1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Syk
    Apoptosis
  3. BAY 61-3606 dihydrochloride

BAY 61-3606 dihydrochloride 

Cat. No.: HY-14985 Purity: 98.21%
Handling Instructions

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

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

BAY 61-3606 dihydrochloride Chemical Structure

BAY 61-3606 dihydrochloride Chemical Structure

CAS No. : 648903-57-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1152 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of BAY 61-3606 dihydrochloride:

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Description

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].

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].

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].

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.
Molecular Weight

463.32

Formula

C₂₀H₂₀Cl₂N₆O₃

CAS No.

648903-57-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.14 mg/mL (15.41 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 provided by MCE.
References
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Product Name:
BAY 61-3606 dihydrochloride
Cat. No.:
HY-14985
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