Danusertib
Based on 8 publication(s) in Google Scholar
Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.68%
- No. CAS: 827318-97-8
- Fòrmula: C26H30N6O3
- Peso molecular:474.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Danusertib
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Biochem Pharmacol. 2024 May:223:116155. [Abstract]
- Mol Cancer Ther. 2020 Aug;19(8):1751-1760. [Abstract]
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
- Patent. US20210299273A1.
- Patent. US20180263995A1.
- Technical University of Munich. 24.01.2018.
Ver todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
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Aurora A 13 nM (IC50) |
Aurora B 79 nM (IC50) |
Aurora C 61 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.028 μM
Compound: 9d
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Antiproliferative activity against A2780 cells
Antiproliferative activity against A2780 cells
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[PMID: 17125279] |
| A2780 | IC50 |
28 μM
Compound: 8, PHA-739358
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Antiproliferative activity against human A2780 cells assessed as accumulation of 4N DNA
Antiproliferative activity against human A2780 cells assessed as accumulation of 4N DNA
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[PMID: 19320489] |
| HCT-116 | EC50 |
80 nM
Compound: 9d
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Cell cycle arrest in HCT116 cells by accumulation at G2/M phase
Cell cycle arrest in HCT116 cells by accumulation at G2/M phase
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[PMID: 17125279] |
| HCT-116 | IC50 |
0.031 μM
Compound: 8, PHA-739358
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Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs
Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs
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[PMID: 19320489] |
| HCT-116 | IC50 |
31 nM
Compound: 9d
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Antiproliferative activity against HCT116 cells
Antiproliferative activity against HCT116 cells
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[PMID: 17125279] |
| HeLa | IC50 |
>25 μM
Compound: 21; MMV676600
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
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[PMID: 30647879] |
| HeLa | IC50 |
0.14 μM
Compound: 9d
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Antiproliferative activity against HeLa cells
Antiproliferative activity against HeLa cells
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[PMID: 17125279] |
| MCF7 | IC50 |
0.08 μM
Compound: 9d
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Antiproliferative activity against MCF7 cells
Antiproliferative activity against MCF7 cells
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[PMID: 17125279] |
| MOLT-4 | EC50 |
0.15 μM
Compound: 1, PHA-739358
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Cytotoxicity against human MOLT4 cells assessed as inhibition of cell growth after 4 days by Cell Titer Blue end-point assay
Cytotoxicity against human MOLT4 cells assessed as inhibition of cell growth after 4 days by Cell Titer Blue end-point assay
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[PMID: 22889561] |
Danusertib (0.01 to 50 μM) significantly decreases viability of C13 and A2780cp cells. The IC50s are 10.40 and 1.83 μM for C13 cells, and 19.89 and 3.88 μM for A2780cp cells after 24- and 48-h treatment. Danusertib induces cell cycle arrest in G2/M phase in C13 and A2780cp cells. Danusertib treatment results in a marked increase in the percentage of cells arrested in G2/M phase and an accumulation of polyploidy in C13 and A2780cp cells. Danusertib demotes the expression of CDK1/CDC2 and cyclin B1 but promotes the expression of p21 Waf1/Cip1, p27 Kip1, and p53. Danusertib induces autophagy in C13 and A2780cp cells with the involvement of PI3K/Akt/mTOR signaling pathway[1].
PHA-739358 strongly inhibits proliferation of all leukemic cell lines tested, with IC50 values ranging from 0.05 μM to 3.06 μM. PHA-739358 induces antiproliferative effects in BaF3-p210 cells, including IM-resistant M351T, E255K, and T315I mutants. PHA-739358 (5 μM) reduces phosphorylation of CrkL in BaF3-p210 wt cells and IM-resistant mutants[2].
Danusertibsertib leads to cell-cycle arrest and completely inhibits cell proliferation of the GEP-NET cells in vitro[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 827318-97-8
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Appearance Solid
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Peso molecular 474.55
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Fòrmula C26H30N6O3
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Color White to yellow
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SMILES
O=C(N1CC2=C(NN=C2NC(C3=CC=C(N4CCN(CC4)C)C=C3)=O)C1)[C@@H](C5=CC=CC=C5)OC
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Synonyms
PHA-739358
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (8)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Biochem Pharmacol
Suppression of NSCLC progression via the co-administration of Danusertib, an AURK inhibitor, and KRIBB11, an HSF1 inhibitor. [Abstract]2024 May:223:116155. PMID: 38521474 -
Mol Cancer Ther
Discovery of New Targets to Control Metastasis in Pancreatic Cancer by Single-cell Transcriptomics Analysis of Circulating Tumor Cells. [Abstract]2020 Aug;19(8):1751-1760. PMID: 32499301 -
bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
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Solvente y solubilidad
DMSO : 50 mg/mL (105.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
The MTT assay is performed to examine the effect of danusertib on the viability of C13 and A2780cp cells. Briefly, cells are seeded in 96-well culture plates at a density of 8×l03 cells/well. After cells are attached, the cells are treated with danusertib at different concentrations (0.01-50 μM). The control cells receive the vehicle only. After 24-h incubation, 10 μL MTT (5 g/L) is added to each well and cultured for another 4 h. Then, the media is carefully aspirated and 100 μL DMSO is added. The absorbance at the 450 nm wavelength is measured with a Synergy H4 Hybrid microplate reader. The IC50 values are determined using the relative viability over danusertib concentration curve using GraphPad Prism 6.0.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
To evaluate the efficacy and toxicity of PHA-739358 in vivo, a subcutaneous animal model for CML is used; 5×107 K562 cells are injected into the flanks of female SCID mice and tumor growth is monitored daily by palpation. On day 7, when tumors reach an estimated weight of 100 to 150 mg, animals are assigned to 3 experimental groups by random selection and receive the following treatment for a period of 10 days: group 1, control, vehicle solution (7 mice); group 2, PHA-739358 twice a day intraperitoneally at a dose of 15 mg/kg (7 mice); and group 3, IM twice a day per os at 100 mg/kg. Tumor growth is assessed by caliper, and tumor weight is calculated according to the following formula: Tumor weight=[length (mm) × width2 (mm)]/2. Toxicity is monitored by changes in body weight and vitality of the animals.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zi D, et al. Danusertib Induces Apoptosis, Cell Cycle Arrest, and Autophagy but Inhibits Epithelial to Mesenchymal Transition Involving PI3K/Akt/mTOR Signaling Pathway in Human Ovarian Cancer Cells. Int J Mol Sci. 2015 Nov 13;16(11):27228-51. [Content Brief]
[2]. Gontarewicz A, et al. Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I. Blood. 2008 Apr 15;111(8):4355-64. [Content Brief]
[3]. Fraedrich K, et al. Targeting Aurora Kinases with Danusertib (PHA-739358) Inhibits Growth of Liver Metastases from Gastroenteropancreatic Neuroendocrine Tumors in an Orthotopic Xenograft Model. Clin Cancer Res. 2012 Sep 1;18(17):4621-32. Epub 2012 Jul 2. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1073 mL | 10.5363 mL | 21.0726 mL | 52.6815 mL |
| 5 mM | 0.4215 mL | 2.1073 mL | 4.2145 mL | 10.5363 mL | |
| 10 mM | 0.2107 mL | 1.0536 mL | 2.1073 mL | 5.2681 mL | |
| 15 mM | 0.1405 mL | 0.7024 mL | 1.4048 mL | 3.5121 mL | |
| 20 mM | 0.1054 mL | 0.5268 mL | 1.0536 mL | 2.6341 mL | |
| 25 mM | 0.0843 mL | 0.4215 mL | 0.8429 mL | 2.1073 mL | |
| 30 mM | 0.0702 mL | 0.3512 mL | 0.7024 mL | 1.7560 mL | |
| 40 mM | 0.0527 mL | 0.2634 mL | 0.5268 mL | 1.3170 mL | |
| 50 mM | 0.0421 mL | 0.2107 mL | 0.4215 mL | 1.0536 mL | |
| 60 mM | 0.0351 mL | 0.1756 mL | 0.3512 mL | 0.8780 mL | |
| 80 mM | 0.0263 mL | 0.1317 mL | 0.2634 mL | 0.6585 mL | |
| 100 mM | 0.0211 mL | 0.1054 mL | 0.2107 mL | 0.5268 mL |
Danusertib Related Classifications
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