Size | Price | Stock | Qty |
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500μg |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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Purity: =100%
Targets |
JAK2; STAT3/5
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ln Vitro |
In Ba/F3-hMpl cells, butyzamide (3 μM; 15 min) phosphorylates JAK2, STAT3, STAT5, and MAPK [1]. Human CD34+ hematopoietic progenitors are stimulated by butyzamide (3 μM; 48 hours) to produce polyploid megakaryocytes and megakaryocytes that form colony-forming units [1].
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ln Vivo |
Butanamide (10 mg/kg, 50 mg/kg; lateral; once daily for 20 days) elevates human prospective levels in NOG implanted with human fetal liver-derived CD34+ cells [1]. < br/>
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Enzyme Assay |
For the establishment of Ba/F3-hMpl, Ba/F3-mMpl and Ba/F3-hMpl(H499L) cells, Ba/F3 cells were transfected with each constructed plasmid by electroporation. The cells were cloned by a limiting dilution method in the presence of 2 mg/mL geneticin. For the establishment of Ba/F3-mMpl(L490H) cells, 293GP2 packaging cells were transfected with pQCXIP-mMpl(L490H) and pVSV-G vector (Invitrogen) by Fugene 6, according to the manufacturer’s protocol. The culture supernatant was collected and used to infect Ba/F3 cells. These established stable cell lines proliferated in response to rmIL-3, as well as parental Ba/F3 cells, and appeared to maintain the character of parental Ba/F3 cells [1].
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Cell Assay |
Cells were cultured at a density of 7.5×10 cells/200 μL in 96-well plates with various concentrations of butyzamide or recombinant cytokines. The plates were incubated for 48 h at 37°C in a humidified chamber with 5% CO2, and 10 μL WST-8 reagent were added to each well during the last 4 h of culture. The absorbance was measured at a wavelength of 450 nm using a 96-well microplate reader, Model 680 [1].
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Animal Protocol |
Immunodeficient NOD/Shi-scid,IL-2Rγ (NOG) mice (8–10 weeks old) were irradiated with 2.4 Gy (125 kV, 10 mA, 0.45 Gy/min) by MBR-1520R-3 (Hitachi Medico, Tokyo, Japan), and on the next day, 6.7×10 human fetal liver (FL)-derived CD34 cells were transplanted intravenously. Two months after transplantation, the NOG mice were randomized into three groups, based on the number of human platelets and body weight. The vehicle or butyzamide at a dose of 10 or 50 mg/kg was administered orally for 21 days. The numbers of human platelets and megakaryocytes were calculated as described below [1].
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References |
[1]. Nogami W, et al. The effect of a novel, small non-peptidyl molecule butyzamide on human thrombopoietin receptor and megakaryopoiesis. Haematologica. 2008 Oct;93(10):1495-504.
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Molecular Formula |
C29H32CL2N2O5S
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Molecular Weight |
591.55
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Exact Mass |
590.14089
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CAS # |
1110767-45-7
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Appearance |
White to off-white solid
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LogP |
7.6
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tPSA |
126Ų
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SMILES |
C(O)(=O)/C(/C)=C/C1=C(Cl)C=C(C(NC2=NC(C3=CC=CC(C(OCCC)C(C)(C)C)=C3OC)=CS2)=O)C=C1Cl
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InChi Key |
BBEZGQPYGPBSLA-FOWTUZBSSA-N
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InChi Code |
InChI=1S/C29H32Cl2N2O5S/c1-7-11-38-25(29(3,4)5)19-10-8-9-18(24(19)37-6)23-15-39-28(32-23)33-26(34)17-13-21(30)20(22(31)14-17)12-16(2)27(35)36/h8-10,12-15,25H,7,11H2,1-6H3,(H,35,36)(H,32,33,34)/b16-12+
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Chemical Name |
(E)-3-[2,6-dichloro-4-[[4-[3-(2,2-dimethyl-1-propoxypropyl)-2-methoxyphenyl]-1,3-thiazol-2-yl]carbamoyl]phenyl]-2-methylprop-2-enoic acid
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~169.05 mM)
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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 | 1.6905 mL | 8.4524 mL | 16.9047 mL | |
5 mM | 0.3381 mL | 1.6905 mL | 3.3809 mL | |
10 mM | 0.1690 mL | 0.8452 mL | 1.6905 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.