| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
DC-BPi-03 specifically targets the BPTF bromodomain (BPTF-BRD). BPTF (bromodomain PHD finger transcription factor) is a component of the NURF (nucleosome remodeling factor) complex and plays a role in chromatin remodeling and gene transcription. By inhibiting the BPTF bromodomain, the compound disrupts the interaction of BPTF with acetylated histones, potentially affecting gene expression programs involved in cancer.
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|---|---|
| ln Vitro |
In vitro, DC-BPi-03 potently inhibits BPTF-BRD with an IC₅₀ of 698.3 nM and a Kd of 2.81 μM. These values indicate a strong binding affinity and potent inhibitory activity against the target bromodomain. The compound's activity suggests potential for modulating BPTF-dependent pathways in cancer cells.
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| ln Vivo |
In vivo activity of DC-BPi-03 is not extensively detailed in publicly available sources. As a potent BPTF-BRD inhibitor, it is being investigated for its potential anti-cancer phenotype in leukemia.
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| Enzyme Assay |
The binding affinity of DC-BPi-03 to BPTF-BRD is assessed using biochemical assays such as surface plasmon resonance (SPR) or AlphaScreen to measure the Kd. Inhibitory activity (IC₅₀) is determined using competition binding assays with a labeled probe.
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| Cell Assay |
Cellular assays for DC-BPi-03 involve treating leukemia cell lines with the compound and assessing cell viability, proliferation, and changes in gene expression related to BPTF function.
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| Animal Protocol |
In vivo studies are conducted in mouse xenograft models of leukemia. The compound is administered via intraperitoneal (i.p.) injection or oral gavage, and tumor growth inhibition is monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DC-BPi-03 are not extensively detailed in publicly available sources. The compound is formulated in DMSO for in vitro studies.
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| Toxicity/Toxicokinetics |
DC-BPi-03 is intended for research use only and is not approved for clinical use. Its toxicological profile would be evaluated in preclinical studies.
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| References | |
| Additional Infomation |
DC-BPi-03 is a potent and selective inhibitor of the BPTF bromodomain, a promising target for epigenetic cancer therapy. It is being studied for its potential in leukemia research. The compound was discovered and characterized in a study published in the Journal of Medicinal Chemistry.
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| Molecular Formula |
C14H14N4O2S
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|---|---|
| Molecular Weight |
302.351561069489
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| Exact Mass |
302.083
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| CAS # |
2758411-46-8
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| PubChem CID |
155903113
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
464
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNC1=NC(=NC(=C1)C2=CC3=C(C=C2)NC=C3)S(=O)(=O)C
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| InChi Key |
RTONKOFFKFVXAW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14N4O2S/c1-15-13-8-12(17-14(18-13)21(2,19)20)9-3-4-11-10(7-9)5-6-16-11/h3-8,16H,1-2H3,(H,15,17,18)
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| Chemical Name |
6-(1H-indol-5-yl)-N-methyl-2-methylsulfonylpyrimidin-4-amine
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: ~33.3 mg/mL (~110.2 mM; with ultrasonication and warming by heating to 80°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 3.33 mg/mL (11.01 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (33.3 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 3.33 mg/mL (11.01 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (33.3 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: 3.33 mg/mL (11.01 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (33.3 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3074 mL | 16.5371 mL | 33.0743 mL | |
| 5 mM | 0.6615 mL | 3.3074 mL | 6.6149 mL | |
| 10 mM | 0.3307 mL | 1.6537 mL | 3.3074 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.
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