JAK kinase specificity profile and clinical trials of distinct TKIs
| Drug name . | IC50 (nM) . | Clinical trial . | Reference . | |||
|---|---|---|---|---|---|---|
| JAK1 . | JAK2 . | JAK3 . | TYK2 . | |||
| INCB18424 (Ruxolitinib) | 3.3 | 2.8 | 428 | 19 | FDA approved for MF; phase II for CML-BC; recruiting for phase I/II for CML under nilotinib treatment | 75 |
| TQ101348 (SAR302503) | 115 | 3 | 1002 | 405 | Phase I/II in MPN | 76 |
| CYT387 | 11 | 18 | 155 | NA | Phase I/II in MPN | 77 |
| SB1518 (Pacritinib) | 1280 | 23 | 520 | 50 | Phase II in MPN | 78 |
| CEP7O1 (Lestaurtinib) | NA | 0.9 | 3 | NA | Phase II in MPN | 79 |
| LY2784544 | NA | 3 | 48 | NA | Phase I ongoing in MPN | 80 |
| NS-018 | 33 | 1 | 39 | 22 | Phase I/II ongoing in MPN | 81 |
| AZD1480 | 1.3 | 0.3 | 3.9 | NA | Phase I/II ongoing in MPN | 82 |
| BMS-911543 | 356 | 1 | 73 | 66 | Phase I/II ongoing in MPN | 83 |
| LY3009104 (Baricitinib) | 5.9 | 5.7 | 560 | 53 | Phase II ongoing in rheumatoid arthritis | 84 |
| TG101209 | NA | 6 | 169 | NA | In vitro use only | 85 |
| JAK inhibitor 1 | 15 | 1 | 5 | 1 | In vitro use only | 86 |
| Drug name . | IC50 (nM) . | Clinical trial . | Reference . | |||
|---|---|---|---|---|---|---|
| JAK1 . | JAK2 . | JAK3 . | TYK2 . | |||
| INCB18424 (Ruxolitinib) | 3.3 | 2.8 | 428 | 19 | FDA approved for MF; phase II for CML-BC; recruiting for phase I/II for CML under nilotinib treatment | 75 |
| TQ101348 (SAR302503) | 115 | 3 | 1002 | 405 | Phase I/II in MPN | 76 |
| CYT387 | 11 | 18 | 155 | NA | Phase I/II in MPN | 77 |
| SB1518 (Pacritinib) | 1280 | 23 | 520 | 50 | Phase II in MPN | 78 |
| CEP7O1 (Lestaurtinib) | NA | 0.9 | 3 | NA | Phase II in MPN | 79 |
| LY2784544 | NA | 3 | 48 | NA | Phase I ongoing in MPN | 80 |
| NS-018 | 33 | 1 | 39 | 22 | Phase I/II ongoing in MPN | 81 |
| AZD1480 | 1.3 | 0.3 | 3.9 | NA | Phase I/II ongoing in MPN | 82 |
| BMS-911543 | 356 | 1 | 73 | 66 | Phase I/II ongoing in MPN | 83 |
| LY3009104 (Baricitinib) | 5.9 | 5.7 | 560 | 53 | Phase II ongoing in rheumatoid arthritis | 84 |
| TG101209 | NA | 6 | 169 | NA | In vitro use only | 85 |
| JAK inhibitor 1 | 15 | 1 | 5 | 1 | In vitro use only | 86 |
NA, not available.