Trilaciclib (G1T28)

For research use only.

Catalog No.S8389 Synonyms: G1T28-1

Trilaciclib (G1T28) Chemical Structure

CAS No. 1374743-00-6

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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Biological Activity

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.
Targets
CDK4/cyclin D1 [1]
(Cell-free assay)
CDK6/cyclin D3 [1]
(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.[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]

Protocol

Cell Research:

[1]

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  • 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
  • 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. Membranes are blocked in LiCor Membrane Blocking Buffer and incubated overnight with rabbit anti-pRb (Ser807/811) antibody at a 1:1,000 dilution and mouse anti-MAPK antibody at a 1:2,000 dilution, as a loading control. Secondary antibodies (LiCor) are Goat anti- rabbit (680RD) and Goat antimouse (800CW) at a 1:15,000 dilution. Blots are incubated for one hour, washed and imaged using LiCor ImageStudio software.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: 8-week-old female FVB mice
  • Dosages: 50 mg/kg, 100 mg/kg, 150 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO Insoluble
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 446.55
Formula

C24H30N8O

CAS No. 1374743-00-6
Storage powder
in solvent
Synonyms G1T28-1
Smiles CN1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04863248 Recruiting Drug: Trilaciclib|Drug: Placebo|Drug: Docetaxel Metastatic Non-Small Cell Lung Cancer|NSCLC|Lung Cancer G1 Therapeutics Inc. April 16 2021 Phase 2
NCT02978716 Active not recruiting Drug: Trilaciclib|Drug: Gemcitabine|Drug: Carboplatin Triple-Negative Breast Neoplasms|Breast Neoplasm|Breast Cancer|Triple-Negative Breast Cancer G1 Therapeutics Inc. February 7 2017 Phase 2
NCT02514447 Active not recruiting Drug: Trilaciclib|Drug: Placebos|Drug: Topotecan Small Cell Lung Cancer G1 Therapeutics Inc. October 5 2015 Phase 1|Phase 2
NCT02243150 Completed Drug: G1T28-1 (CDK 4/6 Inhibitor)|Drug: Placebo Healthy Volunteers G1 Therapeutics Inc. September 2014 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID