Mivavotinib (Synonyms: TAK-659; CB-659)

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TAK-659 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 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Mivavotinib monohydrochloride) usually boasts enhanced water solubility and stability.

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Mivavotinib Chemical Structure

CAS No. : 1312691-33-0

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Other In-stock Forms of Mivavotinib:

Mivavotinib monohydrochloride

Other Forms of Mivavotinib:

Mivavotinib monohydrochloride In-stock

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC50: 3.2 nM (Syk), 4.6 nM (FLT3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	EC₅₀	> 10 μM Compound: 3b; TAK-659	Cytotoxicity against human hepatocytes assessed as decrease in cell viability after 72 to 96 hrs by MTS assay Cytotoxicity against human hepatocytes assessed as decrease in cell viability after 72 to 96 hrs by MTS assay	[PMID: 27839918]
MOLM-13	EC₅₀	0.11 μM Compound: 3b; TAK-659	Cytotoxicity against FLT3-ITD dependent human MOLM13 cells assessed as decrease in cell viability after 72 to 96 hrs by MTS assay Cytotoxicity against FLT3-ITD dependent human MOLM13 cells assessed as decrease in cell viability after 72 to 96 hrs by MTS assay	[PMID: 27839918]
MV4-11	EC₅₀	0.018 μM Compound: 3b; TAK-659	Cytotoxicity against FLT3-ITD dependent human MV411 cells assessed as decrease in cell viability after 72 to 96 hrs by MTS assay Cytotoxicity against FLT3-ITD dependent human MV411 cells assessed as decrease in cell viability after 72 to 96 hrs by MTS assay	[PMID: 27839918]
Ramos	EC₅₀	9.8 nM Compound: 3b; TAK-659	Inhibition of SYK in TgM-stimulated human Ramos cells expressing RA1/GFP-tagged BLNK assessed as reduction in RA1/GFP-tagged BLNK phosphorylation preincubated for 1 hr followed by IgM stimulation for 20 mins by TR-FRET assay Inhibition of SYK in TgM-stimulated human Ramos cells expressing RA1/GFP-tagged BLNK assessed as reduction in RA1/GFP-tagged BLNK phosphorylation preincubated for 1 hr followed by IgM stimulation for 20 mins by TR-FRET assay	[PMID: 27839918]
RS4-11	EC₅₀	1.4 μM Compound: 3b; TAK-659	Cytotoxicity against human RS4:11 cells harboring wild type FLT3 assessed as decrease in cell viability after 72 to 96 hrs by MTS assay Cytotoxicity against human RS4:11 cells harboring wild type FLT3 assessed as decrease in cell viability after 72 to 96 hrs by MTS assay	[PMID: 27839918]
Sf9	IC₅₀	135 nM Compound: 3b; TAK-659	Inhibition of human N-terminal 6His-tagged VEGFR2 (807 to 1171 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-EEPLYWSFPAKKK-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay Inhibition of human N-terminal 6His-tagged VEGFR2 (807 to 1171 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-EEPLYWSFPAKKK-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay	[PMID: 27839918]
Sf9	IC₅₀	3.2 nM Compound: 3b; TAK-659	Inhibition of human C-terminal 6His-tagged SYK (356 to 635 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-EEPLYWSFPAKKK-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay Inhibition of human C-terminal 6His-tagged SYK (356 to 635 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-EEPLYWSFPAKKK-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay	[PMID: 27839918]
Sf9	IC₅₀	4.6 nM Compound: 3b; TAK-659	Inhibition of human N-terminal 6His-tagged FLT3 (564 to 993 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-KKKKEEIYFFFG-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay Inhibition of human N-terminal 6His-tagged FLT3 (564 to 993 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-KKKKEEIYFFFG-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay	[PMID: 27839918]

In Vitro

TAK-659 inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines^[1]^[3].
TAK-659 (5 μM; 1-24 hours) induces Casp3 activation in the LMP2A/MYC cells which was readily apparent at 4 h and reached maximum levels at 8 h of treatment^[4].
TAK-659 (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[4]

Cell Line:	LMP2A/MYC cells
Concentration:	5 µM
Incubation Time:	1 hour, 2 hours, 4 hours, 8 hours, 24 hours
Result:	Induced apoptosis in LMP2A/MYC lymphoma cells.

Western Blot Analysis^[2]

Cell Line:	Ramos cells
Concentration:	0.01 μM,0.1 μM,1 μM,10 μM
Incubation Time:	1 hour
Result:	Enhanced expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 in stimulated Ramos cells.

In Vivo

TAK-659 (100 mg/kg/day; p.o.; 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 treatment kills tumor cells, but not host cells within the spleen and tumors^[4].
TAK-659 treatment abrogates metastasis of tumor cells into bone marrow^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

Molecular Weight

344.39

Formula

C₁₇H₂₁FN₆O

CAS No.

1312691-33-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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]

Mivavotinib Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mivavotinib1312691-33-0TAK-659 CB-659TAK659TAK 659CB659CB 659CB-659SykFLT3Spleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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