Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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Targets |
Kd: 1.5 μM (PBRM1-BD2), 3.9 μM (PBRM1-BD5)[1] IC50: 0.26 μM (PBRM1-BD2)[1]
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ln Vitro |
Compound 16 (PBRM1-BD2-IN-5) (0–10 μM; 5 days) inhibits LNCaP cells that express PBRM1 and decreases the binding of full-length PBRM1 to acetylated histone peptides in cell lysates inside the PBAF complex[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: LNCaP cells expressing lentiviral shPBRM1 Tested Concentrations: 0, 0.1, 1 and 10 μM Incubation Duration: 5 days Experimental Results: demonstrated a more significant effect on LNCaP viability in cells with native PBRM1 levels than in cells with PBRM1 knockdown. decreased the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides. |
References |
[1]. Shishodia S, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13.
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Molecular Formula |
C15H13CLN2O
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Molecular Weight |
272.73
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CAS # |
2819989-61-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
N1C2=C(C(Cl)=CC=C2)C(=O)NC1C1=CC=CC(C)=C1
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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 (~366.66 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.5 mg/mL (9.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6666 mL | 18.3332 mL | 36.6663 mL | |
5 mM | 0.7333 mL | 3.6666 mL | 7.3333 mL | |
10 mM | 0.3667 mL | 1.8333 mL | 3.6666 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.