Table 1.
CDK2 inhibitors in clinical trials.
| Candidate Drug | Target (IC50) | Clinical Trials | References |
|---|---|---|---|
| Flavopiridol | CDK1 (30 nM), CDK2 (100 nM), CDK4 (20 nM), CDK6 (60 nM), CDK7 (10 nM), CDK9 (10 nM) |
Phase II | Kaur et al. [37] |
| P276-00 | CDK1 (110 nM), CDK2 (10 nM), CDK4 (130 nM), CDK9 (20 nM) |
Phase II | De Azevedo Jr. et al. [38]; Murthi et al. [39]; Joshi et al. [33] |
| Roscovitine | CDK1 (2.7 μM), CDK2 (0.7 μM), CDK7 (0.5 μM), CDK9 (0.8 μM) |
Phase II | McClue et al. [40]; Meijer et al. [41] |
| PHA-848125 AC | CDK1 (2 nM), CDK2 (3 nM), CDK4 (5 nM), CDK5 (4 nM) |
Phase II | Caporali et al. [42] |
| UCN-01 | CDK2 (42 nM), CDK4 (32 nM), CDK6 (58 nM) |
Phase II | Kawakami et al. [43]; Li et al. [44]; Senderowicz [45] |
| R547 | CDK1 (0.001 μM), CDK2 (0.003 μM), CDK4 (0.001 μM) |
Phase I/II | Chu et al. [46]; DePinto et al. [25] |
| AT-7519 | CDK1 (0.21 μM), CDK2 (0.047 μM), CDK4 (0.1 μM), CDK5 (0.13 μM), CDK6 (0.17 μM), CDK9 (≤0.01 μM) |
Phase I/II | Mahadevan et al. [47]; Squires et al. [48] |
| Dinaciclib | CDK1 (3 nM), CDK2 (1 nM), CDK5 (1 nM), CDK9 (4 nM) |
Phase I | Michael [49]; Parry et al. [50] |
| SNS-032 | CDK2 (38 nM), CDK7 (62 nM), CDK9 (4 nM) | Phase I | Tong et al. [51]; Conroy et al. [52] |
| RGB-286638 | CDK1 (2 nM), CDK2 (3 nM), CDK3 (5 nM), CDK4 (4 nM), CDK9 (1 nM) | Phase I | de Bruijn et al. [53]; van der Biessen et al. [54] |
| BAY-1000394 | CDK1, CDK2, CDK4 and CDK9 (≤11 nM) | Phase I | Siemeister et al. [55]; Siemeister et al. [56] |
| TG02 | CDK1 (9 nM), CDK2 (5 nM), CDK3 (8 nM), CDK5 (4 nM), CDK9 (3 nM) | Phase I | Poulsen et al. [57] |