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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.
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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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Working concentration: mg/ml;

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

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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 2026-05-06)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01042379 RECRUITING
Breast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma; TNBC - Triple-Negative Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; Hormone Receptor Positive Tumor; Hormone Receptor Negative Tumor; Early-stage Breast Cancer; Locally Advanced Breast Cancer
QuantumLeap Healthcare Collaborative
2010-03-01 PHASE2
NCT06698965 RECRUITING
Lung Cancer, Small Cell
Shanghai Chest Hospital
2024-10-13 PHASE2
NCT07736001 NOT_YET_RECRUITING
Tumor Patients
Tianjin Medical University Cancer Institute and Hospital
2026-07
NCT05874401 RECRUITING
Extensive-stage Small-cell Lung Cancer
Pharmacosmos A/S
2023-10-18 PHASE4
NCT07679997 NOT_YET_RECRUITING
Head & Neck Squamous Cell Carcinoma
Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University
2026-06-01 PHASE2
NCT07160283 NOT_YET_RECRUITING
Biliary Tract Neoplasms; Pancreatic Neoplasms
The Second Affiliated Hospital of Shandong First Medical University
2025-09-01 PHASE2

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