Art. -Nr.: HY-10179

Danusertib

(Synonyms: PHA-739358)

8 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.68%
CAS. Nr.: 827318-97-8
Formel: C₂₆H₃₀N₆O₃
Molecular Weight:474.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Danusertib Chemical Structure

CAS. Nr.: 827318-97-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC₅₀ of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

IC₅₀ & Target^[1]

Aurora A

13 nM (IC₅₀)

Aurora B

79 nM (IC₅₀)

Aurora C

61 nM (IC₅₀)

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.028 μM Compound: 9d	Antiproliferative activity against A2780 cells Antiproliferative activity against A2780 cells	[PMID: 17125279]
A2780	IC₅₀	28 μM Compound: 8, PHA-739358	Antiproliferative activity against human A2780 cells assessed as accumulation of 4N DNA Antiproliferative activity against human A2780 cells assessed as accumulation of 4N DNA	[PMID: 19320489]
HCT-116	EC₅₀	80 nM Compound: 9d	Cell cycle arrest in HCT116 cells by accumulation at G2/M phase Cell cycle arrest in HCT116 cells by accumulation at G2/M phase	[PMID: 17125279]
HCT-116	IC₅₀	0.031 μM Compound: 8, PHA-739358	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	[PMID: 19320489]
HCT-116	IC₅₀	31 nM Compound: 9d	Antiproliferative activity against HCT116 cells Antiproliferative activity against HCT116 cells	[PMID: 17125279]
HeLa	IC₅₀	>25 μM Compound: 21; MMV676600	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	[PMID: 30647879]
HeLa	IC₅₀	0.14 μM Compound: 9d	Antiproliferative activity against HeLa cells Antiproliferative activity against HeLa cells	[PMID: 17125279]
MCF7	IC₅₀	0.08 μM Compound: 9d	Antiproliferative activity against MCF7 cells Antiproliferative activity against MCF7 cells	[PMID: 17125279]
MOLT-4	EC₅₀	0.15 μM Compound: 1, PHA-739358	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	[PMID: 22889561]

In Vitro

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.

In Vivo

PHA-739358 (15 mg/kg twice a day, i.p.) and IM are well tolerated, and significantly inhibit proliferation of K562 cells andvirtually suppressed tumor growth during the 10-day treatment period^[2]. In a subcutaneous murine xenograft model, danusertibsertib (2×15 mg/kg/d, i.p.) significantly reduces tumor growth in vivo compared with controls or mice treated with streptozotocine/5-fluorouracil^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 827318-97-8
Appearance Solid
Molecular Weight 474.55
Formel C₂₆H₃₀N₆O₃
Color White to yellow
SMILES

O=C(N1CC2=C(NN=C2NC(C3=CC=C(N4CCN(CC4)C)C=C3)=O)C1)[C@@H](C5=CC=CC=C5)OC
Synonyms

PHA-739358
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Closing the loop: Teaching single-cell foundation models to learn from perturbations. [Abstract]

2025 Jul 12:2025.07.08.663754. PMID: 40672312
Patent

US20210299273A1.
Patent

US20180263995A1.
Technical University of Munich

24.01.2018.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1073 mL

10.5363 mL

21.0726 mL

5 mM

0.4215 mL

2.1073 mL

4.2145 mL

10 mM

0.2107 mL

1.0536 mL

2.1073 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[1]

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.

Animal Administration^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Danusertib

8 Cited Publications

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Danusertib

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Anti-Blood Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Danusertib

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Danusertib

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Anti-Blood Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Danusertib

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Danusertib Related Classifications

HY-10179 Related Classifications