Crenolanib

Crenolanib 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.

Product Specifications

CAS Number

[670220-88-9]

Product Name Alternative

CP-868596

UNSPSC

12352005

Target

Autophagy; FLT3; PDGFR

Type

Reference compound

Related Pathways

Autophagy; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/crenolanib.html

Concentration

10mM

Purity

99.68

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C26H29N5O2

Molecular Weight

443.54

References & Citations

[1]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.|[2]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.|[3]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.