-IN-1) is a novel, potent and selective inhibitor of FLT3 (fms-like tyrosine kinase 3) that may be potentially used for the treatment of cutaneous inflammation and psoriasis-like symptoms of disease. SKLB4771 inhibited FLT3 phosphorylation dose-dependently. Consistent with the downregulation of the phosphorylation of FLT3, the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations > 0.1 uM. In an MV4-11 xenograft mouse model, a once-daily dose of SKLB4771 at 100 mg/kg for 18 days led to complete tumor regression without obvious toxicity.

References: J Med Chem. 2012 Apr 26; 55(8):3852-66.