Danusertib NEW
| Price | $54 | $77 | $118 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Danusertib | CAS No.: 827318-97-8 |
| Purity: 98.44% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Danusertib |
| Description | Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed. |
| Cell Research | For short-term expansion assays, 1 × 103 CD34+ cells are plated in triplicates in 96-well plates containing 100 μL of serum-free medium per well supplemented with human stem-cell factor (100 ng/mL), human Flt-3 Ligand (100 ng/mL), human thrombopoietin (50 ng/mL), human interleukin-3 and -6 (IL-3 and IL-6, respectively, both 20 ng/mL), and granulocyte colony-stimulating factor (20 ng/mL) along with Danusertib at the indicated concentrations. After 5 days, an additional 100 μL of cytokine and Danusertib containing medium are added. Cell numbers within each individual well are estimated on days 3, 6, and 9 or on days 3, 6, and 12 for healthy donor samples. (Only for Reference) |
| Kinase Assay | Biochemical kinase Assays: The Km values for ATP and the specific substrate are initially determined, and each assay is then run at optimized ATP (2Km) and substrate (5Km) concentrations. This setting enabled direct comparison of IC50 values of Danusertib across the applied kinase selectivity screening panel for the evaluation of the selectivity profile. |
| In vitro | Danusertib significantly inhibits the proliferation of K562 cells and suppresses tumor growth over a 10-day treatment period. Administering 25 mg/kg of Danusertib (b.d.i.v.) to HL-60 xenograft rats resulted in a 75% inhibition of tumor growth, with complete regression observed in one animal. |
| In vivo | In cellular assays, treatment with Danusertib in wild-type and p53-deficient mouse embryonic fibroblasts (MEFs) resulted in the arrest of wild-type cells in mitosis (4N) for up to 48 hours, whereas p53-deficient cells did not exhibit arrest at the 4N DNA stage and proceeded through mitosis, leading to DNA content >8N. Danusertib treatment was associated with increased levels of p53 protein and an upregulation of p21 protein, which is known to be transcriptionally regulated by p53. Additionally, Danusertib inhibited the activity of other kinases, such as FGFR1, Abl, Ret, and Trka, with IC50 values of 47 nM, 25 nM, 31 nM, and 31 nM, respectively. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 88 mg/mL (185.4 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| Keywords | inhibit | PHA 739358 | Autophagy | Danusertib | PHA739358 | Inhibitor | Aurora Kinase |
| Inhibitors Related | Stavudine | Xylitol | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Ferulic Acid | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
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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