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

TAK-659 

Cat. No.: HY-100867
Handling Instructions

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).

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].

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].

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.
Molecular Weight

344.39

Formula

C₁₇H₂₁FN₆O

CAS No.

1312691-33-0

SMILES

FC1=C(N[[email protected]@H]2CCCC[[email protected]@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.

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