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Trilaciclib (G1T28) is a potent first-in-class reversible CDK4/6 inhibitor with IC50 of 1 nM and 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively. Trilaciclib (G1T28) protects RB competent cells from damage by chemotherapy as assessed by gamma-H2A.X (γH2AX) and apoptosis through caspase 3/7 activation in vitro and in vivo. In vivo, G1T28 regulates the proliferation of HSPCs in both mouse and canine bone marrow, in a reversible, doseand time-dependent manner.
| Cell Experiment | |
|---|---|
| Cell lines | HS68 cells, WM2664 cells, A2058 cells |
| Preparation method | HS68, WM2664 and A2058 cells are treated with 300 nM G1T28 or DMSO (0.1%), for 4, 8, 16 or 24 hours. Whole cell extracts are prepared using 1× radioimmunoprecipitation assay buffer (RIPA) containing 1× HALT protease and phosphatase inhibitors. Total protein concentration is determined by using the bicinchoninic acid (BCA) Protein Assay Kit, according to manufacturer's instructions. Fifteen micrograms of protein is heat denatured for 10 minutes at 70 ℃ and resolved by Novex NuPAGE SDS-PAGE gel system and transferred to 0.45 μm nitrocellulose membrane by electroblotting. |
| Concentrations | 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM |
| Incubation time | 4 h, 8 h, 16 h, 24 h |
| Animal Experiment | |
|---|---|
| Animal models | 8-week-old female FVB mice |
| Formulation | 20% Solutol |
| Dosages | 50 mg/kg, 100 mg/kg, 150 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 446.55 |
| Formula | C24H30N8O |
| CAS Number | 1374743-00-6 |
| Solubility (25°C) | Slightly soluble in water Slightly soluble in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CDK Products |
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AT7519 is a novel small molecule multi-cyclin-dependent (CDK) kinase inhibitor. |
| Flavopiridol
Flavopiridol (Alvocidib) is a competitive broad-spectrum CDK inhibitor with IC50 of 30,170,100 nM against CDK1, CDK2 and CDK4, respectively. |
| R547
R547 is a potent and selective ATP-competitive CDK inhibitor, with Ki values of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively. |
| JNJ-7706621
JNJ-7706621 is a dual cell cycle inhibitor with activity against cyclin-dependent kinases (CDK1, 2, 3, 6) with an IC50 of 3-175 nM and Aurora kinases (A and B) with an IC50 of 11-15 nM respectively. |
| PD 0332991 HCL
PD-0332991 HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. |
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