PP2 is Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.
PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
PRT062607 (P505-15, BIIB057) HCl
PRT062607 (P505-15) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM, >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.
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.
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 1/2.
Features:The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
KX2-391 (KX01), the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 1/2.
Ibrutinib is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.
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.
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.