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Lerociclib

Catalog No. T11345   CAS 1628256-23-4
Synonyms: G1T38

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 2nM, 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively.

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Lerociclib Chemical Structure
Lerociclib, CAS 1628256-23-4
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5 mg 8-10 weeks $ 198.00
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Biological Description
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Description Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 2nM, 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively.
Targets&IC50 cdk6/cyclin D3:2 nM, CDK5/p35:0.832 μM, cdk2/cyclin A:1.5 μM, CDK5/p25:1.2 μM, CDK1/cyclinB1:2.4 μM, CDK2/CyclinE:3.6 μM, Cdk4/cyclin D1:1 nM, CDK9/Cyclin T:28 nM, CDK7/Cyclin H/MAT1:2.4 μM
In vitro Lerociclib produces a robust and sustained G1 arrest in CDK4/6 dependent cells with an EC50 of ~20 nM.?A dose dependent increase of cells in the G1 phase of the cell cycle is observed when CDK4/6 dependent WM2664 cells are treated with Lerociclib for 24 hours.?This arrest is maintained through 300 nM, more than 300x the biochemical IC50.?WM2664 cells treated with 30-1000 nM of Lerociclib for 24 hours exhibits a complete inhibition of RB phosphorylation compared to vehicle controls.?Treatment with Lerociclib reduces RB phosphorylation within 1 hour post-treatment and generates near complete inhibition of RB phosphorylation by 16 hours post-treatment.?Lerociclib produces a robust inhibition of proliferation in a diverse array of tumor cell lines including breast, melanoma, leukemia and lymphoma with EC50 concentrations as low as 23 nM.Within the CDK family, Lerociclib is least selective against CDK9/cyclin T, ~30 fold between CDK4/cyclin D1 and CDK9/ cyclin T at the biochemical IC50.
In vivo In this HER2+ breast cancer model, Mice treated with Lerociclib elicits 8% tumor regression after 21 days of treatment while control animals have a 577% increase in tumor burden over the same treatment period.?Compared to the vehicle-treated mice, daily treatment with 100 mg/kg of Lerocyclib or palbociclib shows tumor regression within 10 days in the MCF7 xenograft model.?After 27 days of treatment, tumor growth inhibition is observed in the 10, 50, and 100 mg/kg Lerociclib cohorts (approximately 12%, 74%, and 90% inhibition, respectively).?Daily oral palbociclib treatment causes an 18%, 66%, and 87% tumor growth inhibition in the 10, 50, and 100 mg/kg dosage cohorts, respectively.
Synonyms G1T38
Molecular Weight 474.6
Formula C26H34N8O
CAS No. 1628256-23-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Bisi JE, et al. Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors. Oncotarget. 2017 Jun 27;8(26):42343-42358.

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Keywords

Lerociclib 1628256-23-4 Cell Cycle/Checkpoint CDK G1T38 inhibitor inhibit

 

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