MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC™) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib (Iressa, Cat. No. 3000). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50 values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax > 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.
Negative control (Cat. No. 7396) also available.
PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license.
Caractéristiques techniques
| Marque | Tocris Bioscience |
|---|
| Réf. B-LABO | BL-RE-126301 |
|---|
| Réf. fabricant | 18797856 |
|---|
| Nom chimique ou matériau | 3-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-N-(8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)octyl)propanamide |
|---|
| CAS | 2550393-21-8 |
|---|
| Quantité | 5 mg |
|---|
| Cible | Active Degraders |
|---|
| Formule moléculaire | C<sub>46</sub>H<sub>54</sub>ClFN<sub>8</sub>O<sub>8</sub> |
|---|
| Pureté | 0.98 |
|---|
Une question, une configuration particulière ?
Contactez-nous pour un devis.
