Crenolanib benzenesulfonate  (Synonyms: CP 868596-26)

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 K_ds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

Kd: 2.1 nM (PDGFRα), 3.2 nM (PDGFRβ), 0.74 nM (FLT3)

601.72

C₃₂H₃₅N₅O₅S

670220-93-6

NC1CCN(C2=CC=CC3=C2N=C(N4C5=CC=C(C=C5N=C4)OCC6(COC6)C)C=C3)CC1.O=S(C7=CC=CC=C7)(O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]