BAY-1816032
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.73%
- CAS No.: 1891087-61-8
- 화학식: C27H24F2N6O4
- 분자량:534.51
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BAY-1816032
More- Cell. 2019 Aug 22;178(5):1132-1144.e10. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Mar 3;16(1):2116. [Abstract]
- Sci Adv. 2022 Jan 21;8(3):eabk0114. [Abstract]
- Cell Death Dis. 2025 Apr 3;16(1):241. [Abstract]
- EMBO J. 2023 Oct 16;42(20):e112630. [Abstract]
- J Bone Miner Res. 2024 Apr 19;39(3):341-356. [Abstract]
- iScience. 2026 Jun 16;29(7):116312. [Abstract]
- Sci Rep. 2026 Apr 21;16(1):18544. [Abstract]
- J Proteome Res. 2021 Jul 2;20(7):3414-3427. [Abstract]
- bioRxiv. 2025 Jul 25.
- DNA (Basel). 2025 Mar 12.
- bioRxiv. 2024 May 10:2024.05.07.592812. [Abstract]
- Preprints. 2024 Apr 24.
- Brunel University London. 2023 May.
- SSRN. 2023 Jun 9.
- bioRxiv. 2021 Feb 5.
- bioRxiv. 2020 Jun.
Biological Activity
IC50: 7 nM (BUB1)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1891087-61-8
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Appearance Solid
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분자량 534.51
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화학식 C27H24F2N6O4
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Color Off-white to yellow
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SMILES
COC1=C(NC2=NC(C3=NN(CC4=C(F)C=C(OCCO)C=C4F)C5=C3C=CC=C5)=NC=C2OC)C=CN=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
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Most Recent
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Cell
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
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
2021 Jul 2;20(7):3414-3427. PMID: 34087075 -
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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 -
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용액&용해도
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)
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.
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.
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 (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.
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 (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.
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.
순도&문서
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Data Sheet (282 KB)
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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)
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Handling Instructions (2659 KB)
References
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, 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 |
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