flavopiridol |
Inhibits CDK 2, 4, 6, 9 |
G1/S arrest |
Phase I/II (hematologic and several solid tumors) |
Roscovitine |
Inhibits cyclinE/CDK2, cyclinB/CDK1, cyclinH/CDK7, cyclinT1/CDK9; p53 activation, NF-κB, decreases Mcl-1 |
S/G2/M arrest |
Phase I/II (solid tumors) |
E7070 |
Inhibits CDK2, cyclin E |
G1/S progression |
Phase I/II (several solid tumors, melanoma) |
SNS-032 |
Inhibits CDK 2, 7, 9, VEGF |
Inhibits progression and transcription, angiogenesis |
Phase I (advanced B-cell lymphomas, several solid tumors) |
bryostatin-1 |
Affects protein kinase C, CDK2; induces p21 |
Cell cycle modulation |
Phase I/II (combination therapy for hematologic and several solid tumors) |
AZD5438 |
Inhibits CDK1, 2, 9 |
Affects all phases of cell cycle |
Trials terminated dues to safety concerns |