1. Protein Tyrosine Kinase/RTK
  2. Syk
    FLT3
  3. TAK-659 hydrochloride

TAK-659 hydrochloride 

Cat. No.: HY-100867A Purity: 99.69%
Handling Instructions

TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).

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

TAK-659 hydrochloride Chemical Structure

TAK-659 hydrochloride Chemical Structure

CAS No. : 1952251-28-3

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2 mg USD 90 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL)[1][2][3][4].

IC50 & Target

IC50: 3.2 nM (Syk), 4.6 nM (FLT3)[1]

In Vitro

TAK-659 hydrochloride inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines[1][3].
TAK-659 hydrochloride (5 µM; 1-24 hours) induces Casp3 activation in the LMP2A/MYC cells which was readily apparent at 4 h and reached maximum levels at 8 h of treatment[4].
TAK-659 hydrochloride (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[4]

Cell Line: LMP2A/MYC cells
Concentration: 5 µM
Incubation Time: 1 hour, 2 hours, 4 hours, 8 hours, 24 hours
Result: Induced apoptosis in LMP2A/MYC lymphoma cells.

Western Blot Analysis[2]

Cell Line: Ramos cells
Concentration: 0.01 μM,0.1 μM,1 μM,10 μM
Incubation Time: 1 hour
Result: Enhanced expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 in stimulated Ramos cells.
In Vivo

TAK-659 hydrochloride (100 mg/kg/day; p.o.; daily, for 10 days) treatment totally abrogates splenomegaly and tumor development in LMP2A/MYC mice in both pretumor and tumor cell transfer experiments[4].
TAK-659 hydrochloride treatment kills tumor cells, but not host cells within the spleen and tumors[4].
TAK-659 hydrochloride treatment abrogates metastasis of tumor cells into bone marrow[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: LMP2A/MYC double transgenic mice[4]
Dosage: 100 mg/kg/day
Administration: Oral gavage; for 10 days
Result: Inhibited LMP2A-induced tumor cell survival in vivo.
Clinical Trial
Molecular Weight

380.85

Formula

C₁₇H₂₂ClFN₆O

CAS No.

1952251-28-3

SMILES

FC1=C(N[[email protected]@H]2CCCC[[email protected]@H]2N)N=C(C3=CN(C)N=C3)C4=C1CNC4=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 2 mg/mL (5.25 mM; ultrasonic and adjust pH to 3 with HCl)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6257 mL 13.1285 mL 26.2571 mL
5 mM 0.5251 mL 2.6257 mL 5.2514 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.69%

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Keywords:

TAK-659TAK659TAK 659SykFLT3Spleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3SpleentyrosinekinaseSYKfmsrelatedCLLInhibitorinhibitorinhibit

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Product Name:
TAK-659 hydrochloride
Cat. No.:
HY-100867A
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