ChemicalBook CAS DataBase List 2138473-38-6

2138473-38-6

Name	INDEX NAME NOT YET ASSIGNED
CAS	2138473-38-6
Molecular Formula	C23H23FN2O4
Molecular Weight	410.45
MOL File	2138473-38-6.mol

Chemical Properties

Boiling point	550.0±50.0 °C(Predicted)
density	1.36±0.1 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO: 2mg/mL, clear
form	Solid
pka	13.82±0.20(Predicted)
color	Off-white to light yellow

Hazard Information

Uses

GSK973 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)[1].

Biological Activity

Orally availablepotent and selective pan-second bromodomain (BD2) inhibitor th at effectively inhibits LPS-induced MCP-1 release in human whole blood.

GSK973 is an orally availablepotent and selective pan-second bromodomain (BD2) inhibitor (BD2/BD1 pIC50 = 7.5/4.4/BRD27.8/4.5/BRD37.8/4.6/BRD47.4/4.5/BRDT) th at effectively inhibits LPS-induced MCP-1 release in human whole blood (pIC50 = 7.3; IC50 = 50 nM).

in vivo

GSK973 (1 mg/kg; i.v.) treatment shows the CL, CI_renal, V_ss, and T_1/2 are 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively^[1].
GSK973 (3 mg/kg; p.o) treatment shows the F_po of 48%^[1].

Animal Model:	Male Wistar Han Rats^[1]
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	I.v.
Result:	The CL, CI_renal, V_ss, and T_1/2 were 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.

IC 50

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)

References

[1] Preston A, et al. GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family. ACS Med Chem Lett. 2020;11(8):1581-1587. Published 2020 Jul 6. DOI:10.1021/acsmedchemlett.0c00247

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