GSK973
Based on 1 Customer Validation
GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 2138473-38-6
- Formula: C23H23FN2O4
- Molecular Weight:410.44
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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BRD4 BD2 7.8 (pIC50) |
BRD2 BD2 7.5 (pIC50) |
BRD3 BD2 7.8 (pIC50) |
BRDT BD2 7.4 (pIC50) |
BRD4 BD2 8.7 (pKd) |
BRD2 BD2 8.3 (pKd) |
BRD3 BD2 8.5 (pKd) |
BRDT BD2 8.3 (pKd) |
GSK973 (3 mg/kg; p.o) treatment shows the Fpo of 48%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar Han Rats[1]
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Dosage:1 mg/kg (Pharmacokinetic Analysis)
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Administration:I.v.
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Result:The CL, CIrenal, Vss, and T1/2 were 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.
Chemical Information
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CAS No. 2138473-38-6
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Appearance Solid
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Molecular Weight 410.44
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Formula C23H23FN2O4
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Color Off-white to light yellow
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SMILES
[H][C@]1([C@@H]2NC(C3=CC(C(NC)=O)=C4C([C@@H]([C@H](O4)CF)C5=CC=CC=C5)=C3)=O)[C@]2([H])COC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (304.55 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)
Purity & Documentation
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Data Sheet (277 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)
- 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 | 2.4364 mL | 12.1820 mL | 24.3641 mL | 60.9102 mL |
| 5 mM | 0.4873 mL | 2.4364 mL | 4.8728 mL | 12.1820 mL | |
| 10 mM | 0.2436 mL | 1.2182 mL | 2.4364 mL | 6.0910 mL | |
| 15 mM | 0.1624 mL | 0.8121 mL | 1.6243 mL | 4.0607 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2182 mL | 3.0455 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL | 2.4364 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8121 mL | 2.0303 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5228 mL | |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4873 mL | 1.2182 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6091 mL |
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