BAY 61-3606
Based on 12 publication(s) in Google Scholar
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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- CAS 番号: 732983-37-8
- 分子式: C20H18N6O3
- 分子量:390.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 BAY 61-3606
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.
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Ramos | EC50 |
0.081 μM
Compound: 2, BAY-613606
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Inhibition of SYK in human Ramos B cells assessed as reduction in Ca2+ release
Inhibition of SYK in human Ramos B cells assessed as reduction in Ca2+ release
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[PMID: 22257213] |
| U-937 | EC50 |
0.052 μM
Compound: 2, BAY-613606
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Inhibition of SYK in human U937 cells assessed as reduction FcgammaR-mediated superoxide production
Inhibition of SYK in human U937 cells assessed as reduction FcgammaR-mediated superoxide production
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[PMID: 22257213] |
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.
化学情報
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CAS 番号 732983-37-8
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性状 Solid
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分子量 390.40
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分子式 C20H18N6O3
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=CN=C1NC2=NC(C3=CC=C(OC)C(OC)=C3)=CC4=NC=CN24)N
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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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溶剤 & 溶解度
DMSO : 5 mg/mL (12.81 mM; ultrasonic and warming and heat to 80°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (285 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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取扱説明書 (2659 KB)
参考文献
[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. 2 [Content Brief]
[2]. Gioia R, et al. Quantitative phosphoproteomics revealed interplay between Syk and Lyn in the resistance to nilotinib in chronic myeloid leukemia cells. Blood. 2011 Aug 25;118(8):2211-21. [Content Brief]
[3]. 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]
[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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5615 mL | 12.8074 mL | 25.6148 mL | 64.0369 mL |
| 5 mM | 0.5123 mL | 2.5615 mL | 5.1230 mL | 12.8074 mL | |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5615 mL | 6.4037 mL |
BAY 61-3606 関連分類
HY-76474 関連分類
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