Size | Price | |
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500mg | ||
1g | ||
Other Sizes |
Targets |
Ki: 11.97 nM (BRD3 BD1); 2.35 nM (BRD3 BD2) [1]. IC50: 6.31 nM (MV4-11 cell); 95.2 nM (MM.1 S cell) [1].
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ln Vitro |
GXF-111 (Compound 24) exhibits binding affinities with Ki values of 2.35 nM and 11.97 nM for BRD3 BD2 and BRD3 BD1, respectively [1]. MV4-11 and MM.1 S cell lines exhibit cellular activity in response to GXF-111, with IC50 values of 6.31 nM and 95.2 nM, respectively [1]. GXF-111 (2, 10 nM; 24 h) inhibits BET family protein degradation in MM.1 S cells with strong cell growth inhibitory action [1]. In seven human cancer cell lines, GXF-111(4 days) exhibits anti-proliferative action with IC50 values ranging from 6.31 nM to 17.25 μM[1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: MM.1 S cells; MM.1 S, HGC-27, and MCF-7 cells; Multiple cancer cell lines Tested Concentrations: 2, 10 nM; 0.1, 0.3, 1, 3 nM; 30 nM; 3, 10, 30, 100, 300 nM Incubation Duration: 24 h; 8 h; 1, 3, 6, 8, 24 h; 24 h Experimental Results: Efficiently depleted BRD3 and BRD4-L in MM.1 S cells at 2 nM. Dose-dependently depleted BRD3 and BRD4-L and partially depleted BRD2 at 10 nM. Had good degradation kinetics of BET proteins in three selected cancer cell lines, ie MM.1S, MCF-7, and HGC-27 cells. Only BRD3 and BRD4-L, were depleted dose-dependently in five cancer cell lines, ie HGC27, MCF-7, A549, Hela, and HepG2 cells. Cell Cycle Analysis[1] Cell Types: MM.1 S cell Tested Concentrations: 1, 3, 10, 30, 100, 300 nM Incubation Duration: 24 h Experimental Results: Dose-dependently induced cell cycle arrest at G1 phase. |
References |
[1]. Yan Z, et al. Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines. Eur J Med Chem. 2023;254:115381.
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Molecular Formula |
C42H42CLN7O3
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Molecular Weight |
728.28
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Appearance |
Typically exists as solid 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 | 1.3731 mL | 6.8655 mL | 13.7310 mL | |
5 mM | 0.2746 mL | 1.3731 mL | 2.7462 mL | |
10 mM | 0.1373 mL | 0.6865 mL | 1.3731 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.