CG 858 is a selective BRAF-V600E protein Degrader (uSMITETM). CG 858 comprises the BRAF kinase inhibitor vemurafenib linked to the E3 ligase ligand Thalidomide (Cat. No. 0652). CG 858 dose-dependently degrades BRAF-V600E but not wild type BRAF, and reduces cell viability and colony formation in HT-29 and A375 cells (DC50 values are 124 nM and 500 nM, respectively). Exhibits 88% degradation at 500 nM. CG 858 also impairs melanoma cell growth.
CG 858 negative control (Cat. No. 7428) also available.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-125328 |
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| Réf. fabricant | 18708686 |
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| Nom chimique ou matériau | N-[[4-[3-[2,6-Difluoro-3-[(propylsulfonyl)amino]benzoyl]-1 H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1 H-isoindol-5-yl]amino]pentanamide |
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| CAS | 2417296-82-1 |
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| Quantité | 5 mg |
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| Cible | Active Degraders |
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| Formule moléculaire | C<sub>42</sub>H<sub>39</sub>F<sub>2</sub>N<sub>7</sub>O<sub>8</sub>S |
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| Pureté | 0.98 |
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