Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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1 mg | 在庫あり | ¥ 7,500 | |||
2 mg | 在庫あり | ¥ 10,000 | |||
5 mg | 在庫あり | ¥ 16,500 | |||
10 mg | 在庫あり | ¥ 28,000 | |||
25 mg | 在庫あり | お問い合わせ | |||
50 mg | 在庫あり | お問い合わせ |
説明 | 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. |
ターゲット&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. |
別名 | G1T38 dihydrochloride |
分子量 | 547.52 |
分子式 | C26H36Cl2N8O |
CAS No. | 2097938-59-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 1mg/ml, Sonication is recommended.
H2O: 4 mg/mL (7.31 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Lerociclib dihydrochloride 2097938-59-3 Cell Cycle/Checkpoint CDK Inhibitor G1T38 Dihydrochloride G1T38 dihydrochloride Lerociclib Dihydrochloride inhibit G1T38 Lerociclib Cyclin dependent kinase inhibitor