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100mg | ||
250mg | ||
500mg |
ln Vitro |
HIF is a heterodimer made up of two bHLH-PAS (Basic Helix Loop Helix-Per-ARNT-Sim) subunits, which include aryl hydrocarbon receptors and HIF-α homologs (HIF-1α, -2α, and -3α). The ARNT/CCC complex formation for both coactivators is significantly reduced by KG-548 (0-250 μM; 16 hr overnight). Additionally, KG-548 (0-2 mM; 16 hr overnight) in vitro and cellular localization ARNT PAS-B/TACC3 composite was linked in a dosage-dependent way (320 μM). interferes with the ARNT2 PAS-B/TACC3 reaction [1]. The shock caused by FaDu hypopharyngeal thyroid glycolysis is greatly inhibited by KG-548 [2].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293T cell lysates Tested Concentrations: 0, 5, 50, IC50 is 25 μM[1]. 100, 250, 500 μM and 1 mM, 2 mM Incubation Duration: 16 hrs (hours) Experimental Results: ARNT/TACC3 interaction weakened from 5 μM to 500 μM in a dose-dependent manner and diminished the intensity of ARNT protein associated with immunoprecipitated TACC3 protein82 % (500 μM), 59% (1 mM), 43% (2 mM). |
References |
[1]. Guo Y, et al. Regulating the ARNT/TACC3 axis: multiple approaches to manipulating protein/protein interactions with small molecules. ACS Chem Biol. 2013 Mar 15;8(3):626-35.
[2]. Kleszcz R, et al. The inhibition of c-MYC transcription factor modulates the expression of glycolytic and glutaminolytic enzymes in FaDu hypopharyngeal carcinoma cells. Adv Clin Exp Med. 2018 Jun;27(6):735-742. |
Molecular Formula |
C9H4F6N4
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Molecular Weight |
282.145
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CAS # |
175205-09-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC(C1C([H])=C(C2N=NN([H])N=2)C([H])=C(C(F)(F)F)C=1[H])(F)F
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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) |
DMSO : ~100 mg/mL (~354.42 mM)
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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 | 3.5442 mL | 17.7211 mL | 35.4421 mL | |
5 mM | 0.7088 mL | 3.5442 mL | 7.0884 mL | |
10 mM | 0.3544 mL | 1.7721 mL | 3.5442 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.