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TH-Z827
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Catalog No. T79092Cas No. 2847881-81-4
TH-Z827 is a mutant-selective inhibitor targeting KRAS(G12D) with an IC50 of 2.4 μM, demonstrating specificity by not binding to KRAS(WT) or KRAS(G12C). Additionally, it disrupts the KRAS(G12D)-CRAF interaction with an IC50 of 42 μM [1].
TH-Z827
😃Good
Catalog No. T79092Cas No. 2847881-81-4
TH-Z827 is a mutant-selective inhibitor targeting KRAS(G12D) with an IC50 of 2.4 μM, demonstrating specificity by not binding to KRAS(WT) or KRAS(G12C). Additionally, it disrupts the KRAS(G12D)-CRAF interaction with an IC50 of 42 μM [1].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | Inquiry | 8-10 weeks | 8-10 weeks | |
| 50 mg | Inquiry | 8-10 weeks | 8-10 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | TH-Z827 is a mutant-selective inhibitor targeting KRAS(G12D) with an IC50 of 2.4 μM, demonstrating specificity by not binding to KRAS(WT) or KRAS(G12C). Additionally, it disrupts the KRAS(G12D)-CRAF interaction with an IC50 of 42 μM [1]. |
| Targets&IC50 | KRas (G12D):2.4 μM |
| In vitro | In two pancreatic cancer cell lines bearing the KRAS G12D mutation (PANC-1 and Panc 04.03), TH-Z827 exhibited anti-proliferative effects with IC50 values of 4.4 and 4.7 μM, respectively. Treatment with TH-Z827 also resulted in reduced levels of pERK and pAKT in both PANC-1 and Panc 04.03 cells, confirming its ability to inhibit the activation of the MAPK and PI3K/mTOR signaling pathways [1]. |
| In vivo | BALB/c nude mice were subcutaneously inoculated with Panc 04.03 cells and C57BL/6 mice with KPC cells. Within the nude mouse model, TH-Z827 (10-30mg/kg) significantly reduced tumor volume in a dose-dependent manner. However, intraperitoneal administration of 30mg/kg TH-Z827 resulted in observed weight loss, indicating potential off-target effects [1]. |
| Molecular Weight | 498.66 |
| Formula | C30H38N6O |
| Cas No. | 2847881-81-4 |
| Smiles | O(C[C@H]1N(C)CCC1)C2=NC(=C3C(CN(CC3)C=4C5=C(C=CC4)C=CC=C5C)=N2)N6C7CCC6CNC7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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
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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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