Home Cell Cycle CDK inhibitor Trilaciclib

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Trilaciclib CDK inhibitor

Trilaciclib is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. This compound inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively.

Trilaciclib CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 446.55

Purity & Quality Control

Chemical Information

Molecular Weight 446.55 Formula

C24H30N8O
CAS No. 1374743-00-6 SDF --
Synonyms G1T28, G1T28-1
Smiles CN1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6

Storage and Stability

Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 2 mg/mL ( (4.47 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Mechanism of Action

Targets
CDK4/cyclin D1 [1]
(Cell-free assay)		 CDK6/cyclin D3 [1]
(Cell-free assay)
1 nM 4 nM

In vitro
In vitro

Trilaciclib 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, this compound protects RB competent cells from damage by chemotherapy as assessed by gamma-H2A.X (γH2AX) and apoptosis through caspase 3/7 activation.[1]
Cell Research 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 this compound 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.

In Vivo
In vivo

In vivo, this compound regulates the proliferation of HSPCs in both mouse and canine bone marrow, in a reversible, doseand time-dependent manner. Pretreatment of mice with this compound allows a faster recovery of complete blood counts (CBCs) following chemotherapy. In addition, it does not protect RB deficient tumors from chemotherapy but, instead, adds to the anti-tumor effect.[1]
Animal Research Animal Models 8-week-old female FVB mice
Dosages 50 mg/kg, 100 mg/kg, 150 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05113966 Active not recruiting
Triple Negative Breast Cancer
G1 Therapeutics Inc.
 November 22 2021 Phase 2
NCT02978716 Terminated
Triple-Negative Breast Neoplasms|Breast Neoplasm|Breast Cancer|Triple-Negative Breast Cancer
G1 Therapeutics Inc.
 February 2 2017 Phase 2
NCT02514447 Terminated
Small Cell Lung Cancer
G1 Therapeutics Inc.
 October 5 2015 Phase 1|Phase 2
NCT02243150 Completed
Healthy Volunteers
G1 Therapeutics Inc.
 September 2014 Phase 1

References
  • https://pubmed.ncbi.nlm.nih.gov/26826116/
  • https://pubmed.ncbi.nlm.nih.gov/33004541/

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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