Bioactivity | Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively. |
Target | Kd: 2.1 nM (PDGFRα), 3.2 nM (PDGFRβ), 0.74 nM (FLT3) |
CAS | 670220-93-6 |
Formula | C32H35N5O5S |
Molar Mass | 601.72 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Mathias TJ, et al. The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations. Invest New Drugs. 2015 Apr;33(2):300-9. [2]. Wang P, et al. Crenolanib, a PDGFR inhibitor, suppresses lung cancer cell proliferation and inhibits tumor growth in vivo. Onco Targets Ther. 2014 Sep 26;7:1761-8. [3]. Heinrich MC, et al.Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with STI571-resistant gastrointestinal stromal tumors. Clin Cancer Res, 2012, Jun 27. |