APS03118
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES) . APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI) -resistant, RET-driven cancer research[1].
Product Specifications
CAS Number
2598870-24-5
UNSPSC
12352005
Target
ERK; RET
Related Pathways
MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
CCOC1=CN2NC3=NN=CC3=C2C(C4=CC=C(N5CC6N(C(C6)C5)CC7=CN=C(C=C7)OC)N=C4)=C1
Molecular Formula
C27H28N8O2
Molecular Weight
496.56
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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