DD 03-171 is a potent and selective BTK Degrader (PROTAC™) (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license
.
Caractéristiques techniques
| Marque | Tocris |
|---|
| Réf. B-LABO | BL-RE-158016 |
|---|
| Réf. fabricant | 18756836 |
|---|
| Nom chimique ou matériau | 4-(1,1-Dimethylethyl)-N-[3-[6-[[4-[[4-[6-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1 H-isoindol-4-yl]amino]acetyl]amino]hexyl]-1-piperazinyl]carbonyl]phenyl]amino]-4,5-dihydro-4-methyl-5-oxo-2-pyrazinyl]-2-methylphenyl]benzamide |
|---|
| CAS | 2366132-45-6 |
|---|
| Quantité | 5 mg |
|---|
| Cible | Active Degraders |
|---|
| Formule moléculaire | C<sub>55</sub>H<sub>62</sub>N<sub>10</sub>O<sub>8</sub> |
|---|
| Pureté | 0.98 |
|---|
Une question, une configuration particulière ?
Contactez-nous pour un devis.
