QZ2135

Chemical Structure : QZ2135

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	923.10
分子式	C53H54N12O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Qian Zhang, et al. J Med Chem. 2025 Jan 9;68(1):753-775.

QZ2135

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物理化学性质&存储条件

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QZ2135

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