Home Cell Cycle CDK inhibitor Trilaciclib

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Trilaciclib CDK inhibitor

Cat.No.S8389

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

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Quality Control

Batch: Purity: 99.55%
99.55

Solubility

In vitro
Batch:

DMSO : 2 mg/mL (4.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 446.55 Formula

C24H30N8O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1374743-00-6 -- Storage of Stock Solutions

Synonyms G1T28, G1T28-1 Smiles CN1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6

Mechanism of Action

Targets/IC50/Ki
CDK4/cyclin D1
(Cell-free assay)
1 nM
CDK6/cyclin D3
(Cell-free assay)
4 nM
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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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