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.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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
|
M.Wt
|
1008.14
|
|
Formula
|
C55H59F2N11O6
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
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
|
References
1. Qiao JX, et al. J Med Chem. 2024 Oct 22. doi: 10.1021/acs.jmedchem.4c02083.
Contact Us
sales@probechem.com
