Table 3.
CDK9 Inhibitors in Clinical Trials.
| Clinical Trials |
||||
|---|---|---|---|---|
| Name | Additional Targets | Phase | Tumors* | IC50 (nM)** |
| Flavopiridol | CDK1, CDK2, CDK4, CDK6, CDK7, CDK9, GSK3β35,83 | II | AML56; PPC57; CLL58 | AML: 40084; Ov202: 10085; B-CLL: 10086 |
| I | RMM64; NHL65; CLL63,69; AML70; ALL70; ABLs70 | U266: 1087; RPMI-8226: 1087; JeKo-1: 7088; Molt-4: 10089; K562: 35089 | ||
| Dinaciclib | CDK1, CDK2, CDK5, CDK983,89 | II | ABC71; NSLC72; AML73; ALL73; | Breast: 890; Lung: 6–1490; Leukemia: 690; |
| I | CLL74; RMM76 | J558: 291 | ||
| Seliciclib | CDK1, CDK2, CDK5, CDK7, CDK9, CK1, GSK3A, DIRK1A,ERK183 | I | SAT78,79 | Mean: 740092 |
| SNS-032 | CDK1, CDK2, CDK4, CDK7, CDK983 | I | SAT80; CLL81; RMM81 | Leukemia:13993 |
| RGB-286638 | CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK982,83 | I | SAT82 | Myeloma: 10094 |
*
AML: Acute myelogenous leukemia; PPC: Primary peritoneal carcinoma; CLL: Chronic lymphocytic leukemia; RMM: Relapsed multiple myeloma; NHL: Non-Hodgkin's lymphoma; ALL: Acute lymphoblastic leukemia; ABLs: Acute byphenotypic leukemias; ABC: Advanced breast cancer; NSLC: Non-small cell lung cancer; SAT: Solid advanced tumors.
**
Half maximal inhibitory concentration of each drug against the cell lines indicated and expressed in nM.