Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
BRD4 BRD2 Cereblon
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ln Vitro |
With an IC50 value of 12.25 nM, PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) exhibits anti-proliferation activity. In MV4-11 cells, the BRD4 protein is decreased extremely effectively after ≥8 hours of treatment[1]. With an IC50 value of 12.25 nM, PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) exhibits anti-proliferation activity. In MV4-11 cells, the BRD4 protein is decreased extremely effectively after ≥8 hours of treatment[1]. MV4-11 apoptotic lines are induced by PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours)[1]. In six NCI leukemia cell lines, PROTAC BRD2/BRD4 degrader-1 demonstrates strong anti-proliferative action. The three leukemia cell lines' GI50 values were less than 50 nM, which is in line with the activity of leukemia MV4-11 cells[1]. With regard to prostate cancer (22RV1 IC50: 0.081 μM), colon cancer (colo-205 IC50: 0.1557 μM), and thyroid cancer (TT IC50: 0.037451 μM), PROTAC BRD2/BRD4 degrader-1 exhibits good anti-proliferation activity[1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MV4- 11 leukemia cells Tested Concentrations: 100 nM Incubation Duration:≥8 hrs (hours) Experimental Results: The BRD4 protein was diminished very efficiently. Western Blot Analysis[1] Cell Types: MV4-11 leukemia cells Tested Concentrations: 10, 50, 100, 500 nM Incubation Duration: 18 hrs (hours) Experimental Results: Performed depletion selectivity for BRD4 and BRD2 over BRD3, with good selectivity intra-BET proteins selectivity. |
References |
[1]. Jiang F, et al. Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2019 Nov 11:115181.
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Molecular Formula |
C39H38N6O9S
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Molecular Weight |
766.82
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CAS # |
2570470-42-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1=C(C=C2C(=CC=C3C2=C1C(=O)N3C)NS(=O)(=O)C1=C(C=CC=C1)OC)CCC(NCCCCNC1C2C(=O)N(C3C(=O)NC(=O)CC3)C(C=2C=CC=1)=O)=O
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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 | 1.3041 mL | 6.5204 mL | 13.0409 mL | |
5 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL | |
10 mM | 0.1304 mL | 0.6520 mL | 1.3041 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.