BAY 61-3606 dihydrochloride
Based on 12 publication(s) in Google Scholar
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 648903-57-5
- Formula: C20H20Cl2N6O3
- Molecular Weight:463.32
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
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Publications Citing Use of MedChemExpress (MCE) BAY 61-3606 dihydrochloride
More- Neuro Oncol. 2018 Apr 9;20(5):621-631. [Abstract]
- Mol Ther. 2025 Dec 10:S1525-0016(25)01033-0. [Abstract]
- NPJ Precis Oncol. 2025 Dec 15;9(1):398. [Abstract]
- Proc Natl Acad Sci U S A. 2022 Oct 25;119(43):e2207280119. [Abstract]
- Front Immunol. 2018 Feb 15:9:249. [Abstract]
- Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. [Abstract]
- JCI Insight. 2024 Jun 13;9(14):e174746. [Abstract]
- Int J Mol Sci. 2021 Mar 24;22(7):3323. [Abstract]
- Pulm Pharmacol Ther. 2026 Jun:93:102421. [Abstract]
- Hematology. 2025 Dec;30(1):2495221. [Abstract]
- University of Pennsylvania. 2026.
- Research Square Preprint. 2024 Apr 19.
Biological Activity
BAY 61-3606 (0.01-10 μM ; 48 hours) significantly reduces the cell viability of SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells in a dose-dependent matter. SH-SY5Y cells expressing high SYK levels are significantly more sensitive to BAY 61-3606 in comparison to SK-N-BEcells expressing very low or no SYK[2].
BAY 61-3606 (0.4 and 0.8 μM; 4 or 24 hours) inhibits SYK activity by reducing ERK1/2 and Akt phosphorylation in neuroblastoma cell SH-SY5Y[2].
BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation in K-rn cell lysates[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells
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Concentration:0.01, 0.1, 1, and 10 μM
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Incubation Time:48 hours
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Result:Significantly reduced the cell viability of both cell lines in a dose-dependent matter.
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Cell Line:SH-SY5Y cells
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Concentration:0.4 and 0.8 μM
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Incubation Time:4 or 24 hours
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Result:Reduced the phosphorylation of ERK1/2 and Akt after a 4 or 24 h treatment.
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Cell Line:K-rn cell lysates
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Concentration:2 μM
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Incubation Time:2 hours
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Result:Induced a large decrease of Syk phosphorylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft[4]
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Dosage:50 mg/kg
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Administration:Injected intraperitoneally twice a week with Bay 61–3606 (50 mg/kg), TRAIL (10 mg/kg) or a combination of Bay 61-3606 (50 mg/kg) and TRAIL (10 mg/kg); TRAIL was given 2 h after the injection of Bay 61-3606; for two weeks
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Result:Led to efficacious reductions in tumor growth.
Chemical Information
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CAS No. 648903-57-5
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Appearance Solid
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Molecular Weight 463.32
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Formula C20H20Cl2N6O3
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Color Off-white to yellow
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SMILES
O=C(N)C1=CC=CN=C1NC2=NC(C3=CC=C(C(OC)=C3)OC)=CC4=NC=CN24.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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Neuro Oncol
SYK inhibition blocks proliferation and migration of glioma cells and modifies the tumor microenvironment. [Abstract]2018 Apr 9;20(5):621-631. PMID: 29401256 -
Mol Ther
FcεRγI promotes canine CD8 chimeric antigen receptor T cell cytotoxicity through a Syk-NF-κB axis. [Abstract]2025 Dec 10:S1525-0016(25)01033-0. PMID: 41376156 -
NPJ Precis Oncol
Siglec-14-LGALS3BP glycoimmune axis shapes tumor-associated macrophage polarization and confers poor outcome in colorectal cancer. [Abstract]2025 Dec 15;9(1):398. PMID: 41398201 -
Proc Natl Acad Sci U S A
Endocytosis triggers V-ATPase-SYK-mediated priming of cGAS activation and innate immune response. [Abstract]2022 Oct 25;119(43):e2207280119. PMID: 36252040 -
Front Immunol
Whole-Genome Expression Profiling in Skin Reveals SYK As a Key Regulator of Inflammation in Experimental Epidermolysis Bullosa Acquisita. [Abstract]2018 Feb 15:9:249. PMID: 29497423 -
Mol Cancer Ther
AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]2024 Oct 1;23(10):1404-1417. PMID: 38894678 -
JCI Insight
2024 Jun 13;9(14):e174746. PMID: 38869957 -
Int J Mol Sci
A Combined Activity of Thrombin and P-Selectin Is Essential for Platelet Activation by Pancreatic Cancer Cells. [Abstract]2021 Mar 24;22(7):3323. PMID: 33805059 -
Pulm Pharmacol Ther
Evodiamine protects against lung ischemia-reperfusion injury by attenuating SYK-associated TLR4/NLRP3 inflammasome activation and ferroptosis-related injury signatures. [Abstract]2026 Jun:93:102421. PMID: 41951097 -
Hematology
Shikonin promotes ferroptosis though NSUN2-mediated m5C methylation modification of TFRC in acute myelocytic leukemia. [Abstract]2025 Dec;30(1):2495221. PMID: 40270446 -
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Solvent & Solubility
H2O : 4.55 mg/mL (9.82 mM; ultrasonic and warming and heat to 60°C)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 0.71 mg/mL (1.53 mM); Clear solution
This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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: ≥ 0.71 mg/mL (1.53 mM); Clear solution
This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Yamamoto N, et al. The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. J Pharmacol Exp Ther. 2003 Sep;306(3):1174-81. [Content Brief]
[2]. Tümmler C, et al. SYK Inhibition Potentiates the Effect of Chemotherapeutic Drugs on Neuroblastoma Cells in Vitro. Cancers (Basel). 2019 Feb 10;11(2). pii: E202. [Content Brief]
[3]. Gioia R, et al. Quantitative phosphoproteomics revealed interplay between Syk and Lyn in the resistance to AMN107 in chronic myeloid leukemia cells. Blood. 2011 Aug 25;118(8):2211-21. [Content Brief]
[4]. Kim SY, et al. Bay 61-3606 Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer Cells. PLoS One. 2015 Dec 31;10(12):e0146073. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.1583 mL | 10.7917 mL | 21.5834 mL | 53.9584 mL |
| 5 mM | 0.4317 mL | 2.1583 mL | 4.3167 mL | 10.7917 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
BAY 61-3606 dihydrochloride Related Classifications
HY-14985 Related Classifications
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