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.
性状
Solid
IC50 & Target[1][2]
BRAF-V600E 2 nM (Kd) Braf 2.4 nM (Kd)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay-tbl">
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Han XR, et al. Discovery of Selective Small Molecule Degraders of BRAF-V600E. J Med Chem. 2020 Apr 23;63(8):4069-4080.