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Trilaciclib

Cat. No. M10033
Trilaciclib Structure
Synonym:

G1T28; G1T-28

Size Price Availability Quantity
5mg USD 360  USD400 In stock
10mg USD 495  USD550 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Trilaciclib (G1T28) is a potent first-in-class reversible CDK4/6 inhibitor with IC50 of 1 nM and 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively. Trilaciclib (G1T28) protects RB competent cells from damage by chemotherapy as assessed by gamma-H2A.X (γH2AX) and apoptosis through caspase 3/7 activation in vitro and in vivo. In vivo, G1T28 regulates the proliferation of HSPCs in both mouse and canine bone marrow, in a reversible, doseand time-dependent manner.

Protocol
Cell Experiment
Cell lines HS68 cells, WM2664 cells, A2058 cells
Preparation 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.
Concentrations 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
Incubation time 4 h, 8 h, 16 h, 24 h
Animal Experiment
Animal models 8-week-old female FVB mice
Formulation 20% Solutol
Dosages 50 mg/kg, 100 mg/kg, 150 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 446.55
Formula C24H30N8O
CAS Number 1374743-00-6
Purity >99%
Solubility Slightly soluble in water
Slightly soluble in DMSO
Storage at -20°C
References

CDK4/6 inhibition enhances antitumor efficacy of chemotherapy and immune checkpoint inhibitor combinations in preclinical models and enhances T-cell activation in patients with SCLC receiving chemotherapy
Anne Y Lai, et al. J Immunother Cancer. 2020 Oct;8(2):e000847. PMID: 33004541.

Transient CDK4/6 inhibition protects hematopoietic stem cells from chemotherapy-induced exhaustion
Shenghui He, et al. Sci Transl Med. 2017 Apr 26;9(387):eaal3986. PMID: 28446688.

Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression
John E Bisi, et al. Mol Cancer Ther. 2016 May;15(5):783-93. PMID: 26826116.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Trilaciclib, G1T28; G1T-28 supplier, CDK, inhibitors

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