Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 54.00 | |
2 mg | In stock | $ 77.00 | |
5 mg | In stock | $ 118.00 | |
10 mg | In stock | $ 198.00 | |
25 mg | In stock | $ 385.00 | |
50 mg | In stock | $ 585.00 | |
100 mg | In stock | $ 836.00 | |
500 mg | In stock | $ 1,690.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 123.00 |
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. |
Targets&IC50 | TrkA:31 nM, Aurora A:13 nM, Abl:25 nM, FGFR1:47 nM, RET:31 nM |
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. |
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) |
Synonyms | PHA-739358 |
Molecular Weight | 474.55 |
Formula | C26H30N6O3 |
CAS No. | 827318-97-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 88 mg/mL (185.4 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Danusertib 827318-97-8 Angiogenesis Apoptosis Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling Tyrosine Kinase/Adaptors FGFR Trk receptor c-RET Aurora Kinase Bcr-Abl inhibit PHA-739358 PHA 739358 PHA739358 Inhibitor inhibitor