PROTAC RAF Degrader 1 (Synonyms: SJF-0628) |
| رقم الكتالوجGC91586 |
PROTAC RAF degrader 1 is a proteolysis-targeting chimera (PROTAC) that contains the inhibitor of mutant V600E and wild-type B-RAF vemurafenib (PLX4032; ) conjugated to VHL ligand 1 .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2413035-41-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
PROTAC RAF degrader 1 is a proteolysis-targeting chimera (PROTAC) that contains the inhibitor of mutant V600E and wild-type B-RAF vemurafenib (PLX4032; ) conjugated to VHL ligand 1 .[1] 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.
References:
[1].Alabi, S., Jaime-Figueroa, S., Yao, Z., et al.Mutant-selective degradation by BRAF-targeting PROTACsNat. Commun.12(1)920(2021).
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *