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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