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100mg | ||
250mg | ||
500mg |
ln Vitro |
MCF-7 cells' ability to grow is inhibited by buclizine (0.1–100 μM; 72 hours) [2]. In a dose-dependent manner, buclizine (9.625-77 μM; 72 hours) stops the cell cycle in the G1 phase [2]. In MCF-7 cells, buclizine (0-75 μM; 72 hours) boosts pro-apoptotic MCL-1S expression while decreasing the expression of cell cycle regulatory proteins and TCTP (translationally controlled tumor protein) [2].
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ln Vivo |
Rats are strongly teratogenic to buclizine diHClide (30-200 mg/kg; gestation days 10 to 15 and 12 to 15) [3].
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Cell Assay |
Cell Proliferation Assay[2]
Cell Types: MCF-7 Cell Tested Concentrations: 0-100 μM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated considerable growth inhibition (IC50=19.18 μM). Cell cycle analysis[2] Cell Types: MCF-7 Cell Tested Concentrations: 9.625, 19.25, 38.5 and 77 μM Incubation Duration: 72 hrs (hours) Experimental Results: The percentage of cells in G1 phase increased to 73% at 77 μM. Western Blot Analysis[2] Cell Types: MCF-7 Cell Tested Concentrations: 0-75 μM Incubation Duration: 72 hrs (hours) Experimental Results: TCTP expression diminished by 40% at 75 μM. The expression of cyclin D1, cyclin D3, CDK2 and CDK4 diminished after 72 hrs (hours). |
Animal Protocol |
Animal/Disease Models: 87 adult female rats, weighing 240±20 grams [3]
Doses: 30, 40, 60, 100, 200 mg/kg Doses: 30-200 mg/kg; pregnancy days 10 to 15 and Results on days 12 to 15: Dose levels of 60-100 mg/kg resulted in malformations in 100% of the pups. |
References |
[1]. Gamal A E Mostafa, et al. Buclizine. Profiles Drug Subst Excip Relat Methodol. 2011;36:1-33.
[2]. Ean-Jeong Seo, et al. Interaction of antihistaminic drugs with human translationally controlled tumor protein (TCTP) as novel approach for differentiation therapy. Oncotarget. 2016 Mar 29;7(13):16818-39. [3]. C T King, et al. Teratogenic effect of buclizine and hydroxyzine in the rat and chlorcyclizine in the mouse. Am J Obstet Gynecol. 1966 May 1;95(1):109-11. |
Molecular Formula |
C28H33N2CL
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Molecular Weight |
433.02802
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CAS # |
82-95-1
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Related CAS # |
Buclizine dihydrochloride;129-74-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
ClC1C=CC(C(C2C=CC=CC=2)N2CCN(CC3C=CC(C(C)(C)C)=CC=3)CC2)=CC=1
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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 |
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) |
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
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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 | 2.3093 mL | 11.5465 mL | 23.0931 mL | |
5 mM | 0.4619 mL | 2.3093 mL | 4.6186 mL | |
10 mM | 0.2309 mL | 1.1547 mL | 2.3093 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.