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DC-BPi-11 2758411-61-7

DC-BPi-11 2758411-61-7

CAS No.: 2758411-61-7

DC-BPi-11 is an inhibitor (blocker/antagonist) of bromodomain PHD finger transcription factor (BPTF) with IC50 of 698 nM
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DC-BPi-11 is an inhibitor (blocker/antagonist) of bromodomain PHD finger transcription factor (BPTF) with IC50 of 698 nM. DC-BPi-11 has a significant inhibitory effect on leukemia cell proliferation/growth.

Physicochemical Properties


CAS # 2758411-61-7
Related CAS # DC-BPi-11 hydrochloride
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 698 nM (BPTF)[1]
ln Vitro In human leukemia MV-4-11 cells, DC-BPi-11 (0.1 nM-1 μM; 24 h) suppresses BPTF with an EC50 value of 120 nM[1]. The proliferation of human leukemia MV-4-11 cells is greatly inhibited by DC-BPi-11 (0.01 μM-100 μM; 24 h) (IC50=0.89 μM), and downstream oncogene expression is decreased by DC-BPi-11 (2.5-20 μM; 24 h)[1]. The level of c-Myc protein is dose-dependently decreased by DC-BPi-11 (0.6-50 μM; 24 h)[1]. On normal cells, DC-BPi-11 is harmless and has negligible effects[1].
Cell Assay Western Blot Analysis[1]
Cell Types: Human leukemia MV-4-11 cells
Tested Concentrations: 0.6 μM, 1.8 μM, 5.6 μM, 16.6 μM, and 50 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Resulted depletion of c-Myc in a dose-dependent manner.

Apoptosis Analysis[1]
Cell Types: Human leukemia MV-4-11 cells
Tested Concentrations: 5 μM, 10 μM, 20 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Induced cell apoptosis by arresting cell cycle at G1 phase.
References [1]. Lu T, et al. Discovery of High-Affinity Inhibitors of the BPTF Bromodomain. J Med Chem. 2021 Aug 26;64(16):12075-12088.

Solubility Data


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
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.)