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Table 1 Summary of the impact of eight RTK inhibitors on cancer cell lines from CCLE. For each cancer cell line the metabolism was simulated based on the GEP

From: Computational analysis of receptor tyrosine kinase inhibitors and cancer metabolism: implications for treatment and discovery of potential therapeutic signatures

Drug Target Tumor diagnosis for clinical treatment application (PubMed) Nr. of Significantly affected Metabolic Components in MCPM model Nr. of affected metabolic / signaling pathways Top 5 affected metabolic pathways (Nr. of significantly affected components within the pathway)
AEW541 IGF1R, InsR Testing phase, none specified (17361225) 125 18 / 2 Purine (19), Glycerolipid (10), Glycolysis (8), Amino-sugar (8), Sucrose (6)
PF-2341066 (Crizotinib) c-MET, ALK Non-small cell lung cancer (23724913) 1220 30 / 2 Purine (250), Pyrimidine (114), Inositol-phosphate (62), Fatty-acid (48), Valine/Leucine/Isoleucine (41), Glycolysis (41)
PHA-665752 c-MET Testing phase, none specified (14612533) 445 24 / 1 Purine (88), Inositol-phosphate (36), Pyrimidine (22), Glycolysis (20), Valine/Leucine/Isoleucine (18), Nicotinate (18)
Sorafenib ABL, AURKB/C, BRAF, CDK, DDR, EPHA, FGFR, FLT, KIT, MKNK, MAPK, NTRK Renal cell, hepatocellular, and thyroid cancer (17215530) 1058 30 / 10 Purine (195), Pyrimidine (81), Inositol-phosphate (64), Valine/Leucine/Isoleucine (49), Pyruvate (45)
TKI258 (Dovitinib) FLT3, KIT, FGFR, VEGFR, InsR, EphA, HER2, IGF1R Testing phase, none specified (23658459) 1109 28 / 9 Purine (225), Pyrimidine (111), Fatty-acid (59), Inositol-phosphate (53), Glycolysis (47), Pyruvate (47)
Lapatinib EGFR, ERBB2/4, STK10, PIRK2 Breast cancer (18188694) 504 28 / 7 Purine (82), Pyrimidine (33), Nicotinate (31), Fatty-acid (25), Glycerolipid (22)
ZD6474 (Vandetanib) EGFR, ERBB2/4, FGFR, ABL, EPHA/B Thyroid cancer (26678514) 158 27 / 8 Valine/Leucine/Isoleucine (17), Purine (15), Butanoate (11), Pentose (8), Pyrimidine (7)
Erlotinib EGFR, ABL1, FLT3/4, RET, KIT, RET, SLK, PDGFRA/B, others Non-small cell lung and pancreatic cancer (21388312) 245 23 / 15 Purine (50), Fatty-acid (12), Nicotinate (12), Glycolysis (11), Fructose (11)
  1. The spearman correlation coefficient was calculated between the simulated values of each component/reaction in the MCPM model and IC50 values of the corresponding cancer cell lines. A spearman correlation coefficient with an absolute value ≥0.15 was considered significant after Benferroni correction