Tyk2 Selective 阻害剤

製品コード 製品名 製品説明 Selective / Pan IC50 / Ki
S7634 Cerdulatinib (PRT062070, PRT2070) Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM. Selective TYK2, IC50: 0.5 nM
S1134 AT9283 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. Pan TYK2, IC50: 1 nM-10 nM
S2686 NVP-BSK805 2HCl NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2. Pan TYK2, IC50: 10.76 nM
S2902 S-Ruxolitinib (INCB018424) S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3. Pan TYK2, IC50: 19 nM
S2179 LY2784544 LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2. Pan TYK2, IC50: 44 nM
S8057 Pacritinib (SB1518) Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM, respectively. Phase 3. Pan TYK2, IC50: 50 nM
S2851 Baricitinib (LY3009104, INCB028050) Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3. Pan TYK2, IC50: 53 nM
S7605 Filgotinib (GLPG0634) Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2. Pan TYK2, IC50: 116 nM
S7036 XL019 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1. Pan TYK2, IC50: 348.3 nM
Tags: Tyk2 inhibitor | Tyk2 cancer | Tyk2 activity | Tyk2 phosphorylation | Tyk2 mutation