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[CAS NO. 648903-57-5] BAY61-3606dihydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-14985 |
| Brand: | MCE |
| CAS: | 648903-57-5 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 463.32 |
| Molecular Formula | C20H20Cl2N6O3 |
| SMILES | O=C(N)C1=CC=CN=C1NC2=NC(C3=CC=C(C(OC)=C3)OC)=CC4=NC=CN24.[H]Cl.[H]Cl |
5 Publications Citing Use of MCE
Summary
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a K i of 7.5 nM an IC 50 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] .
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [2]
| Cell Line: | SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells |
| Concentration: | 0.01, 0.1, 1, and 10 μM |
| Incubation Time: | 48 hours |
| Result: | Significantly reduced the cell viability of both cell lines in a dose-dependent matter. |
Cell Proliferation Assay [2]
| 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 [3]
| Cell Line: | K-rn cell lysates |
| Concentration: | 2 μM |
| Incubation Time: | 2 hours |
| Result: | Induced a large decrease of Syk phosphorylation. |
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft [4] |
| Dosage: | 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 weeks |
| Result: | Led to efficacious reductions in tumor growth. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 5 mg/mL ( 10.79 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1583 mL | 10.7917 mL | 21.5834 mL |
| 5 mM | 0.4317 mL | 2.1583 mL | 4.3167 mL |
| 10 mM | 0.2158 mL | 1.0792 mL | 2.1583 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.71 mg/mL (1.53 mM); Clear solution
References
- [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.
Synonyms
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