Network Version
BAY 61-3606 Data Sheet
| Product Name: | BAY 61-3606 |
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|---|---|---|
| CAS No.: | 732983-37-8 | |
| Cat. No.: | HY-76474 | |
| MWt: | 390.4 | |
| Formula: | C20H18N6O3 | |
| Purity : | >98% | |
| Solubility: | DMSO : 5 mg/mL (ultrasonic;warming;heat to 80°C) | |
| Mechanisms: | Target: Cancer Inflammation/Immunology | |
| Biological Activity: | ||
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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[1]. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell[2]. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates[3]. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells[4].
IC50 & Target: Ki: 7.5 nM (Syk)[1] IC50: 10 nM (Syk)[1] In Vitro: 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]. In Vivo: 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[4]. |
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