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| 10mg |
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| Targets |
DW71177 selectively targets the BD1 domain of BET proteins (BRD2, BRD3, BRD4, and BRDT). BET proteins are epigenetic readers that recognize acetylated lysines on histones and play a crucial role in regulating gene transcription. By selectively inhibiting BD1, DW71177 disrupts the binding of BET proteins to chromatin, thereby modulating the expression of oncogenes such as MYC, which is implicated in leukemia.
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| ln Vitro |
In vitro, DW71177 demonstrates potent inhibition of BET proteins and shows strong antileukemic activity. It has been shown to be effective in preclinical models of acute myeloid leukemia (AML). The compound's BD1-selectivity may offer advantages over pan-BET inhibitors by potentially reducing toxicity while maintaining efficacy.
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| ln Vivo |
In vivo, DW71177 has shown efficacy in models of acute myeloid leukemia. Its strong antileukemic activity translates to significant anti-tumor effects in animal models. Further details on specific in vivo models and dosing regimens are available in the primary literature.
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| Enzyme Assay |
In vitro binding assays for DW71177 involve assessing its affinity for the BD1 and BD2 domains of BET proteins. These are typically performed using AlphaScreen, TR-FRET, or surface plasmon resonance (SPR) assays with recombinant bromodomains. Selectivity for BD1 over BD2 is determined by comparing the IC50 or KD values for each domain.
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| Cell Assay |
In vitro cell-based studies are performed using acute myeloid leukemia (AML) cell lines. Cells are treated with varying concentrations of DW71177, and anti-proliferative effects are assessed using cell viability assays (e.g., MTT, CellTiter-Glo). The compound's effect on downstream targets, such as MYC expression, is evaluated by qPCR and Western blotting to confirm target engagement and mechanism of action.
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| Animal Protocol |
In vivo efficacy studies are conducted in mouse xenograft models of AML. DW71177 is typically administered orally or intraperitoneally. Tumor growth is monitored, and at the end of the study, tumors are harvested for analysis of target modulation (e.g., MYC levels) and pharmacodynamic biomarkers. Pharmacokinetic parameters are also assessed in these studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DW71177 are available from the supplier. The compound has a molecular weight of 384.48 and is soluble in DMSO at 40 mg/mL (104.04 mM). For in vivo studies, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline. Detailed PK parameters (half-life, bioavailability, clearance) can be obtained from the supplier's datasheet.
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| Toxicity/Toxicokinetics |
The toxicological profile of DW71177 is not extensively detailed in publicly available sources. As a research compound, its safety profile is being evaluated in preclinical studies. BET inhibitors are generally known to have on-target toxicities, such as effects on platelet counts and gastrointestinal issues, but the BD1-selectivity of DW71177 may offer an improved therapeutic window.
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| References | |
| Additional Infomation |
Additional information: DW71177 (CAS 2241311-72-6) has a molecular formula of C20H28N6O2 and a molecular weight of 384.48. It is a research compound with a purity of ≥95%, available from chemical suppliers. It is not approved for clinical use and is intended for research purposes only, particularly in the study of acute myeloid leukemia. The primary reference for this compound is Ali I, et al. Eur J Med Chem. 2024 Feb 5:265:116052.
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| CAS # |
2241311-72-6
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| Appearance |
White to off-white solid powder
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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 :~50 mg/mL (~130.05 mM; with sonication (<60°C))
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.50 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 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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: 2.5 mg/mL (6.50 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 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution 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. View More
Solubility in Formulation 3: 2.5 mg/mL (6.50 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. |
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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