PROTAC BRAF-V600E degrader-1

PROTAC BRAF-V600E degrader-1 (compoun 23) (1-1000 nM; 16 h) induces dose-dependent degradation of endogenous BRAF^V600E and inhibition of ERK phosphorylation in A375 melanoma cells, with significant activity starting at 12 nM over 16 h^[1].
PROTAC BRAF-V600E degrader-1 (1-1000 nM; 16 h) does not induce significant degradation of endogenous wild-type BRAF in A549 lung cancer cells after 16 h of treatment at concentrations up to 1000 nM^[1].
PROTAC BRAF-V600E degrader-1 (1-1000 nM; 16 h) selectively induces dose-dependent degradation of the BRAF^V600E kinase domain but not the wild-type BRAF kinase domain in stably transduced A375 melanoma cells after 16 h of treatment^[1].
PROTAC BRAF-V600E degrader-1 (500 nM; 6 h)-mediated degradation of BRAF^V600E in A375 melanoma cells is dependent on the cereblon E3 ligase and the ubiquitin-proteasome system^[1].
PROTAC BRAF-V600E degrader-1 (10^-10-10^-5 M; 3 days) reduces the viability of BRAF^V600E-expressing A375 melanoma cells with an IC₅₀ of 500 nM over 3 days^[1].
PROTAC BRAF-V600E degrader-1 (10^-10-10^-5 M; 3 days) reduces the viability of BRAF^V600E-expressing HT-29 colon cancer cells with an IC₅₀ of 124 nM over 3 days^[1].
PROTAC BRAF-V600E degrader-1 (40-1000 nM; 7 days) dose-dependently inhibits colony formation by BRAF^V600E-expressing A375 melanoma cells, with significant inhibition at concentrations of 200 nM and 1000 nM over 7 days^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.