MS 39 is a potent, high affinity and selective Degrader (PROTAC™) of mutant epidermal growth factor receptor (EGFR), comprising gefitinib (Iressa, Cat. No. 3000) conjugated via a linker to a VHL ligand. MS 39 potently induces degradation of mutant EGFR (DC50 values are 5 nM and 3.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) lung cancer cell lines, respectively), but exhibits no significant effect in cell lines bearing wild-type EGFR at concentrations up to 10 μM. MS 39 inhibits proliferation of H3255 lung cancer cells
in vitro
, and is bioavailable in mice following ip administration.
PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-124802 |
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| Réf. fabricant | 18756556 |
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| Nom chimique ou matériau | (2 S,4 R)-1-(-2-(11-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-11-oxoundecanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
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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>71</sub>ClFN<sub>9</sub>O<sub>7</sub>S |
|---|
| Pureté | 0.98 |
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