2 Results for "

RET-Y806

" in MedChemExpress (MCE) Product Catalog:
Products (2)

2 Results for "RET-Y806" in MCE Product Catalog:

  • Targets Recommended:
Cat. No.: HY-E70781
Target:  

RET

Research Areas:  

Cancer

Rearranged during transfection (RET) is a transmembrane receptor protein tyrosine kinase (PTK) activated normally by forming ternary complexes with its cognate ligands and co-receptors. RET alterations by point mutations and gene fusions were found in diverse cancers. RET Y806H is a mutant of RET. RET Y806H Recombinant Human Active Protein Kinase is a recombinant RET Y806H protein that can be used to study RET Y806H-related functions .
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Cat. No.: HY-178061
CAS No.: 2598870-24-5
Target:  

ERK RET

Research Areas:  

Cancer

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 .
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