1952251-28-3
Chemical Structure
Mivavotinib monohydrochloride
Synonym(s): TAK-659 monohydrochloride; CB-659 monohydrochloride
- CAS No.: 1952251-28-3
- Formula:C17H22ClFN6O
- Molecular Weight:380.85
IUPAC Name: 6-(((1R,2S)-2-aminocyclohexyl)amino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one hydrochloride
InChIKey: PTCFBXMEFRIEGV-ZVWHLABXSA-N
SMILES: FC1=C(N[C@@H]2CCCC[C@@H]2N)N=C(C3=CN(C)N=C3)C4=C1CNC4=O.Cl
Biological Activity: 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].
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Mivavotinib monohydrochloride | 99.50% | 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). | ||||||||||||||||||||
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Mivavotinib monohydrochloride (Standard) | ≥98% | Mivavotinib (monohydrochloride) (Standard) is the analytical standard of Mivavotinib (monohydrochloride) (HY-100867A). This product is intended for research and analytical applications. 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). | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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). [Content Brief]
