| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
BRCA2-RAD51-IN-3 (compound 19) inhibited the protein-protein interaction of RAD51-BRCA2 in in vitro ELISA assays, with an EC50 of 29.35 μM and a maximum inhibition rate of 76%[1]. BRCA2-RAD51-IN-3 can directly bind to recombinant human RAD51, and its Kd value was 75.14 μM as determined by MST[1]. Nuclear magnetic resonance (NMR) displacement assays confirmed that BRCA2-RAD51-IN-3 (50 μM; 1 μM RAD51 plus 2-5 μM BRC4 peptide) can bind to the RAD51-BRCA2 interaction interface[1]. BRCA2-RAD51-IN-3 (10-80 μM) inhibited homologous recombination in BxPC-3 cells in a dose-dependent manner, with an IC50 of 21.74 μM and an inhibition rate of 81% at 80 μM[1]. BRCA2-RAD51-IN-3 (10-60 μM) inhibited homologous recombination in HEK-293 cells, reducing the proportion of cells with homologous recombination activity at 40 μM [1]. BRCA2-RAD51-IN-3 disrupted the formation of RAD51 aggregates in BxPC-3 cells following cisplatin-induced DNA damage, consistent with the inhibition of RAD51-BRCA2-mediated DNA repair [1]. BRCA2-RAD51-IN-3 (40 μM; 6 days, in combination with 10 μM olaparib) synergistically reduced cell viability in two-dimensional BxPC-3 and HPAC cells (interaction indices of 0.77 and 0.72, respectively), had no significant effect on the viability of normal H-6037 pancreatic epithelial cells, and induced apoptosis in BxPC-3 and HPAC cells, as evidenced by a significantly increased BAX/BCL2 ratio. BRCA2-RAD51-IN-3 (40-60 μM; 144 hours, used in combination with 10 μM olaparib) synergistically reduced the viability of three-dimensional BxPC-3 spheres, inhibited their growth, and induced their death, with a three-dimensional interaction index of 0.85 after 144 hours of treatment [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: BxPC-3 human pancreatic adenocarcinoma cells (two-dimensional culture) Tested Concentrations: 40 μM (used in combination with 10 μM olaparib) Incubation Duration: 6 days Experimental Results: No significant effect on cell viability; when used in combination with olaparib, it significantly enhanced anti-proliferative activity, with an interaction index of 0.77, indicating a synergistic effect. Cell viability assay [1] Cell Types: HPAC human pancreatic adenocarcinoma cells (2D culture) Tested Concentrations: 40 μM (used in combination with 10 μM olaparib) Incubation Duration: 6 days Experimental Results: No significant effect on cell viability; when used in combination with olaparib, it significantly enhanced antiproliferative activity, with an interaction index of 0.72, indicating a synergistic effect. Cell viability assay [1] Cell Types: H-6037 normal human pancreatic epithelial cells (two-dimensional culture) Tested Concentrations: 40 μM (used in combination with 10 μM olaparib) Incubation Duration: 6 days Experimental Results: This combination had no significant effect on cell viability.
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| References |
| Molecular Formula |
C21H14NNAO4
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|---|---|
| Molecular Weight |
367.33
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(C1=CC(C2=CC=C(C3=CC=CC=C3)O2)=NC4=CC=C(OC)C=C14)O[Na]
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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 | 2.7223 mL | 13.6117 mL | 27.2235 mL | |
| 5 mM | 0.5445 mL | 2.7223 mL | 5.4447 mL | |
| 10 mM | 0.2722 mL | 1.3612 mL | 2.7223 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.