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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with K d value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth
In Vitro
PROTAC BRAF-V600E degrader-1 (compound 23) (1 nM-10 μM; 72 h) inhibits the cell viability of A375 and HT-29. PROTAC BRAF-V600E degrader-1 (1-1000 nM; 16 h or 0-24 h) inhibits p-ERK and BRAF-V600E protein in A375 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A375 and HT-29 Concentration: 1 nM-10 μM Incubation Time: 72 h Result: Inhibited the cell viability of A375 and HT-29 with IC 50 s of 46.5 nM and 51 nM. Western Blot AnalysisCell Line: A375 Concentration: 1, 4, 12, 37, 111, 333 and 1000 nM Incubation Time: 16 h or 0-24 h Result: Induced the reduction in the phosphorylation of ERK. Inhibited p-ERK and BRAF-V600E in a dose- and time-dependent manner.
Form:Solid
IC50& Target:BRAF-V600E 2 nM (Kd) Braf 2.4 nM (Kd)