| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BJ-2302 inhibits the Src-regulated PI3K/AKT and Ras/Raf/ERK signaling pathways in MDA-MB-231 cells and inhibits the invasion of MDA-MB-231 cells[1]. BJ-2302 (0.01-10 µM; 18 h) inhibits serum-induced invasion of MDA-MB-231 triple-negative breast cancer (TNBC) cells, with an IC50 of 0.08 µM and an IC90 of 0.71 µM[3]. BJ-2302 (0.01-10 µM) downregulates the mRNA and protein expression of basal CTSS and MMP-9 in MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner[3]. BJ-2302 (0.01–1 µM) inhibited NF-κB nuclear translocation in MDA-MB-231 triple-negative breast cancer (TNBC) cells in vitro in a concentration-dependent manner, and also inhibited PI3K/Akt phosphorylation and phosphorylation of molecules in the Ras/Raf/ERK pathway [3]. BJ-2302 (0.01–10 µM; 73 h) inhibited serum-induced proliferation of MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, and completely inhibited cell proliferation at a concentration of 1 µM [3]. BJ-2302 (0.01–1 µM; 19–73 h) inhibited 5-HT (5-hydroxytryptamine)-induced proliferation, invasion, CTSS/MMP-9 expression, and Src phosphorylation of MDA-MB-231 triple-negative breast cancer (TNBC) cells in vitro in a concentration-dependent manner [3].
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|---|---|
| ln Vivo |
BJ-2302 (1 mg/kg; intraperitoneal injection; once daily for 25 days) significantly inhibited the growth of triple-negative mammary tumors in BALB/c nude mice without causing progressive weight loss [3]. BJ-2302 (3–30 pmol/CAM; administered at cell seeding; treatment lasting 5 days) showed concentration-dependent inhibition of tumor growth, angiogenesis, and metastasis in triple-negative breast cancer in a chicken embryo chorioallantoic membrane (CAM) xenograft model [3].
|
| Cell Assay |
Cell invasion assay [3]
Cell Types: MDA-MB-231 human triple-negative breast cancer (TNBC) cells Tested Concentrations: 0.01, 0.1, 1 and 10 µM Incubation Duration: 18 hours Experimental Results: It inhibited serum-induced MDA-MB-231 cell invasion in a concentration-dependent manner, with an IC50 of 0.08 µM and an IC90 of 0.71 µM. Its maximum inhibitory effect was stronger than that of Z-FL-COCHO or batimastat, the latter two of which had IC90 values greater than 10 µM. |
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (7-8 weeks old, female, subcutaneous model of triple-negative breast cancer) [3]
Doses: 1 mg/kg Route of Administration: Intraperitoneal injection; once daily for 25 days Experimental Results: Significantly inhibited tumor volume and weight, with efficacy superior to Z-FL-COCHO (1 mg/kg) or batimastatine (30 mg/kg). Compared with the control group and other treatment groups, the in vivo bioluminescence imaging signal of the tumor was significantly reduced. No progressive weight loss was induced. Animal/Disease Models:Fertilized chicken embryos (developing triple-negative breast cancer CAM xenograft model) [3] Doses: 3 pmol/CAM; 30 pmol/CAM Route of Administration: At cell inoculation; maintenance for 5 days Experimental Results: It inhibited tumor growth and tumor-induced angiogenesis in a concentration-dependent manner, and its efficacy was superior to Z-FL-COCHO (30 pmol/CAM) or Batimastat (300 pmol/CAM). It significantly inhibited the metastasis of MDA-MB-231-luc2-tdTomato cells to the lungs, liver and CAM base, as evidenced by a reduction in red fluorescently labeled cancer cells and a decrease in human HPRT mRNA expression in these tissues, and its activity was stronger than Z-FL-COCHO or Batimastat. |
| References |
|
| Molecular Formula |
C9H10N2O2
|
|---|---|
| Molecular Weight |
178.19
|
| CAS # |
1631056-29-5
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C1NC2=C(C1)C(C)=C(O)C(C)=N2
|
| 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 | 5.6120 mL | 28.0599 mL | 56.1199 mL | |
| 5 mM | 1.1224 mL | 5.6120 mL | 11.2240 mL | |
| 10 mM | 0.5612 mL | 2.8060 mL | 5.6120 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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