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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
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]. |
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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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