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Lerociclib dihydrochloride

Catalog No. T11345L CAS 2097938-59-3

Synonyms: G1T38 dihydrochloride

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

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Lerociclib dihydrochloride Chemical Structure

Lerociclib dihydrochloride, CAS 2097938-59-3

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2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
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Purity: 99.42%

Biological Description

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Storage & Solubility Information

Description	Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 2 nM and 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively.
Targets&IC50	CDK6-CyclinD3:2 nM, CDK5-p35:832 nM, CDK2-CyclinA:1.5 μM, CDK5-p25:1.2 μM, CDK1-CyclinB1:, CDK2-CyclinE:3.6 μM, CDK4-CyclinD1:1 nM, CDK9-CyclinT:28 nM
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 G1T38 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 G1T38 reduces RB phosphorylation within 1 hour post-treatment and generates near complete inhibition of RB phosphorylation by 16 hours post-treatment. G1T38 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, Lerocyclib 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 Lerociclib 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 dihydrochloride
Molecular Weight	547.52
Formula	C26H36Cl2N8O
CAS No.	2097938-59-3

Storage

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

Solubility Information

H2O: 4 mg/mL (7.31 mM), Sonication is recommended.

References 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Prostate Cancer Compound Library Clinical Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library

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Keywords

Lerociclib dihydrochloride 2097938-59-3 Cell Cycle/Checkpoint CDK Inhibitor G1T38 Dihydrochloride G1T38 dihydrochloride Lerociclib Dihydrochloride inhibit G1T38 Lerociclib Cyclin dependent kinase inhibitor

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