GSK737
Based on 1 Customer Validation
GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC50 values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat.
For research use only. We do not sell to patients.
- Purity : 99.89%
- CAS No.: 2748687-95-6
- Formula: C20H21N5O2
- Molecular Weight:363.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
Chemical Information
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CAS No. 2748687-95-6
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Appearance Solid
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Molecular Weight 363.41
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Formula C20H21N5O2
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Color White to light yellow
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SMILES
C[C@@H](C1=CC=CC=N1)OC2=C(C3=CN(C)N=N3)C=C(C=C2)C(NC4CC4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (275.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7517 mL | 13.7586 mL | 27.5171 mL | 68.7928 mL |
| 5 mM | 0.5503 mL | 2.7517 mL | 5.5034 mL | 13.7586 mL | |
| 10 mM | 0.2752 mL | 1.3759 mL | 2.7517 mL | 6.8793 mL | |
| 15 mM | 0.1834 mL | 0.9172 mL | 1.8345 mL | 4.5862 mL | |
| 20 mM | 0.1376 mL | 0.6879 mL | 1.3759 mL | 3.4396 mL | |
| 25 mM | 0.1101 mL | 0.5503 mL | 1.1007 mL | 2.7517 mL | |
| 30 mM | 0.0917 mL | 0.4586 mL | 0.9172 mL | 2.2931 mL | |
| 40 mM | 0.0688 mL | 0.3440 mL | 0.6879 mL | 1.7198 mL | |
| 50 mM | 0.0550 mL | 0.2752 mL | 0.5503 mL | 1.3759 mL | |
| 60 mM | 0.0459 mL | 0.2293 mL | 0.4586 mL | 1.1465 mL | |
| 80 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8599 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6879 mL |