KIT/PDGFRA-IN-1
KIT/PDGFRA-IN-1 (compound 19) is a stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA) inhibitor. KIT/PDGFRA-IN-1 inhibits KIT-wt, KIT-D816H, KIT-T670I, PDGFRA-wt, PDGFRA-D842V, PDGFRA-T674I and PDGFRA-G680R with IC50s of 2.3, 12, 492, 0.8, 99.9, 42.3, and 4.3 μM, respectively. KIT/PDGFRA-IN-1 inhibits GIST-T1, T1-a-D842V and GIST-48B cells (PDGFR- and KIT-Mutant GIST cell Lines) with GR50s of 12, 8900, ≥10 000 nM, respectively[1].
Product Specifications
UNSPSC
12352005
Target
PDGFR
Related Pathways
Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Smiles
CC1=C(C=C(C=C1)C(NC2=CC(C(F)(F)F)=C(C=C2)NC(C=C)=O)=O)C#CC3=CN=C4N3N=CC=C4
Molecular Formula
C26H18F3N5O2
Molecular Weight
489.45
References & Citations
[1]Schulz T, et al. Design, Synthesis, and SAR of Covalent KIT and PDGFRA Inhibitors-Exploring Their Potential in Targeting GIST. J Med Chem. 2025 Feb 13;68 (3) :3238-3259.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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