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. 2021 Jun 9;7(24):eabg0390. doi: 10.1126/sciadv.abg0390

Fig. 4. LLRins506 and VLRins506 mutants are resistant to all RAF inhibitors in clinic or clinical trials albeit sensitive to MEK inhibitor.

Fig. 4

(A to E) Vemurafenib, dabrafenib, PLX8394, and LY3009120 are not able to effectively inhibit the activity of LLRins506 and VLRins506 mutants as they do on BRAF(V600E) or BRAF(ΔNVTAP). 293T transfectants that express individual BRAF mutants were treated with different drugs at indicated concentration for 3 hours, and their ERK signaling was measured by anti–phospho-ERK1/2 immunoblotting (A to D) and quantified to generate graphs by using GraphPad Prism 6 (E). (F and G) MEK inhibitor, trametinib, effectively inhibits the ERK signaling evoked by LLRins506 and VLRins506 mutants. The drug response of 293T transfectants that express individual BRAF mutants was determined as that in (A) to (E). All images are representative of at least three independent experiments.