Art. -Nr.: HY-103020

BAY-1816032

18 Cited Publications

Kundenbewertung

Based on 18 publication(s) in Google Scholar

BAY-1816032, a chemical probe, is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC₅₀ of 7 nM.

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Reinheit: 99.73%
CAS. Nr.: 1891087-61-8
Formel: C₂₇H₂₄F₂N₆O₄
Molecular Weight:534.51

Speicherung:

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

BAY-1816032 Chemical Structure

CAS. Nr.: 1891087-61-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (18)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

BAY-1816032, a chemical probe, is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC₅₀ of 7 nM.

IC₅₀ & Target

IC50: 7 nM (BUB1)^[1]

In Vitro

BAY-1816032 inhibits BUB1 enzymatic activity with an IC₅₀ of 7 nM, shows slow dissociation kinetics resulting in a long target residence time of 87 min, and an excellent selectivity on a panel of 395 kinases. Mechanistically BAY-1816032 abrogates nocodazole-induced Thr-120 phosphorylation of the major BUB1 target protein histone H2A in HeLa cells with an IC₅₀ of 29 nM, induced lagging chromosomes and mitotic delay. Persistent lagging chromosomes and missegregation are observed upon combination with low concentrations of paclitaxel. Single agent BAY-1816032 inhibits proliferation of various tumor cell lines with a median IC₅₀ of 1.4 μM and demonstrates synergy or additivity with paclitaxel or docetaxel in almost all cell lines evaluated (minimal combination index 0.3)^[1].

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

In Vivo

In tumor xenograft studies BAY 1816032 only marginally inhibits tumor growth as single agent upon oral administration, however, upon combination with paclitaxel or docetaxel a strong and statistically significant reduction of tumor size as compared to the respective monotherapy is observed^[1].

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

Chemical Information

CAS. Nr. 1891087-61-8
Appearance Solid
Molecular Weight 534.51
Formel C₂₇H₂₄F₂N₆O₄
Color Off-white to yellow
SMILES

COC1=C(NC2=NC(C3=NN(CC4=C(F)C=C(OCCO)C=C4F)C5=C3C=CC=C5)=NC=C2OC)C=CN=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (18)

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Journal Impact Factor

Cell

Molecular Strategies of Meiotic Cheating by Selfish Centromeres. [Abstract]

2019 Aug 22;178(5):1132-1144.e10. PMID: 31402175
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Meiosis-specific distal cohesion site decoupled from the kinetochore. [Abstract]

2025 Mar 3;16(1):2116. PMID: 40032846
Sci Adv

Biallelic BUB1 mutations cause microcephaly, developmental delay, and variable effects on cohesion and chromosome segregation. [Abstract]

2022 Jan 21;8(3):eabk0114. PMID: 35044816
Cell Death Dis

Genome-wide CRISPR screen identifies BUB1 kinase as a druggable vulnerability in malignant pleural mesothelioma. [Abstract]

2025 Apr 3;16(1):241. PMID: 40180891
EMBO J

A bifunctional kinase-phosphatase module balances mitotic checkpoint strength and kinetochore-microtubule attachment stability. [Abstract]

2023 Oct 16;42(20):e112630. PMID: 37712330
J Bone Miner Res

Bub1 suppresses inflammatory arthritis-associated bone loss in mice through inhibition of TNFα-mediated osteoclastogenesis. [Abstract]

2024 Apr 19;39(3):341-356. PMID: 38477771
iScience

hSpindly dynamics modulate spindle assembly checkpoint signaling, promoting resistance to mitotic inhibitors. [Abstract]

2026 Jun 16;29(7):116312. PMID: 42338480
Sci Rep

BUB1 as a candidate non-oncogene addiction vulnerability in metastatic phaeochromocytoma/paraganglioma. [Abstract]

2026 Apr 21;16(1):18544. PMID: 42014906
J Proteome Res

Mapping Proximity Associations of Core Spindle Assembly Checkpoint Proteins. [Abstract]

2021 Jul 2;20(7):3414-3427. PMID: 34087075
bioRxiv

2025 Jul 25.
DNA (Basel)

2025 Mar 12.
bioRxiv

BUB1 regulates non-homologous end joining pathway to mediate radioresistance in triple-negative breast cancer. [Abstract]

2024 May 10:2024.05.07.592812. PMID: 38766122
Preprints

2024 Apr 24.
Brunel University London

2023 May.
SSRN

2023 Jun 9.
bioRxiv

2021 Feb 5.
bioRxiv

2020 Jun.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (46.77 mM; Need ultrasonic and warming; 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

1.8709 mL

9.3544 mL

18.7087 mL

5 mM

0.3742 mL

1.8709 mL

3.7417 mL

10 mM

0.1871 mL

0.9354 mL

1.8709 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (3.89 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 (3.89 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 (3.89 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Siemeister G, et al. BAY 1816032, a novel BUB1 kinase inhibitor with potent antitumor activity [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Ishington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 287. doi:10.1158/1538-7445.AM2017-287

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8709 mL	9.3544 mL	18.7087 mL	46.7718 mL
	5 mM	0.3742 mL	1.8709 mL	3.7417 mL	9.3544 mL
	10 mM	0.1871 mL	0.9354 mL	1.8709 mL	4.6772 mL
	15 mM	0.1247 mL	0.6236 mL	1.2472 mL	3.1181 mL
	20 mM	0.0935 mL	0.4677 mL	0.9354 mL	2.3386 mL
	25 mM	0.0748 mL	0.3742 mL	0.7483 mL	1.8709 mL
	30 mM	0.0624 mL	0.3118 mL	0.6236 mL	1.5591 mL
	40 mM	0.0468 mL	0.2339 mL	0.4677 mL	1.1693 mL

Keywords

BAY-1816032

18 Cited Publications

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BAY-1816032

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Chemical Probe Library

Targeted Diversity Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) BAY-1816032

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BAY-1816032

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Chemical Probe Library

Targeted Diversity Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) BAY-1816032

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BAY-1816032 Related Classifications

HY-103020 Related Classifications