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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.

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Danusertib, CAS 827318-97-8

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Purity: 98%

Biological Description

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Storage & Solubility Information

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	RET:31 nM, Aurora A:13 nM, TrkA:31 nM, FGFR1:47 nM, Abl:25 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 2 years

Solubility Information

DMSO: 88 mg/mL (185.4 mM)

H2O: <1 mg/mL

Ethanol: <1 mg/mL

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

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.

Citations

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 Compound Library Preclinical Compound Library Autophagy Compound Library Anti-Lung Cancer Compound Library TGF-beta/Smad Compound Library Hematonosis Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library DNA Damage & Repair Compound Library Cell Cycle Compound Library

Related Products

Related compounds with same targets

Tripolin A CCT129202 SCH-1473759 L 888607 Racemate LY3295668 Centrinone-B Barasertib Aurora B inhibitor 1

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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.

Keywords

Danusertib 827318-97-8 表观遗传蛋白酪氨酸激酶凋亡细胞骨架细胞周期血管生成自噬 Aurora Kinase Autophagy Bcr-Abl c-RET FGFR Trk receptor inhibit PHA739358 PHA-739358 Inhibitor PHA 739358 inhibitor

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