Crenolanib

Crenolanib is an orally bioavailable, selective inhibitor of type III tyrosine kinases with nanomolar potencies against platelet-derived growth factor receptor α (PDGFRα) and PDGFRβ and Fms-related tyrosine kinase 3 (FLT3; IC₅₀s = 11, 3.2, and 4 nM, respectively).^1,2 It also inhibits medically-relevant mutant forms of these kinases, including the D842V-containing form of PDGFR and D835Y and internal tandem duplication mutations of FLT3, at nanomolar concentrations.^1,3,4 Crenolanib is more than 100-fold selective for these kinases over other tyrosine and serine/threonine kinases. It is effective when used in cells and in vivo.^1,2,4

WARNING This product is not for human or veterinary use.

1. Heinrich, M.C., Griffith, D., McKinley, A., et al. Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin. Cancer Res. 18(16), 4375-4385 (2012).

2. Smith, C.C., Lasater, E.A., Lin, K.C., et al. Crenolanib is a selective type I pan-FLT3 inhibitor. Proc. Natl. Acad. Sci. USA 111(14), 5319-5324 (2014).

3. Dai, J., Kong, Y., Si, L., et al. Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib. Clin. Cancer Res. 19(24), 6935-6942 (2013).

4. Galanis, A., Ma, H., Rajkhowa, T., et al. Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants. Blood 123(1), 94-100 (2014).