Trilaciclib (G1T28) - 98%, high purity , Cyclin-dependent kinase 6 inhibitor, CAS No.1374743-00-6, Cyclin-dependent kinase 6 inhibitor

Item Number

T413997

• Synonyms: BCP25013 | 2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one | trilaciclibum | UNII-U6072DO9XG | 4-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]spiro[1,3,5,11-t
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: 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.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Cyclin-dependent kinase 6 inhibitor

Product Description

Information

Trilaciclib (G1T28) 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.

Targets

CDK4/cyclin D1 (Cell-free assay); CDK6/cyclin D3 (Cell-free assay) 1 nM; 4 nM

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.

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.

Cell Research(from reference)

Cell lines：HS68 cells, WM2664 cells, A2058 cells 

Concentrations：10 nM, 30 nM, 100 nM, 300 nM, 1000 nM 

Incubation Time：4 h, 8 h, 16 h, 24 h