| Stereochemistry | ABSOLUTE |
| Molecular Formula | C17H21FN6O |
| Molecular Weight | 344.3866 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C=C(C=N1)C2=C3C(=O)NCC3=C(F)C(N[C@@H]4CCCC[C@@H]4N)=N2
InChI
InChIKey=MJHOMTRKVMKCNE-NWDGAFQWSA-N
InChI=1S/C17H21FN6O/c1-24-8-9(6-21-24)15-13-10(7-20-17(13)25)14(18)16(23-15)22-12-5-3-2-4-11(12)19/h6,8,11-12H,2-5,7,19H2,1H3,(H,20,25)(H,22,23)/t11-,12+/m0/s1
| Molecular Formula | C17H21FN6O |
| Molecular Weight | 344.3866 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
TAK-659 is an investigational, reversible, and potent dual inhibitor of SYK and FLT-3 kinases. TAK-659 inhibited the pro-survival, proliferative, chemoresistant, and activation effects promoted by the microenvironment. Combination of TAK-659 with other BCR inhibitors showed a synergistic effect in inducing apoptosis. Combination of TAK-659 and ibrutinib induced significantly higher cytotoxicity toward CLL cells. TAK-659 suppressed splenomegaly and tumor development in an LMP2A/Myc mouse model in nanomolar concentrations. In addition, TAK-659 also blocked metastasis of tumor cells into bone marrow. A phase Ib/II study of TAK-659 is underway in patients with relapsed or refractory acute myelogenous leukemia
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 3.2 nM [IC50] |
PubMed
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