Table 1 CDK9 inhibitors

Alvocidib (flavopiridol) [47, 48]

Intravenous

CDK9: 6 nM

CDK4: 10 nM

CDK7: 23 nM

CDK11: 57 nM

CDK5: 110 nM

Phase 2: AML, ALL, CLL, DLBCL, MCL, MM, various lymphomas

Phase 1: AML, ALL, B-cell CLL, CML, MCL, SLL, various lymphomas

AT7519 [49]

Intravenous

CDK9: <  10 nM CDK5: 13 nM

CDK2: 47 nM

CDK4: 100 nM

CDK6: 179 nM

Phase 2: CLL, MCL

BAY 1143572 [50]

Oral

Not published

Phase 1: AML, ALL, DLBCL

CDKI-73 (LS-007) [51, 52]

Intravenous, oral

CDK2: 3 nM

CDK9: 6 nM

CDK1: 8 nM

CDK4: 8 nM

CDK6: 37 nM

CDK7: 134 nM

Preclinical

Dinaciclib [53, 54]

Intravenous

CDK2: 1 nM

CDK5: 1 nM

CDK1: 3 nM

CDK9: 4 nM

Phase 3: CLL^a

Phase 2: AML^a, ALL^a, B-cell CLL^a, MCL^a, MM

Phase 1: CLL, DLBCL, MM

LY2857785 [46]

Intravenous

CDK9: 11 nM

CDK8: 16 nM

CDK7: 246 nM

Preclinical

P276–00^b [55, 56]

Intravenous

CDK9: 20 nM

CDK4: 63 nM

CDK1: 79 nM

CDK2: 224 nM

Phase 2: MCL^a, MM

Phase 1: MM

SNS-032 (BMS-387032) [57, 58]

Intravenous

CDK9: 4 nM

CDK2: 38 nM

CDK7: 62 nM

Phase 1: CLL, MM

TG02 [59]

Oral

CDK9: 3 nM

CDK5: 4 nM

CDK2: 5 nM

CDK3: 8 nM

CDK1: 9 nM

CDK7: 37 nM

Phase 1: AML, CML, SLL