Mivavotinib monohydrochloride
Based on 1 Customer Validation
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).
For research use only. We do not sell to patients.
- Purity: 99.50%
- CAS No.: 1952251-28-3
- Formula: C17H22ClFN6O
- Molecular Weight:380.85
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Storage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 3.2 nM (Syk), 4.6 nM (FLT3)[1]
TAK-659 hydrochloride inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines[1][3].
TAK-659 hydrochloride (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 hydrochloride (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.
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Cell Line:LMP2A/MYC cells
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Concentration:5 µM
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Incubation Time:1 hour, 2 hours, 4 hours, 8 hours, 24 hours
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Result:Induced apoptosis in LMP2A/MYC lymphoma cells.
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Cell Line:Ramos cells
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Concentration:0.01 μM,0.1 μM,1 μM,10 μM
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Incubation Time:1 hour
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Result:Enhanced expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 in stimulated Ramos cells.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LMP2A/MYC double transgenic mice[4]
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Dosage:100 mg/kg/day
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Administration:Oral gavage; for 10 days
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Result:Inhibited LMP2A-induced tumor cell survival in vivo.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1952251-28-3
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Appearance Solid
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Molecular Weight 380.85
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Formula C17H22ClFN6O
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Color White to off-white
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SMILES
FC1=C(N[C@@H]2CCCC[C@@H]2N)N=C(C3=CN(C)N=C3)C4=C1CNC4=O.Cl
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Synonyms
TAK-659 monohydrochloride; CB-659 monohydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
H2O : 2 mg/mL (5.25 mM; ultrasonic and adjust pH to 3 with HCl)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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]
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.6257 mL | 13.1285 mL | 26.2571 mL | 65.6426 mL |
| 5 mM | 0.5251 mL | 2.6257 mL | 5.2514 mL | 13.1285 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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