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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
PDGFRα; PDGFRβ
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