[CAS NO. 648903-57-5] BAY61-3606dihydrochloride

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PRODUCTS SPECIFICATIONS [648903-57-5]

Catalog

HY-14985

Brand

MCE

CAS

648903-57-5

DESCRIPTION [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

For research use only. We do not sell to patients.

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] .

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] .

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

In Vitro:

H ₂ O : 5 mg/mL ( 10.79 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 0.71 mg/mL (1.53 mM); Clear solution
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

* All of the co-solvents are available by MCE.

References

Synonyms

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

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

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

BAY 61-3606 dihydrochloride