Trilaciclib hydrochloride

SKU: orb1308992

Description

Trilaciclib hydrochloride (G1T28 hydrochloride) is a potent and selective CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. It is widely used in preclinical research to investigate cell cycle arrest, chemoprotection, and antitumor efficacy in both in vitro and in vivo cancer models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1977495-97-8
• MW: 519.47
• Purity: 99.69%
• Formula: C₂₄H₃₂Cl₂N₈O
• SMILES: Cl.Cl.CN1CCN(CC1)c1ccc(Nc2ncc3cc4C(=O)NCC5(CCCCC5)n4c3n2)nc1
• Target: CDK
• Solubility: DMSO:Insoluble;H2O:10 mM

Bioactivity

• Target IC50:
  CDK6-CyclinD3:4 nM|CDK4-CyclinD1:1 nM
• In Vivo:
  G1T28 inhibits the phosphorylation of RB and induces an exclusive, reversible G1 arrest.n vivo, G1T28 reversibly and in a dose-dependent manner, regulates the proliferation of HSPCs.Pretreatment of mice with oral G1T28 allows for the faster recovery of CBCs following chemotherapy treatment.Likewise, oral G1T28 does not protect RB-deficient tumors from chemotherapy but adds to the antitumor effect.Although this effect was found in athymic mice that lack T lymphocytes, it is still possible that the enhanced efficacy is due to preservation of other immune cell types such as natural killer cells.
• In Vitro:
  Incubation with Trilaciclib hydrochloride (G1T28) for 24 hours can induce a strong G1 cell cycle arrest (time=0). Cells have re-entered the cell cycle and demonstrate cell-cycle kinetics similar to untreated control cells By 16 hours after Trilaciclib hydrochloride washout. These results demonstrate that Trilaciclib hydrochloride causes a transient, and reversible G1 arrest. A transient Trilaciclib hydrochloride-mediated G1 cell-cycle arrest in CDK4/6-sensitive cells decreases the in vitro toxicity of a variety of commonly used cytotoxic chemotherapy agents associated with myelosuppression.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cyclin dependent kinase, CDK, CDK4/Cyc D1, Cdk4/cyclin D1, cdk6/cyclin D3, CDK6/CyclinD3, Inhibitor, inhibit, G1T28, G1T28 Hydrochloride, G1T28 hydrochloride, Trilaciclib, Trilaciclib hydrochloride, Trilaciclib Hydrochloride

Compound Identifiers

PubChem CID

124081865