Chemical Structure : LDD 39
CAS No.:
3028786-01-5
LDD 39
(RET degrader LDD39)
Catalog No.: PC-23265Not For Human Use, Lab Use Only.
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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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1008.14
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Formula
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C55H59F2N11O6
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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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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
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References
1. Qiao JX, et al. J Med Chem. 2024 Oct 22. doi: 10.1021/acs.jmedchem.4c02083.
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