
NSC305787 NEW
Price | $347 | $1140 | $1490 |
Package | 5mg | 25mg | 50mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2025-05-08 |
Product Details
Product Name: NSC305787 | CAS No.: 785718-37-8 |
Purity: 99.40% | Supply Ability: 10g |
Release date: 2025/05/08 |
Product Introduction
Bioactivity
Name | NSC305787 |
Description | NSC305787 is an ezrin inhibitor with antitumor activity, inhibits PKCΙ-induced ezrin phosphorylation, reduces β2AR expression in the cell membrane, and induces intracellular vesicular or punctate expression of ezrin and β2AR, and can be used to study pancreatic cancer. |
In vitro | NSC305787 is a small molecule inhibitor that specifically targets ezrin with a binding dissociation constant (Kd) of 5.85 μM and shows significant anti-tumor effects. The compound exhibited different inhibitory activities by inhibiting the phosphorylation of ezrin, moesin, radixin, and MBP by PKCI with IC50 values of 8.3 μM, 9.4 μM, 55 μM, and 58.9 μM, respectively.Although NSC305787 was also bound to PKCI (Kd=172.4 μM), it inhibited ezrin mainly through direct binding to ezrin. Although NSC305787 also binds to PKCI (Kd=172.4 μM), it mainly inhibits the phosphorylation of ezrin T567 by directly binding to ezrin, rather than by blocking PKCI kinase activity. In cellular assays, NSC305787 significantly inhibited the ezrin-mediated invasion of K7M2 osteosarcoma cells at concentrations of 1 μM and 10 μM. In addition, NSC305787 was able to reduce the cell motility phenotype in zebrafish at a concentration of 10 μM and effectively blocked the metastatic growth of osteosarcoma in lung organ culture. [1] |
In vivo | In in vivo experiments, NSC305787 (0.240 mg/kg/day, intraperitoneal injection) significantly inhibited the growth of ezrin-dependent osteosarcoma metastases in the lungs of mice. [1] In a transgenic osteosarcoma mouse model (Osx-Cre+p53fl/flpRBfl/fl), NSC305787 (240 μg/kg, intraperitoneal injection) also significantly inhibited lung metastasis while demonstrating superior pharmacokinetic properties to NSC305787. [2] |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 4 mg/mL (8.98 mM), Sonication and heating are recommended. |
Keywords | NSC-305787 | NSC305787 | NSC 305787 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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TargetMol Chemicals Inc.
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TargetMol Chemicals Inc.
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- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, USA
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