SJF 1528
This bifunctional degrader, composed of lapatinib linked to a VHL ligand, potently induces the degradation of wild-type EGFR (DC50 = 39.2 nM in OVCAR8) and HER2, and is active against Exon20Ins mutant EGFR. It inhibits proliferation in HER2-driven breast cancer models like SKBr3 cells (IC50 = 102 nM), supporting its use in targeted protein degradation research for oncology.
Product Specifications
CAS Number
2230821-38-0
Field of Research
Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction
Smiles
Cc1ncsc1-c1ccc (CNC (=O) [C@@H]2C[C@@H] (O) CN2C (=O) [C@@H] (NC (=O) COCCOCCOc2ccc (cc2) -c2ccc3ncnc (Nc4ccc (OCc5cccc (F) c5) c (Cl) c4) c3c2) C (C) (C) C) cc1 |@:67|
Molecular Formula
C55H57ClFN7O8S
Molecular Weight
1030.61
Storage Conditions
-20°C
Notes
For research use only.
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