Formulation: A solid
Formal Name: (2S,4R)-1-((S)-2-(2-(4-(4-(3-(2,6-difluoro-3-(propylsulfonamido)benzoyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98%
Formula Markup: C51H57F2N9O7S2
Formula Weight: 1010,2
Shelf life (days): 1460
CAS Number: 2413035-41-1
Notes: PROTAC RAF degrader 1 is a proteolysis-targeting chimera (PROTAC) that contains the inhibitor of mutant V600E and wild-type B-RAF vemurafenib (PLX4032; Item No. 10618) conjugated to VHL ligand 1 (Item No. 21591).{69768} It selectively induces the degradation of B-RAF containing a valine-to-glutamate substitution at position 600 (B-RAFV600E) over wild-type B-RAF in SK-MEL-239 melanoma cells at 10 to 1,000 nM but non-selectively inhibits the activity of wild-type B-RAF and a panel of mutant B-RAF isoforms (IC50s = 5.8 and 1.87 nM). PROTAC RAF degrader 1 reduces cell viability of SK-MEL-28, SK-MEL-239, and SK-MEL-246 melanoma cells (EC50s = 215, 37, and 243 nM, respectively). In vivo, PROTAC RAF degrader 1 (50 mg/kg twice per day) reduces tumor growth and volume in an SK-MEL-246 mouse xenograft model.
English
Deutsch
