| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In FLT3-dependent AML cell lines and SYK-dependent DLBCL cell lines, TAK-659 reduces cell growth [1][3]. In LMP2A/MYC cells, TAK-659 (5 µM; 1-24 hours) causes Casp3 activation, which is visible at 4 hours and reaches its peak after 8 hours of treatment [4]. In Ramos cells, TAK-659 (0.01-10 μM; 1 hour) enhances phospho-ERK1/2 and induces the production of phospho-Syk at Tyr525 and Tyr352 [2].
|
|---|---|
| ln Vivo |
TAK-659 (100 mg/kg/day; oral; for 10 days) totally prevented splenomegaly and tumor formation in LMP2A/MYC mice in pre-tumor and tumor cell metastasis assays [4]. Treatment with TAK-659 destroys tumor cells in the spleen and tumor, but not host cells [4]. Treatment with TAK-659 prevents bone marrow metastasis of tumor cells [4].
|
| Cell Assay |
Apoptosis analysis [4]
Cell Types: LMP2A/MYC Cell Tested Concentrations: 5 µM Incubation Duration: 1 hour, 2 hrs (hours), 4 hrs (hours), 8 hrs (hours), 24 hrs (hours) Experimental Results: Induction of apoptosis in LMP2A/MYC lymphoma cells. Western Blot Analysis[2] Cell Types: Ramos Cell Tested Concentrations: 0.01 μM, 0.1 μM, 1 μM, 10 μM Incubation Duration: 1 hour Experimental Results: Phospho-Syk at Tyr525 and Tyr352 and Phospho-ERK1/2 in stimulated Ramos expression-enhanced cells. |
| Animal Protocol |
Animal/Disease Models: LMP2A/MYC double transgenic mice [4]
Doses: 100 mg/kg/day Route of Administration: po (oral gavage); 10 days Experimental Results: Inhibition of LMP2A-induced tumor cell survival in vivo. |
| References |
|
| Additional Infomation |
Mivavotinib is an inhibitor of spleen tyrosine kinase (syk), with potential anti-inflammatory, immunomodulating, and antineoplastic activities. Upon administration, mivavotinib may inhibit the activity of syk, which abrogates downstream B-cell receptor (BCR) signaling and leads to an inhibition of B-cell activation, chemotaxis, adhesion and proliferation. Syk, a BCR-associated non-receptor tyrosine kinase that mediates diverse cellular responses, including proliferation, differentiation, and phagocytosis, is expressed in hematopoietic tissues and is often overexpressed in hematopoietic malignancies.
See also: Mivavotinib Citrate (annotation moved to). |
| Molecular Formula |
C17H21FN6O
|
|---|---|
| Molecular Weight |
344.386646032333
|
| Exact Mass |
344.176
|
| CAS # |
1312691-33-0
|
| Related CAS # |
TAK-659 hydrochloride;1952251-28-3
|
| PubChem CID |
53252276
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
0.5
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
508
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CN1C=C(C=N1)C2=NC(=C(C3=C2C(=O)NC3)F)N[C@@H]4CCCC[C@@H]4N
|
| InChi Key |
MJHOMTRKVMKCNE-NWDGAFQWSA-N
|
| InChi Code |
InChI=1S/C17H21FN6O/c1-24-8-9(6-21-24)15-13-10(7-20-17(13)25)14(18)16(23-15)22-12-5-3-2-4-11(12)19/h6,8,11-12H,2-5,7,19H2,1H3,(H,20,25)(H,22,23)/t11-,12+/m0/s1
|
| Chemical Name |
6-[[(1R,2S)-2-aminocyclohexyl]amino]-7-fluoro-4-(1-methylpyrazol-4-yl)-1,2-dihydropyrrolo[3,4-c]pyridin-3-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9037 mL | 14.5184 mL | 29.0368 mL | |
| 5 mM | 0.5807 mL | 2.9037 mL | 5.8074 mL | |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9037 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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