Mivavotinib (monohydrochloride)

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].

Product Specifications

CAS Number

[1952251-28-3]

Product Name Alternative

TAK-659 (monohydrochloride) ; CB-659 (monohydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

FLT3; Syk

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mivavotinib-monohydrochloride.html

Purity

99.91

Solubility

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

Smiles

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

Molecular Formula

C17H22ClFN6O

Molecular Weight

380.85

Precautions

H302, H315, H319, H335

References & Citations

[1]Lam B, et al. Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK) . Bioorg Med Chem Lett. 2016 Dec 15;26 (24) :5947-5950.|[2]Purroy N, et al. Inhibition of BCR signaling using the Syk inhibitor TAK-659 prevents stroma-mediated signaling in chronic lymphocytic leukemia cells. Oncotarget. 2017 Jan 3;8 (1) :742-756.|[3]Jie Yu, et al. Anti-tumor activity of TAK-659, a dual inhibitor of SYK and FLT-3 kinases, in AML models. Journal of Clinical Oncology 34, no. 15_suppl.|[4]Cen O, et al. Spleen Tyrosine Kinase Inhibitor TAK-659 Prevents Splenomegaly and Tumor Development in a Murine Model of Epstein-Barr Virus-Associated Lymphoma. mSphere. 2018 Aug 22;3 (4) .