RIPK2 modulator; pro-drug of cRIPGM; orally bioavailable and brain penetrant
RIPGBM is a RIPK2 modulator, pro-drug of cRIPGM. cRIPGM binds RIPK2 (apparent Kd = 2.3 μM). Selectively induces apoptosis in glioblastoma multiforme cancer stem cell lines (EC50 is <500 nM). Five-fold selective for CSCs compared with control cell types. Reduces the formation of a prosurvival RIPK2/ TAK1 complex and increases the formation of a proapoptotic RIPK2/caspase 1 complex. Inhibits tumor formation and growth
in vivo
. Orally bioavailable and brain penetrant.
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-124578 |
| Réf. fabricant | 18776156 |
| Nom chimique ou matériau | N-[1,4-Dihydro-1,4-dioxo-3-[(phenylmethyl)amino]-2-naphthalenyl]-N-[(4-fluorophenyl)methyl]acetamide |
| CAS | 355406-76-7 |
| Quantité | 50 mg |
| Cible | RIP Kinase Inhibitors |
| Formule moléculaire | C<sub>26</sub>H<sub>21</sub>FN<sub>2</sub>O<sub>3</sub> |
| Poids de la formule | 7272 |
| Pureté | 98% |
