LDD 39 | RET degrader | Probechem Biochemicals

Chemical Structure : LDD 39

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LDD 39 (RET degrader LDD39)

货号: PC-23265Not For Human Use, Lab Use Only.

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生物&药学活性

LDD 39 is a pyrazolopyridine-based heterobifunctional RET ligand-directed degrader with IC50 of 2.0/1.1/7.5 nM for WT RET/V804M/G810R respectively, and DC50 of 0.97/3.2/6.4 nM in TPC-1 cells against both RET WT and the two mutants.
LDD 39 exhibited a differentiated and favorable in vivo profile compared to the corresponding tyrosine kinase inhibitor (TKI) selpercatinib.
LDD 39 (15-75 mg/kg) induced robust and sustained degradation of total-RET (tRET) protein and inhibition of phospho-RET (pRET) signaling in TPC-1 xenograft tumors driven by RET and the RET/G810R mutant.

物理化学性质&存储条件

分子量	1008.14
分子式	C55H59F2N11O6
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	N-(1-(5-(3-Cyano-6-ethoxypyrazolo[1,5-a]pyridin-4-yl)pyridin-2-yl)-4-((4-cis-(3-(4-(2-(2,6-dioxopiperidin-3-yl)-3-oxoisoindolin-5-yl)piperidin-1-yl)cyclobutane-1-carbonyl)piperazin-1-yl)methyl)piperidin-4-yl)-2,5-difluorobenzamide

参考文献

1. Qiao JX, et al. J Med Chem. 2024 Oct 22. doi: 10.1021/acs.jmedchem.4c02083.

LDD 39 (RET degrader LDD39)

生物&药学活性

物理化学性质&存储条件

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LDD 39 (RET degrader LDD39)

生物&药学活性

物理化学性质&存储条件

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