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BAY 61-3606 dihydrochloride

Catalog No. T6776   CAS 648903-57-5
Synonyms: BAY 61-3606, BAY-61-3606 dihydrochloride

BAY 61-3606 dihydrochloride (BAY 61-3606) is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM).

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BAY 61-3606 dihydrochloride Chemical Structure
BAY 61-3606 dihydrochloride, CAS 648903-57-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 53.00
2 mg In stock $ 75.00
5 mg In stock $ 126.00
10 mg In stock $ 197.00
25 mg In stock $ 328.00
50 mg In stock $ 489.00
100 mg In stock $ 713.00
1 mL * 10 mM (in DMSO) In stock $ 148.00
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Purity: 99.46%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BAY 61-3606 dihydrochloride (BAY 61-3606) is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM).
Targets&IC50 Syk: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].
Kinase Assay GST-Syk (3.2?ng), 0.5?μg AL, 30?μM ATP, and testing compound in the presence of 0.25% Me2SO are mixed in 50?μL/well of kinase assay buffer in polypropylene U-bottom 96-well microtiter plates. The mixture is incubated for 1?h at room temperature, and the reaction is terminated by the addition of 120?μL of termination buffer. To capture AL, 120?μL of the terminated mixture is transferred to streptavidin-coated plates, followed by incubation at room temperature for more than 30?min. After three ishes with washing buffer, 100?μL of antibody buffer is added and incubated at room temperature for more than 30?min. After three more ishes, 100?μL of enhancement solution is added. Time-resolved fluorescence is measured by multilabel counter ARVO.
Cell Research 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.(Only for Reference)
Synonyms BAY 61-3606, BAY-61-3606 dihydrochloride
Molecular Weight 463.32
Formula C20H18N6O3·2HCl
CAS No. 648903-57-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 12 mg/mL (25.9 mM)

TargetMolReferences and Literature

1. Yamamoto N, et al. J Pharmacol Exp Ther. 2003, 306(3):1174-81. 2. Kim SY, et al. PLoS One. 2015, 10(12):e0146073.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Angiogenesis related Compound Library Anti-Breast Cancer Compound Library Apoptosis Compound Library Orally Active Compound Library Bioactive Compound Library

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Keywords

BAY 61-3606 dihydrochloride 648903-57-5 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors Syk BAY 613606 dihydrochloride Spleen tyrosine kinase inhibit Inhibitor BAY-61-3606 BAY 61-3606 BAY-61-3606 Dihydrochloride BAY 61 3606 dihydrochloride BAY-61-3606 dihydrochloride BAY 61-3606 Dihydrochloride inhibitor

 

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