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Angiogenesis FGFR Danusertib

Danusertib

Catalog No. T2094   CAS 827318-97-8
Synonyms: PHA-739358

Danusertib 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.

Danusertib, CAS 827318-97-8
Pack Size Availability Price/USD Quantity
2 mg In stock 79.00
5 mg In stock 121.00
10 mg In stock 219.00
25 mg In stock 411.00
50 mg In stock 658.00
1 mL * 10 mM (in DMSO) In stock 124.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description Danusertib 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 Abl :ic50 25nM,   Aurora A :ic50 13nM,   Aurora B :ic50 79nM,   Aurora C :ic50 61nM,   FGFR1 :ic50 47nM,   RET :ic50 31nM,   TrkA :ic50 31nM,  
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)
Cell lines: CD34+ cells
Animal Research
Animal Model: FeSCID mice
Synonyms PHA-739358
Purity 98.44%
Molecular Weight 474.55
Formula C26H30N6O3
CAS No. 827318-97-8

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 88 mg/mL (185.4 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL

Citations

References and Literature
1. Carpinelli P, et al. Mol Cancer Ther, 2007, 12 Pt 1, 3158-3168. 2. Fancelli D, et al. J Med Chem, 2006, 49(24), 7247-7251. 3. Gontarewicz A, et al. Blood, 2008, 111(8), 4355-4364.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Apoptosis Compound Library Autophagy Compound Library Epigenetics Compound Library Tyrosine kinase inhibitor library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Angiogenesis related Compound Library Cell cycle related Compound Library

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