||Selective / Pan
||IC50 / Ki
||GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.
||Abl (Y253F), IC50: 0.35 nM; Abl (M351T), IC50: 0.29 nM; Abl (H396P), IC50: 0.35 nM; Abl (Q252H), IC50: 0.15 nM; Abl (G250E), IC50: 0.71 nM; Abl (E255K), IC50: 0.27 nM; Abl (T315I), IC50: 0.68 nM; Abl, IC50: 0.34 nM
||Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.
||Abl, IC50: 0.37 nM
||Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
||Abl, IC50: 0.6 nM
||Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
||Abl , IC50: 0.6 nM
||DCC-2036 (Rebastinib) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.
||p-Abl1 (T315I), IC50: 4 nM; u-Abl1 (T315I), IC50: 5 nM; Abl1 (H396P), IC50: 1.4 nM; p-Abl1 (native), IC50: 2 nM; u-Abl1 (native), IC50: 0.75 nM
||KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.
||Abl, IC50: 14 nM; Abl (T315I), IC50: 4 nM
||AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also potent to Aurora A/B, Abl(T315I). Phase 2.
||Abl (Q252H), IC50: 10 nM-30 nM; Abl1 (T315I), IC50: 4 nM
||Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.
||Abl, IC50: 5.8 nM
||Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2.
||Abl, IC50: 25 nM
||Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.
||v-Abl, IC50: 30 nM
||Imatinib Mesylate (STI571)
||Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.
||v-Abl, IC50: 600 nM
||NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
||c-Abl, IC50: 1.667 μM