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TAK-659 hydrochloride

Cat. No. M10688
TAK-659 hydrochloride Structure
Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 140  USD140 In stock
25mg USD 280  USD280 In stock
50mg USD 420  USD420 In stock
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Quality Control & Documentation
Biological Activity

TAK-659 hydrochloride is a highly selective, reversible, orally potent dual inhibitor of SYK/FLT3 that acts on SYK and FLT3 IC50 The values are 3.2 nM and 4.6 nM, respectively. TAK-659 hydrochloride induces tumor cell death without acting on non-tumor cells, with potential to study chronic lymphocytic leukemia (CLL).

Chemical Information
Molecular Weight 380.85
Formula C17H22ClFN6O
CAS Number 1952251-28-3
Solubility (25°C) DMSO < 1 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Leo I Gordon, et al. Clin Cancer Res. Phase I Study of TAK-659, an Investigational, Dual SYK/FLT3 Inhibitor, in Patients with B-Cell Lymphoma

[2] Osman Cen, et al. mSphere. Spleen Tyrosine Kinase Inhibitor TAK-659 Prevents Splenomegaly and Tumor Development in a Murine Model of Epstein-Barr Virus-Associated Lymphoma

[3] Delong Liu, et al. J Hematol Oncol. Syk inhibitors in clinical development for hematological malignancies

[4] Noelia Purroy, et al. Oncotarget. Inhibition of BCR signaling using the Syk inhibitor TAK-659 prevents stroma-mediated signaling in chronic lymphocytic leukemia cells

[5] Betty Lam, et al. Bioorg Med Chem Lett. Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK)

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