| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BPRCX 807 (1.5 h) had an IC50 value of 40.4 nM against HEK293T cells[1]. BPRCX 807 had an EC50 value of 48.1 nM against CCRF-CEM cells[1]. BPRCX 807 (10 μM, 24-72 h) significantly inhibited CXCL12-induced accelerated wound healing in HCA-1 cells[1]. BPRCX 807 (0.1-1 μM, 17.5 h) significantly reduced the number of migrating HCA-1 cells at a concentration of 1 μM[1]. BPRCX 807 (10-20 μM, 24-48 h) inhibited hypoxia-induced increase in the expression of interstitial markers in HCA-1 cells in a dose-dependent manner and alleviated hypoxia-induced decrease in the expression of epithelial markers in HCA-1 cells[1]. BPRCX 807 (5-20 μM, 24 h) significantly inhibited CXCL12-mediated ERK and Akt phosphorylation in HCA-1 and JHH-7 cells [1].
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|---|---|
| ln Vivo |
BPRCX 807 (15 mg/kg, subcutaneous injection, once daily for 14 days) alone or in combination with sorafenib significantly inhibited tumor growth in HCA-1 cell allogeneic and JHH-7 cell xenograft models [1]. BPRCX 807 (15 mg/kg, subcutaneous injection, once daily for 14 days) in combination with anti-PD-1 antibody recruited T cells and synergistically inhibited the growth of HCA-1 cell allogeneic mice [1].
|
| Cell Assay |
Cell Migration Assay [1]
Cell Types: HCA-1 cells Tested Concentrations: 10 μM Incubation Duration: 0 h, 24 h, 48 h, 72 h Experimental Results: Significantly inhibited CXCL12-induced accelerated wound closure in HCA-1 cells. Real Time qPCR[1] Cell Types: Hypoxia-induced HCA-1 cells Tested Concentrations: 10 μM, 20 μM Incubation Duration: 24 h, 48 h Experimental Results: Increased in mesenchymal marker expression (including Slug, Fibronectin, N-cadherin, Vimentin, FOXC2, Zeb1, and Zeb2). Alleviated the hypoxia-induced decrease in epithelial markers (E-cadherin, MTA-3, CLDN3, and CLDN5). |
| Animal Protocol |
Animal/Disease Models: HCA-1 or JHH-7 cells were orally implanted into the livers of 7-week-old C3H/HeNCrNarl mice and 9-week-old BALB/cAnN.Cg Foxnlnu/CrlNarl mice, respectively[1].
Doses: 15 mg/kg Route of Administration: S.c., once daily for 14 days Experimental Results: Significantly inhibited tumor growth when used alone. The effect is strongest when used in combination with sorafenib. Combined use significantly prolongs overall survival. Reduced tumor-associated macrophage (TAM) infiltration (F4/80+ cells). Reprogramed TAMs to the M1 phenotype (increased CD86+) and suppresses the M2 phenotype (decreased CD206+). Increased cytotoxic CD8+ T cell infiltration. Animal/Disease Models: HCA-1 cells were in situ implanted into 7-week-old C3H/HeNCrNarl mice. For combined anti-PD-1 immunotherapy, mice were intraperitoneally injected with anti-mouse PD-1 antibodies 10 days after tumor implantation[1]. Doses: 15 mg/kg Route of Administration: S.c., once daily for 14 days Experimental Results: When used in combination with Anti-PD-1, it significantly increased the infiltration of CD4+ and CD8+ T cells within tumors. Synergistically inhibited tumor growth (reducing it by 95%) and lung metastasis. |
| References |
| Molecular Formula |
C31H51N9O4
|
|---|---|
| Molecular Weight |
613.79
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| CAS # |
2236595-58-5
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| Appearance |
Typically exists as solids at room temperature
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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 | 1.6292 mL | 8.1461 mL | 16.2922 mL | |
| 5 mM | 0.3258 mL | 1.6292 mL | 3.2584 mL | |
| 10 mM | 0.1629 mL | 0.8146 mL | 1.6292 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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