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

TAK-659 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 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (TAK-659 hydrochloride) usually boasts enhanced water solubility and stability.

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

TAK-659 Chemical Structure

TAK-659 Chemical Structure

CAS No. : 1312691-33-0

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Description

TAK-659 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 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 inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines[1][3].
TAK-659 (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 (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells[2].

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

TAK-659 Related Antibodies

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 (100 mg/kg/day; p.o.; 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 treatment kills tumor cells, but not host cells within the spleen and tumors[4].
TAK-659 treatment abrogates metastasis of tumor cells into bone marrow[4].

MedChemExpress (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

344.39

Formula

C17H21FN6O
CAS No.
SMILES

FC1=C(N[C@@H]2CCCC[C@@H]2N)N=C(C3=CN(C)N=C3)C4=C1CNC4=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TAK-659 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAK-6591312691-33-0TAK659TAK 659SykFLT3Spleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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