Chemical Structure : QZ2135
CAS No.:
QZ2135
Catalog No.: PC-23910Not For Human Use, Lab Use Only.
QZ2135 is a potent, selective RET PROTAC degrader, effectively degrades RET kinase (DC50=4.7 nM) and its resistant mutants, such as V804M (DC50=17.2 nM) and G810C/R.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
QZ2135 is a potent, selective RET PROTAC degrader, effectively degrades RET kinase (DC50=4.7 nM) and its resistant mutants, such as V804M (DC50=17.2 nM) and G810C/R.
QZ2135 exhibits superior antiproliferative activity against Ba/F3 cells stably expressing oncogenic fusions of RET with solvent-front mutants, including G810C/R/S, compared to its parental inhibitor selpercatinib.
QZ2135 showed antitumor activity in vivo in a Ba/F3-KIF5B-G810C xenograft mouse model.
Physicochemical Properties
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M.Wt
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923.10
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Formula
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C53H54N12O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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6-(1-(1-(7-(2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)hept-6-yn-1-yl)piperidin-4-yl)-1H-pyrazol-4-yl)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
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References
1. Qian Zhang, et al. J Med Chem. 2025 Jan 9;68(1):753-775.
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