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Danusertib

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

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Danusertib Chemical Structure
Danusertib, CAS 827318-97-8
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
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Purity: 98.44%
Purity: 98.20%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)

TargetMolReferences 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.

TargetMolCitations

1. Cheng S, Jin P, Li H, et al. Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model. Frontiers in Pharmacology. 2021: 2866.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Metabolism Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-Aging Compound Library Drug Repurposing Compound Library Target-Focused Phenotypic Screening Library

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N-Desmethyl imatinib Nocodazole Imatinib AN-019 BCR-ABL-IN-8 Flumatinib mesylate PP121 PHA-665752

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Keywords

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

 

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