BAY 61-3606 (dihydrochloride)

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[1]. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell[2]. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates[3]. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells[4].

Product Specifications

CAS Number

[648903-57-5]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Apoptosis; Syk

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/BAY-61-3606-dihydrochloride.html

Purity

99.45

Solubility

H2O : 4.55 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(N)C1=CC=CN=C1NC2=NC(C3=CC=C(C(OC)=C3)OC)=CC4=NC=CN24.[H]Cl.[H]Cl

Molecular Formula

C20H20Cl2N6O3

Molecular Weight

463.32

Precautions

H315, H319, H320

References & Citations

[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.|[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.|[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.|[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.