TAK-659 (hydrochloride)
TAK-659 (hydrochloride) Basic information
- Product Name:
- TAK-659 (hydrochloride)
- Synonyms:
-
- 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
- CS-2611
- TAK659;TAK 659;TAK-659
- TAK-659 (hydrochloride)
- TAK-659 HCl
- 6-{[(1R,2S)-2-aminocyclohexyl]amino}-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H,2H,3H-pyrrolo[3,4-c]pyridin-3-one hydrochloride
- Spleen,Inhibitor,Spleen tyrosine kinase,TAK659,Cluster of differentiation antigen 135,inhibit,CLL,related,tyrosine,kinase,FLT3,Fms like tyrosine kinase 3,CD135,TAK 659 hydrochloride,TAK659 hydrochloride,fms,Syk,TAK 659
- TAK-659 hydrochloride (Mivavotinib
- CAS:
- 1952251-28-3
- MF:
- C17H22ClFN6O
- MW:
- 380.85
- Mol File:
- 1952251-28-3.mol
TAK-659 (hydrochloride) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : < 1 mg/mL (insoluble or slightly soluble);Water : 2 mg/mL (5.25 mM; ultrasonic and adjust pH to 3 with HCl)
- form
- Solid
- color
- White to off-white
TAK-659 (hydrochloride) Usage And Synthesis
Uses
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].
in vivo
TAK-659 hydrochloride (100 mg/kg/day; p.o.; daily, 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 hydrochloride treatment kills tumor cells, but not host cells within the spleen and tumors[4].
TAK-659 hydrochloride 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. |
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. DOI:10.1016/j.bmcl.2016.10.087
[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. DOI:10.18632/oncotarget.13557
[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). DOI:10.1128/mSphereDirect.00378-18
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