Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 0.7 μM (Huh7), 1.4 μM (HepG2), 1.5 μM (SNU475), 7.9 μM (Hep3B), 2.4 μM (FOCUS), 5.2 μM (Hep40), 6.5 μM (PLC-PRF-5), 3.7 μM (Mahlavu), 0.9 μM (MCF7), 0.9 μM (MDA-MB231), 1.0 μM (MDA-MB468), 1.8 μM (SKBR3), 5.5 μM (ZR75), 7.6 μM (MCF10A)[1]
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ln Vitro |
Antitumor agent-79 (0.15-40 μM; 72 h) exhibits growth inhibitory actions against breast cancer and hepatocellular carcinoma cells with IC50 values ranging from 0.7 to 7.9 μM in vitro[1]. By inducing PARP cleavage, antitumor agent-79 (5 μM; 48 h) promotes cell apoptosis[1]. Cell line: Huh7, HepG2, SNU475, Hep3B, FOCUS, Hep40, PLC-PRF-5, Mahlavu, MCF7, MDA-MB231. Antitumor agent-79 Cell Cytotoxicity Assay[1]. The concentration of MDA-MB468, SKBR3, ZR75, and MCF10A cell lines was 0.15–40 μM. The incubation period was 72 hours. The results indicated that the compounds were cytotoxic to both breast cancer and hepatocellular carcinoma cells, with IC50 values for Huh7, HepG2, SNU475, Hep3B, FOCUS, Hep40, PLC-PRF-5, Mahlavu, MCF7, MDA-MB231, MDA-MB468, SKBR3, ZR75, and MCF10A cells, respectively.
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ln Vivo |
In mice xenograft models, anticancer agent-79 (40 mg/kg; po twice a week for 4 weeks) has antitumor effects[1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: Mahlavu, Huh7, MCF-7 and MDA-MB -231 cancer cells Tested Concentrations: 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Increased the PARP cleavage in both breast cancer cells (MCF7 and MDA-MB-231) and hepatocellular carcinoma cells (Mahlavu). Apoptosis Analysis[1] Cell Types: Mahlavu, Huh7, MCF-7 and MDA-MB-231 cancer cells Tested Concentrations: 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced cell apoptosis of cancer cells. |
Animal Protocol |
Animal/Disease Models: 6 −8 weeks old male athymic nude mice with hepatocellular carcinoma (Mahlavu cells) and breast (MDA MB-231 cells) xenografts[1]
Doses: 40 mg/kg Route of Administration: po (oral gavage); 40 mg/kg; twice a week for 4 weeks Experimental Results: Dramatically diminished the tumor volume following 4 weeks treatment with 40% reductions of tumor volumes in the Mahlavu xenografts. Resulted in about a 50% diminished in tumor volumes as compared to the control group in MDA-MB-231 xenografts. demonstrated well tolerated in vivo and neither significant bodyweight loss nor toxic effects or mortality were observed. |
References |
[1]. Turanlı S, et al. Vicinal Diaryl-Substituted Isoxazole and Pyrazole Derivatives with In Vitro Growth Inhibitory and In Vivo Antitumor Activity. ACS Omega. 2022 Oct 3;7(41):36206-36226.
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Molecular Formula |
C23H19CLN2O
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Molecular Weight |
374.86
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CAS # |
2750233-50-0
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Appearance |
Typically exists as solids (or liquids in special cases) 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 | 2.6677 mL | 13.3383 mL | 26.6766 mL | |
5 mM | 0.5335 mL | 2.6677 mL | 5.3353 mL | |
10 mM | 0.2668 mL | 1.3338 mL | 2.6677 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.