Imatinib (STI571): Selectivity & Specificity

Imatinib (STI571) is a potent inhibitor of Abl kinase (~0.005 μM), M343T Abl kinase (~0.01 μM), M351T Abl kinase (~0.05 μM), M472I Abl kinase (~0.01 μM), F486S Abl kinase (~0.1 μM), I502M Abl kinase (~0.005 μM), E509D Abl kinase (~0.005 μM), T315I Abl kinase (>1 μM), recombinant UGT1A3, UGT1A4, UGT2B17 enzymes (UGT1A3: 20 µM; UGT1A4: 15 µM; UGT2B17: 0.07 µM), BCRP (0.08-0.29 µM), Abl1 kinase (0.327 µM), CSF1R (19nM), PDGFR and c-KIT (49.4 ng/mL), Abl tyrosine kinase (10.77 ±0.41), PI3K (312 nM), mTOR kinase (214 nM), PDGFRA-FIP1L1 (3.2 nM), ETV6-PDGFRB (50 nM), BCR-ABL1 (582 nM), STAT3, BCR-ABL (565 ± 656 nM), ABL1 (M351T) (1298 ± 542 nM), ABL1 (F359V) (>10000 nM), ABL1 (E255K) (8222 ± 484 nM), ABL1 (Y253H) (8936 ± 1774 nM), ABL1 (E255V) (7565 ± 3268 nM), ABL1 (M244V) (2963 ± 83 nM), ABL1 (T315I) (>10000 nM), ABL1 (F317L) (526 ± 56 nM), ABL1 (F311I) (3547 ± 223 nM), ABL1 (V299L) (1987 ± 1237 nM), ABL1 (T315I/E255V) (>10000 nM), ABL1 (T315I/F359V) (>10000 nM), ABL1 (T315I/G250E) (>10000 nM), ABL1 (T315I/E255K) (>10000 nM), ABL1 (T315I/E453K) (8466 ± 1628 nM), ABL1 (T315I/M351T) (7603 ± 1498 nM), ABL1 (T315I/F311I) (7144 ± 2459 nM), ABL1 (T315I/H396R) (8953 ± 5314 nM), ABL1 (T315I/Y253H) (>10000 nM), ABL1 (T315I/F317L) (>10000 nM), ABL1 (T315M) (>10000 nM), ABL1 (G250E/V299L) (6486 ± 2622 nM), ABL1 (F317L/F359V) (7195 ± 1729 nM), ABL1 (Y253H/E255V) (>10000 nM), ABL1 (T253H/F359V) (>10000 nM), PDGFRB, KIT, PDGFRA, IDO1, ETV4, PDGFR. Imatinib (STI571) exhibits the greatest inhibitory potency toward PDGFRA-FIP1L1 (IC50 = 3.2 nM).