| Description | Trilaciclib (G1T28, G1T28-1) is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively. | ||||
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| In vitro | G1T28 is a potent and selective CDK4/6 inhibitor that inhibits the phosphorylation of RB and induces an exclusive, reversible G1 arrest. In vitro and in vivo, G1T28 protects RB competent cells from damage by chemotherapy as assessed by gamma-H2A.X (γH2AX) and apoptosis through caspase 3/7 activation.[1] | ||||
| In vivo | In vivo, G1T28 regulates the proliferation of HSPCs in both mouse and canine bone marrow, in a reversible, doseand time-dependent manner. Pretreatment of mice with G1T28 allows a faster recovery of complete blood counts (CBCs) following chemotherapy. In addition, G1T28 does not protect RB deficient tumors from chemotherapy but, instead, adds to the anti-tumor effect.[1] |
Selleck Chemicals提供了超过120,000种用于细胞信号通路研究的抑制剂。我们积极跟踪最新科学，因此我们的客户可以依靠我们成为最新抑制剂的领先供应商。
Selleck的生物活性化合物库由8,000多个具有经过验证的生物学和药理活性的小分子组成。这些分子的安全性和有效性已通过临床前和临床研究证明，其中许多是FDA批准的化合物。
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