Lerociclib
Based on 2 publication(s) in Google Scholar
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
For research use only. We do not sell to patients.
- Purity: 96.42%
- CAS No.: 1628256-23-4
- Formula: C26H34N8O
- Molecular Weight:474.60
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Lerociclib
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Biological Activity
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cdk2/cyclin A 1.5 μM (IC50) |
CDK2/cyclinE 3.6 μM (IC50) |
Cdk4/cyclin D1 1 nM (IC50) |
cdk6/cyclin D3 2 nM (IC50) |
CDK9/Cyclin T 28 nM (IC50) |
CDK5/p35 0.832 μM (IC50) |
CDK1/cyclinB1 2.4 μM (IC50) |
CDK7/Cyclin H/MAT1 2.4 μM (IC50) |
Cdk5/p25 1.2 μM (IC50) |
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. 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1628256-23-4
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Appearance Solid
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Molecular Weight 474.60
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Formula C26H34N8O
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Color Yellow to brown
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SMILES
O=C1NCC2(N3C1=CC4=CN=C(NC5=NC=C(N6CCN(C(C)C)CC6)C=C5)N=C43)CCCCC2
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Synonyms
G1T38
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
CDK4/6 inhibition overcomes venetoclax resistance mechanisms with enhanced combination activity in acute myeloid leukemia. [Abstract]2025 Dec 29:102526. PMID: 41468895 -
Solvent & Solubility
DMSO : 7.14 mg/mL (15.04 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.71 mg/mL (1.50 mM); Clear solution
This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.71 mg/mL (1.50 mM); Clear solution
This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
SupT1, Daudi, MCF7, ZR-75-1, A2058, WM2664, and H69 cells are seeded at 1000 cells per well; MV-4-11 and BV173 cells are plated at 4000 cells per well; Tom-1 cells are plated at 8,000 cells per well; NALM-1 cells are plated at 20,000 cells per well in Costar 3903 96 well plates. After 24 hours, plates are dosed with Lerociclib (G1T38) at a nine-point dose concentration from 10 μM to 1 nM. Cell viability is determined after four or six days. Plates are processed on BioTek Synergy2 multi-mode plate reader and data analyzed using GraphPad Prism 5 statistical software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female MMTV-NEU mice are used to test the efficacy of Lerocyclib (G1T38) (100 mpk, medicated diet). At time of treatment, body composition is assessed and weight measurements (in grams) are recorded and used as a measure of gross toxicity. Female nude mice are implanted with NSCLC PDX CTG0159 tumor. Mice are then randomized into treatment groups and dosing initiated once tumors reached a volume that fell within the range of 150-300 mm3. 100 mg/kg Lerociclib (G1T38) or vehicle is orally administered for 28 consecutive days. Female NCI Ath/nu mice are implanted with H1975 NSC lung adenocarcinoma model. Once tumors reach an average size of 100-150 mm3, mice are randomized into treatment cohorts. Mice are orally administered daily afatinib (20 mg/kg), erlotinib (70 mg/kg), or Lerociclib (50 or 100 mg/kg), as single agents or in combination (Lerociclib+erlotinib or Lerociclib+afatinib) for the duration of the study. All tumors are measured twice weekly until mice reach tumor burden of 1500 mm3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1070 mL | 10.5352 mL | 21.0704 mL | 52.6759 mL |
| 5 mM | 0.4214 mL | 2.1070 mL | 4.2141 mL | 10.5352 mL | |
| 10 mM | 0.2107 mL | 1.0535 mL | 2.1070 mL | 5.2676 mL | |
| 15 mM | 0.1405 mL | 0.7023 mL | 1.4047 mL | 3.5117 mL |
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