SMKIs

lab experiment

FDA-approved small molecule kinase inhibitors-Part 3

Fostamatinib is the precursor drug of active metabolite R406. It is a Syk inhibitor with an IC50 value of 41 nM. It strongly inhibits Syk but does not inhibit Lyn. […]

drug research

FDA-approved small molecule kinase inhibitors-Part 2

Dabrafenib (GSK2118436) is a mutant BRAFV600-specific inhibitor, with an IC50 of 0.7 nM in cell-free assays. It shows 7-fold and 9-fold lower potency against B-Raf(wt) and c-Raf, respectively. Synthetic route: […]

drug development

FDA-approved small molecule kinase inhibitors-Part 1

Kinase inhibitors can be divided into monoclonal antibodies (mAbs) and small molecule kinase inhibitors (SMKIs) based on their structure and size. Monoclonal antibodies have achieved great success in the development […]