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Table 1 CDK9 inhibitors

From: CDK9 inhibitors in acute myeloid leukemia

Agent Mode of Administration CDK Inhibition Profile (IC50) Development Stage/Indication
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: CLLa
Phase 2: AMLa, ALLa, B-cell CLLa, MCLa, MM
Phase 1: CLL, DLBCL, MM
LY2857785 [46] Intravenous CDK9: 11 nM
CDK8: 16 nM
CDK7: 246 nM
Preclinical
P276–00b [55, 56] Intravenous CDK9: 20 nM
CDK4: 63 nM
CDK1: 79 nM
CDK2: 224 nM
Phase 2: MCLa, 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
  1. ALL, acute lymphoblastic leukemia; AML, acute myeloid leukemia; CDK, cyclin-dependent kinase; CLL, chronic lymphocytic leukemia; CML, chronic myeloid leukemia; DLBCL, diffuse large B-cell lymphoma; IC50, half maximal inhibitory concentration; MCL, mantle cell lymphoma; MM, multiple myeloma; SLL, small lymphocytic lymphoma
  2. aStudy terminated
  3. bDevelopment discontinued