| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
In a time- and dose-dependent way, (E/Z)-BCI hydrochloride (2-10 μM; 72 hours) dramatically lowers the cell viability of gastric epithelial cells GES1, GC cell lines, and AGS cell lines [2]. In LPS-activated macrophages, (E/Z)-BCI hydrochloride (0.5–4 μM; 24 hours) dramatically reduces DUSP6 expression [1]. The expression of IL-1β, TNF-α, and IL-6 mRNA in LPS-activated macrophages was considerably reduced by (E/Z)-BCI hydrochloride (0.5-2 μM; 24 hours) treatment [1]. When LPS-activated macrophages are exposed to (E/Z)-BCI hydrochloride, they produce less ROS and activate the Nrf2 pathway [1]. The gastric cancer (GC) cells are more resistant to invasion, migration, and proliferation when exposed to (E/Z)-BCI hydrochloride, which also increases the cytotoxicity of CDDP (increased CDDP-induced cell death and apoptosis) [2].
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|---|---|
| ln Vivo |
Treatment with (E/Z)-BCI hydrochloride (35 mg/kg; intraperitoneal injection; every 7 days; for 4 weeks; female BALB/c nude mice) increased the effectiveness of cisplatin in the PDX model [2].
|
| Cell Assay |
Cell viability assay [2]
Cell Types: gastric epithelial cells GES1, GC cell lines (HGC27, SGC7901, MKN45, BGC823, MGC803, SNU216, NUGC4), AGS cell lines. Tested Concentrations: 2 μM, 4 μM, 6 μM, 8 μM, 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Cell viability was Dramatically diminished in a time- and dose-dependent manner. Western Blot Analysis[1] Cell Types: RAW264.7 macrophages (LPS-activated macrophages) Tested Concentrations: 0.5 μM, 1 μM, 2 μM, 4 μM Incubation Duration: 24 hrs (hours) Experimental Results: DUSP6 protein activated by LPS Dramatically down-regulated macrophages. RT-PCR[1] Cell Types: RAW264.7 macrophages (LPS-activated macrophages) Tested Concentrations: 0.5 μM, 1 μM, 2 μM Incubation Duration: 24 hrs (hours) Experimental Results: IL-1β, TNF-α, and IL Expression of -6 mRNA was Dramatically inhibited in LPS-activated macrophages. |
| Animal Protocol |
Animal/Disease Models: Patient-derived xenograft (PDX) model (4-5 weeks old female BALB/c nude mice) [2]
Doses: 35 mg/kg Route of Administration: intraperitoneal (ip) injection; once every 7 days; 4-week Experimental Results: Tumor weight in PDX models treated with CDDP was Dramatically suppressed compared to tumors in PDX model mice treated with either drug alone. |
| References |
[1]. Zhang F, et al. DUSP6 Inhibitor (E/Z)-BCI Hydrochloride Attenuates Lipopolysaccharide-Induced Inflammatory Responses in Murine Macrophage Cells via Activating the Nrf2 Signaling Axis and Inhibiting the NF-κB Pathway. Inflammation. 2019 Apr;42(2):672-681.
[2]. Wu QN,et al. Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistance. Cancer Lett. 2018 Jan 1;412:243-255. |
| Molecular Formula |
C₂₂H₂₃NO
|
|---|---|
| Molecular Weight |
317.42
|
| CAS # |
15982-84-0
|
| Related CAS # |
BCI;1245792-51-1;BCI hydrochloride;95130-23-7
|
| SMILES |
O=C1C2C=CC=CC=2C(/C/1=C/C1C=CC=CC=1)NC1CCCCC1
|
| Synonyms |
(E/Z)BCI; (E/Z) BCI
|
| 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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1504 mL | 15.7520 mL | 31.5040 mL | |
| 5 mM | 0.6301 mL | 3.1504 mL | 6.3008 mL | |
| 10 mM | 0.3150 mL | 1.5752 mL | 3.1504 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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