BAY 61-3606 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、ATP 竞争性的、可逆的、高选择性的 Syk 酪氨酸激酶抑制剂，Ki 为 7.5 nM。

A potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase with Ki of 7.5 nM, displays no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src; inhibits not only degranulation (IC50=5-46 nM) but also lipid mediator and cytokine synthesis in mast cells; suppresses B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes; suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg in rats; orally bioavailable.Allergy Preclinical.

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. 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.BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation inK-rn cell lysates. Cell Viability AssayCell Line:SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells Concentration:0.01, 0.1, 1, and 10 μMIncubation Time:48 hours Result:Significantly reduced the cell viability of both cell lines in a dose-dependent matter.Cell Proliferation Assay Cell Line:SH-SY5Y cells Concentration:0.4 and 0.8 μM Incubation Time:4 or 24 hours Result:Reduced the phosphorylation of ERK1/2 and Akt after a 4 or 24 h treatment.Western Blot Analysis Cell Line:K-rn cell lysates Concentration:2 μM Incubation Time:2 hours Result:Induced a large decrease of Syk phosphorylation.

Bay 61-3606 (50 mg/kg; administered twice a week for two weeks by intraperitoneal injection) alone leads to more efficacious reductions than that of TNF-related apoptosis-inducing ligand (TRAIL; 10 mg/kg) alone in MCF-7 tumor xenograft-bearing BALB/c nude mice. Bay 61-3606 administered in TRAIL combination significantly reduces the volume of the xenografted tumor. Animal Model:Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograftDosage:50 mg/kg 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 weeksResult:Led to efficacious reductions in tumor growth.

BAY61-3606 dihydrochloride | BAY 61-3606

Angiogenesis

Syk

Syk

Inflammation/Immunology

Allergy

648903-57-5

463.3172

C20H20Cl2N6O3

>98% (HPLC)

DMSO: ≥ 4.6 mg/mL

COC1=C(C=C(C=C1)C2=CC3=NC=CN3C(=N2)NC4=C(C=CC=N4)C(=O)N)OC.Cl.Cl

3-Pyridinecarboxamide, 2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-, hydrochloride (1:2)

(-20℃)

With Ice Pack

≥ 2 years