Product Details
Product Name:
TH-Z827 |
CAS No.:
2847881-81-4 |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | TH-Z827 |
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]. |
Storage | Shipping with blue ice. |
Inhibitors Related | Adagrasib | (S)-AMG-510 | BI-2493 | CCG-257081 | Ketoconazole | Deltarasin | MRTX1133 | Salirasib | RMC-6236 | (S)-(-)-Perillyl alcohol | CASIN | Sotorasib |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries, 10000+ Noval Small Molecucles,16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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