G1T38

For research use only.

Catalog No.S8568 Synonyms: Lerociclib

G1T38 Chemical Structure

CAS No. 1628256-23-4

G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.

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EUR 95 3 months
EUR 164 3 months

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Biological Activity

Description G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.
Targets
CDK4 [1]
(Cell-free assay)
CDK6 [1]
(Cell-free assay)
CDK9 [1]
(Cell-free assay)
1 nM 2 nM 28 nM
In vitro

G1T38 is highly potent and selective for CDK4/cyclin D1 and CDK6/cyclin D3 over CDK1, CDK2, CDK5 and CDK7 and their respective binding partners. In vitro, G1T38 decreases RB1 (RB) phosphorylation, causes a precise G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines including breast, melanoma, leukemia, and lymphoma cells with EC50 concentrations as low as 23 nM[1].

Assay
Methods Test Index PMID
Western blot
pRB(Ser807/811) / RB; 

PubMed: 28418845     


WM2664 cells treated with G1T38 for 24 hours show a dose-dependent decrease in RB phosphorylation with complete inhibition of RB phosphorylation at a 300 nM exposure. 

28418845
In vivo

In vivo, G1T38 treatment leads to equivalent or improved tumor efficacy compared to the first-in-class CDK4/6 inhibitor, palbociclib, in an ER+ breast cancer xenograft model. Furthermore, G1T38 accumulates in mouse xenograft tumors but not plasma, resulting in less inhibition of mouse myeloid progenitors than after palbociclib treatment. In larger mammals, this difference in pharmacokinetics allows for 28 day continuous dosing of G1T38 in beagle dogs without producing severe neutropenia[1].

Protocol

Cell Research:

[1]

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  • Cell lines: WM2664 cells
  • Concentrations: 300 nM
  • Incubation Time: 1, 4, 8, 16, and 24 hours
  • Method:

    --


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: C57BL/6 mice
  • Dosages: 100 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 2 mg/mL (4.21 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 474.60
Formula

C26H34N8O

CAS No. 1628256-23-4
Storage powder
in solvent
Synonyms Lerociclib
Smiles CC(C)N1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03455829 Active not recruiting Drug: G1T38|Drug: Osimertinib Carcinoma Non-Small-Cell Lung|Lung Cancer|Non-small Cell Lung Cancer G1 Therapeutics Inc. March 29 2018 Phase 1|Phase 2
NCT02983071 Active not recruiting Drug: G1T38|Drug: Fulvestrant Carcinoma Ductal Breast|Breast Cancer|Breast Neoplasm G1 Therapeutics Inc. January 2017 Phase 1|Phase 2
NCT02821624 Completed Drug: G1T38 (CDK 4/6 Inhibitor)|Drug: Placebo Healthy Volunteers G1 Therapeutics Inc. May 2016 Phase 1

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

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID