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Lerociclib
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Catalog No. T11345Cas No. 1628256-23-4
Alias G1T-38, G1T38, G1T 38
Lerociclib (G1T38) is a selective and highly potent CDK4/6 inhibitor with anticancer and antitumor activity, inhibits CDK4/CyclinD1 and CDK6/CyclinD3, and inhibits tumor growth in an animal model of endocrine-resistant breast cancer. Due to the poor solubility, for animal studies, the salt form T11345L is recommended.
Lerociclib
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Purity: 99%
Catalog No. T11345Alias G1T-38, G1T38, G1T 38Cas No. 1628256-23-4
Lerociclib (G1T38) is a selective and highly potent CDK4/6 inhibitor with anticancer and antitumor activity, inhibits CDK4/CyclinD1 and CDK6/CyclinD3, and inhibits tumor growth in an animal model of endocrine-resistant breast cancer. Due to the poor solubility, for animal studies, the salt form T11345L is recommended.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $32 | - | In Stock | |
| 5 mg | $73 | - | In Stock | |
| 10 mg | $123 | - | In Stock | |
| 25 mg | $232 | - | In Stock | |
| 50 mg | $372 | - | In Stock | |
| 100 mg | $548 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99%
Appearance:Solid
Color:Yellow
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Product Introduction
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Chemical Properties
Storage & Solubility Information
| Description | Lerociclib (G1T38) is a selective and highly potent CDK4/6 inhibitor with anticancer and antitumor activity, inhibits CDK4/CyclinD1 and CDK6/CyclinD3, and inhibits tumor growth in an animal model of endocrine-resistant breast cancer. Due to the poor solubility, for animal studies, the salt form T11345L is recommended. |
| Targets&IC50 | CDK5-p35:0.832 μM, Cdk4-CyclinD1:1 nM, CDK2-CyclinE:3.6 μM, CDK6-CyclinD3:2 nM, CDK1-cyclinB1:2.4 μM, CDK7-CyclinH-MAT1:2.4 μM, CDK2-CyclinA:1.5 μM, CDK4/6 dependent cells:20 nmol/L (EC50), CDK5-p25:1.2 μM, CDK9-CyclinT:28 nM |
| In vitro | Lerociclib is highly potent and selective for CDK4/cyclin D1 and CDK6/cyclin D3 over CDK1, CDK2, CDK5 and CDK7 and their respective binding partners. Lerociclib produced a robust and sustained G1 arrest in CDK4/6 dependent cells with an EC50 of ~20 nmol/L. [1] |
| In vivo | To evaluate the murine PK/PD relationship of Lerociclib, an ER+ MCF7 xenograft model was utilized. Compound concentrations were measured in plasma and tumors from tumor-bearing mice given a single oral dose of Lerociclib (100 mg/kg). Oral Lerociclib has sufficient mouse PK/PD for assessing efficacy in tumor models. [1] |
| Synonyms | G1T-38, G1T38, G1T 38 |
| Molecular Weight | 474.6 |
| Formula | C26H34N8O |
| Cas No. | 1628256-23-4 |
| Smiles | O=C1NCC2(N3C=4N=C(N=CC4C=C13)NC5=NC=C(C=C5)N6CCN(CC6)C(C)C)CCCCC2 |
| Relative Density. | 1.41 g/cm3 (Predicted) |
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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