Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK973 is a highly selective and orally bioavailable inhibitor that targets the second bromodomains (BD2s) of the BET family. It exhibits a pIC 50 of 7.8 and a pK d of 8.7 specifically for BRD4 BD2. Additionally, GSK973 demonstrates a remarkable selectivity of 1600-fold for BRD4 BD2 over BRD4 BD1. Moreover, it displays good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC 50 ranging from 7.4 to 7.8 and pK d ranging from 8.3 to 8.5.
Pack Size | Availability | Price/USD | Quantity |
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5 mg | Inquiry | $ 970.00 |
Description | GSK973 is a highly selective and orally bioavailable inhibitor that targets the second bromodomains (BD2s) of the BET family. It exhibits a pIC 50 of 7.8 and a pK d of 8.7 specifically for BRD4 BD2. Additionally, GSK973 demonstrates a remarkable selectivity of 1600-fold for BRD4 BD2 over BRD4 BD1. Moreover, it displays good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC 50 ranging from 7.4 to 7.8 and pK d ranging from 8.3 to 8.5. |
In vivo | Treatment with GSK973 at a dosage of 1 mg/kg administered intravenously (i.v.) demonstrated pharmacokinetic properties in male Wistar Han rats, including a clearance (CL) of 73 mL/min/kg, a renal clearance (CI renal) of 4 mL/min/kg, a steady-state volume of distribution (V ss) of 2.1L/kg, and a half-life (T 1/2) of 0.6 hours. Additionally, when administered orally (p.o) at a dose of 3 mg/kg, GSK973 exhibited an oral bioavailability (F po) of 48%. These findings provide insights into the drug's absorption, distribution, metabolism, and excretion characteristics following different routes of administration[1]. |
Synonyms | GSK973 |
Molecular Weight | 410.445 |
Formula | C23H23FN2O4 |
CAS No. | 2138473-38-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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GSK973 2138473-38-6 GSK-973 GSK 973 inhibitor inhibit