LRG20 | GLI1 degrader | Probechem Biochemicals

Chemical Structure : LRG20

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LRG20 (LRG-20)

货号: PC-28804Not For Human Use, Lab Use Only.

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生物&药学活性

LRG20 is a potent, orally bioavailable, CRBN-dependent GLI1 PROTAC degrader with DC50 of 16.93 nM and Dmax=91.1% in HT-29 colorectal cancer cells, preferentially degrading GLI1/GLI2 over GLI3 without obvious degradation of representative CRBN neo-substrates.
LRG20 induces GLI1 degradation via the CRBN-dependent ubiquitin-proteasome pathway.
LRG20 potently inhibited tumor cell proliferation (HT-29, IC50=0.10 uM).
LRG20 (40 mg/kg) significantly suppressed tumor growth in an HT-29 xenograft model (TGI=70.89%) without observable toxicity.

物理化学性质&存储条件

分子量	665.24
分子式	C38H41ClN6O3
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
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(4-(3-((4-(4-(2-(6-chloro-2H-[1,3]oxazino[5,6-h]quinolin-3(4H)-yl)ethyl)phenyl)piperazin-1-yl)methyl)azetidin-1-yl)phenyl)piperidine-2,6-dione

参考文献

1. Ya-Bing Xin, et al. Eur J Med Chem. 2026 Oct 31;321(Pt 3):119480.

LRG20 (LRG-20)

生物&药学活性

物理化学性质&存储条件

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LRG20 (LRG-20)

生物&药学活性

物理化学性质&存储条件

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