Physicochemical Properties
| Molecular Formula | C33H38BRFN4O |
| Molecular Weight | 605.58 |
| Appearance | Typically exists as solid at room temperature |
| 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) |
Biological Activity
| Targets | IC50: 0.8 μM (BLM)[1] |
| ln Vitro | BLM-IN-2 (0–20 μM) exhibits a strong inhibitory impact on BLM, with IC50 values of 0.8 μM and 2.3 μM for binding and unwinding DNA, respectively [1]. BLM-IN-2 is mildly hazardous to normal cells but cytotoxic to CRC cells in a BLM-dependent manner [1]. In CRC cells, BLM-IN-2 (3 μM; 48 h) causes DNA damage and throws off HRR levels while blocking BLM at DSB locations [1]. BLM-IN-2 (0–5 μM; 48 h) efficiently prevents CRC cell invasion, proliferation, cell cycle arrest, and apoptosis [1]. |
| Cell Assay |
Cell Proliferation Assay[1] Cell Types: HCT116 cells; HCT116, SW480 and RKO cells Tested Concentrations: 0-5 μM; 0.5, 1, 2 μM Incubation Duration: 48 h; 10 days Experimental Results: Induced proliferation arrest. Completely inhibited the growth of cancer cells at the concentration around 2 μM, had a good anti-CRC activity. Apoptosis Analysis[1] Cell Types: HCT116, SW480 and RKO cells Tested Concentrations: 1 μM Incubation Duration: 48 h Experimental Results: Induced apoptosis and necrosis in HCT116, SW480 and RKO. Cell Cycle Analysis[1] Cell Types: HCT116, SW480 and RKO cells Tested Concentrations: 4 μM Incubation Duration: 48 h Experimental Results: Changed the cell proportion of the S or G2/M phase in CRC cells, arrested the cell cycle at the S phase in HCT116 and SW480 and arrested the cell cycle of HCT116, SW480 and RKO at the G2/M phase. Cell Invasion Assay[1] Cell Types: HCT116 cells Tested Concentrations: 0.25, 0.5, 1, 2, 4 μM Incubation Duration: 48 h Experimental Results: Obviously diminished the invasion in HCT116 cells with an IC50 value of 1.0 μM and had inhibitory on CRC invasio |
| References | [1]. Jia-Li Tu, et al. Design, synthesis and evaluation of N3-substituted quinazolinone derivatives as potential Bloom's Syndrome protein (BLM) helicase inhibitor for sensitization treatment of colorectal cancer. Eur J Med Chem. 2022 Nov 21;246:114944. |
Solubility Data
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6513 mL | 8.2565 mL | 16.5131 mL | |
| 5 mM | 0.3303 mL | 1.6513 mL | 3.3026 mL | |
| 10 mM | 0.1651 mL | 0.8257 mL | 1.6513 mL |