SJF 1528 is a potent EGFR PROTAC™ Degrader (DC50 values are 39.2 nM for wild-type EGFR in OVCAR8 cells and 736 nM for Exon20Ins mutated EGFR in HeLa cells). Also degrades HER2. SJF 1528 comprises the EGFR inhibitor lapatinib (Cat. No. 6811) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Inhibits proliferation of HER2-driven breast cancer cell lines (IC50 = 102 nM for SKBr3 cells).
PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license
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Caractéristiques techniques
| Marque | Tocris |
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| Réf. B-LABO | BL-RE-151180 |
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| Réf. fabricant | 18799686 |
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| Nom chimique ou matériau | (2 S,4 R)-1-(-2-(2-(2-(2-(4-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6- yl)phenoxy)ethoxy)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
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| CAS | 2230821-38-0 |
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| Quantité | 5 mg |
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| Cible | Active Degraders |
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| Formule moléculaire | C<sub>55</sub>H<sub>57</sub>ClFN<sub>7</sub>O<sub>8</sub>S |
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| Pureté | 0.98 |
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