Supplementary Figure S3 from Discovery of a Long Half-Life AURKA Inhibitor to Treat MYC-Amplified Solid Tumors as a Monotherapy and in Combination with Everolimus

Supplementary Figure S3. Discovery, in vivo tumor suppression efficacy and toxicity profile of DBPR728. (A) N-acyl derivatization of 6K465 leads to DBPR728 and its regioisomer 6. (B) Individual tumor growth curve of NCI-H446 xenografts as presented in Fig. 3C. (C) Individual tumor growth curve of NCI-H446 xenografts as presented in Fig. 3E. (D-F) Body weight change of the mice during the experimental course as presented in Fig. 3, C-E. Errors are mean ± SEM. (G) Blood cell count in mice treated with DBPR728 at 100 mpk QD for 14 days. Blood samples were collected at day 15. *, P < 0.05 (t-test, two-tailed). (H) Sera biochemistry profiles for liver and kidney functions in mice treated with DBPR728 at 300 or 600 mpk QW for 3 doses. Sera were harvest 7 days after the last dose. (I) Sera biochemistry profiles in mice treated with DBPR728 at 100 mpk QD for 14 days. Sera were collected at day 15. (G-I) Errors are mean ± SD. Abbreviations in (H-I), GOT, aspartate aminotransferase; GPT, alanine aminotransferase; ALP, alkaline phosphatase; ALB, albumin; BUN, blood urea nitrogen; CRE, creatinine.