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Art. -Nr.: HY-100867

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Mivavotinib

(Synonyms: TAK-659; CB-659)

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).

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CAS. Nr.: 1312691-33-0
Formel: C₁₇H₂₁FN₆O
Molecular Weight:344.39

Speicherung:

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

Data Sheet (277 KB)

Mivavotinib Chemical Structure

CAS. Nr.: 1312691-33-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

Chemical Information

CAS. Nr. 1312691-33-0
Molecular Weight 344.39
Formel C₁₇H₂₁FN₆O
SMILES

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

TAK-659; CB-659
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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