39 NRB05197 n.a. 40 RH02186 n.a. 41 SCR00400 n.a. Vandetanib 0.95 aPercentage inhibition values of RET activity determined at 100 µM concentration of the test compounds. Values are the average of two determination carried out in triplicate Standard error of the mean (SEM) are 10%. bIC50 values represent the concentration ≤ required to produce 50% enzyme inhibition. Values are the average from at least two independent dose-response curves. Standard error of the mean (SEM) are 10% cNot ≤ active. No inhibition was observed up to 100 of the test compound. μM Table SI3. RET, EGFR, and VEGFR2 Inhibitory Activity of Compounds 7-13. IC50 RET-WT IC50 EGFR IC50 VEGFR-2 N° Compound (μM)a (μM)a (μM)a 7 12.1 n.a.b 17.8 8 20.9 n.a. 21.6 9 54.0 n.a. 92.7 10 63.8 n.a. 67.0 11 68.4 31.8 9.61 12 78.1 14.9 1.66 82.6 n.a. 47.0 13 aIC50 values represent the concentration required to produce 50% enzyme inhibition. Values are the average from at least two independent curves. Standard error of the mean (SEM) are 10 %. bNot active. ≤ No inhibition was observed up to 100 of the test compound. μM
39 NRB05197 n.a. 40 RH02186 n.a. 41 SCR00400 n.a. Vandetanib 0.95 aPercentage inhibition values of RET activity determined at 100 µM concentration of the test compounds. Values are the average of two determination carried out in triplicate Standard error of the mean (SEM) are ≤ 10%. bIC50 values represent the concentration required to produce 50% enzyme inhibition. Values are the average from at least two independent dose-response curves. Standard error of the mean (SEM) are ≤ 10% cNot active. No inhibition was observed up to 100 μM of the test compound. Table SI3. RET, EGFR, and VEGFR2 Inhibitory Activity of Compounds 7-13. N° Compound IC50 RET-WT (μM)a IC50 EGFR (μM)a IC50 VEGFR-2 (μM)a 7 12.1 n.a.b 17.8 8 20.9 n.a. 21.6 9 54.0 n.a. 92.7 10 63.8 n.a. 67.0 11 68.4 31.8 9.61 12 78.1 14.9 1.66 13 82.6 n.a. 47.0 aIC50 values represent the concentration required to produce 50% enzyme inhibition. Values are the average from at least two independent curves. Standard error of the mean (SEM) are ≤ 10 %. bNot active. No inhibition was observed up to 100 μM of the test compound.
1-s2.0-S022352341830223X-mmc1.docx