BAY-61-3606

Catalog No.S7006 Batch:S700602

Technical Data

Formula	C₂₀H₁₈N₆O₃.2HCl
Molecular Weight	463.32	CAS No.	648903-57-5
Solubility (25°C)*	In vitro	DMSO	14 mg/mL (30.21 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). BAY-61-3606 induces cell cycle arrest and apoptosis.

Targets

Syk ^[1]
(Cell-free assay)

7.5 nM(Ki)

In vitro

BAY 61-3606 is a highly selective inhibitor of Syk kinase. Other selected tyrosine kinases, Lyn, Fyn, Src, Itk, and Btk, are not inhibited by BAY 61-3606 in concentrations up to 4.7 μM. BAY 61-3606 is also found to inhibit B cell receptor (BCR)-mediated signaling^[1].

Bay 61-3606 is a sensitizer of TRAIL-induced apoptosis. Mcl-1 downregulation by Bay 61-3606 are concentration- and time-dependent in MCF-7 cells. phosphorylation of Syk is reduced by Bay 61-3606 in MCF-7 and T47D cells. Downregulation of Mcl-1 by Bay 61-3606 is independent of Syk in breast cancer cells. Bay 61-3606 promotes the ubiquitin/proteasome-dependent degradation of the Mcl-1 protein in MCF-7 cells. Bay 61-3606 inhibits the phosphorylation of CDK9, RNA polymerase II, and Mcl-1 expression in MCF-7 cells. Bay 61-3606 inhibits CDK9 kinase activity with an in vitro IC50 of 37 nM^[2].

In vivo

After 20 days of drug administration, the volume of the xenografted tumor was significantly (P <0.001) reduced the efficacy of Bay 61–3606 when administered in TRAIL combination^[2].

Oral administration of BAY 61-3606 to rats significantly suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuates antigen-induced airway inflammation in rats^[1].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines MCF-7 cells Concentrations 2.5 μM or 5 μM Incubation Time 12 h or 24 h Method MCF-7 cells are exposed to TRAIL (indicated concentrations:0, 12.5, 25, 37.5 ng/ml) with or without Bay 61-3606 (2.5 μM) for 24 h; After exposure to the agents for 12 h, MCF-7 cells are subjected to immunocytochemistry using an active Bak antibody; Caspase activity is measured in MCF-7 cells exposed to Bay 61-3606 (5 μM) with or without TRAIL (50 ng/ml) for 24 h.

Cell Assay:^{^[2]}

Cell lines
MCF-7 cells
Concentrations
2.5 μM or 5 μM
Incubation Time
12 h or 24 h
Method
MCF-7 cells are exposed to TRAIL (indicated concentrations:0, 12.5, 25, 37.5 ng/ml) with or without Bay 61-3606 (2.5 μM) for 24 h; After exposure to the agents for 12 h, MCF-7 cells are subjected to immunocytochemistry using an active Bak antibody; Caspase activity is measured in MCF-7 cells exposed to Bay 61-3606 (5 μM) with or without TRAIL (50 ng/ml) for 24 h.

References

Selleck's BAY-61-3606 has been cited by 14 publications

HP1 induces ferroptosis of renal tubular epithelial cells through NRF2 pathway in diabetic nephropathy [ Open Life Sci, 2023, 18(1):20220678]	PubMed: 37589000
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226]	PubMed: 36266272
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226]	PubMed: 36266272
ARPC1B binds WASP to control actin polymerization and curtail tonic signaling in B cells [ JCI Insight, 2021, e149376]	PubMed: 34673575
Dectin-2-mediated initiation of immune responses caused by influenza virus hemagglutinin [ Biomed Res, 2021, 42(2):53-66]	PubMed: 33840686
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790]	PubMed: 31160710
Berberine suppresses mast cell-mediated allergic responses via regulating FcɛRI-mediated and MAPK signaling. [ Int Immunopharmacol, 2019, 71:1-6]	PubMed: 30861392
Multiple sources of signal amplification within the B-cell Ras/MAPK pathway. [ Mol Biol Cell, 2019, 30(13):1610-1620]	PubMed: 31042097
Phosphorylation-Mediated IFN-γR2 Membrane Translocation Is Required to Activate Macrophage Innate Response [Xu X, et al. Cell, 2018, 175(5):1336-1351]	PubMed: 30318148
Whole-Genome Expression Profiling in Skin Reveals SYK As a Key Regulator of Inflammation in Experimental Epidermolysis Bullosa Acquisita [ Front Immunol, 2018, 9:249]	PubMed: 29497423

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SHIPPING AND STORAGE
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