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TH-Z827

Catalog No. T79092 CAS 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].

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TH-Z827, CAS 2847881-81-4

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

TH-Z827 2847881-81-4 GPCR/G Protein MAPK Ras inhibitor inhibit

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