1-(7-(2-Methylsulfonyl-phenyl)-4-propoxy-1-aza-bicyclo[4.3.0]nona-2,4,6,8-tetraen-9-yl)-ethanone

Name	GSK2801
Synonyms	GSK2801 GSK 2801 GSK-2801 GSK2801 GSK-2801 1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone 1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone 1-[1-(2-Methanesulfonyl-phenyl)-7-propoxy-indolizin-3-yl]-ethanone 1-(7-(2-Methylsulfonyl-phenyl)-4-propoxy-1-aza-bicyclo[4.3.0]nona-2,4,6,8-tetraen-9-yl)-ethanone
CAS	1619994-68-1

Molecular Formula	C20 H21 N O4 S
Molar Mass	371.45
Density	1.23±0.1 g/cm3(Predicted)
Solubility	10 mM in DMSO
Storage Condition	-20°C
In vitro study	GSK2801 binds TAF1L(2) with an affinity K B of 0.31μM (K D : 3.2 μM) and a binding enthalpy change ΔH of −8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity K B of 0.826 μM (K D : 1.1 μM) and ΔH of −9.8 kcal/mol. GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC.
In vivo study	In order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.

Hazard Symbols	Xn - Harmful
Risk Codes	22 - Harmful if swallowed

Last Update：2024-01-02 23:10:35

biological activity	GSK2801 is an effective, selective, orally active and cell active acetyllysine competitive BAZ2A and BAZ2B bromide domain inhibitors with Kd values of 136 nM and 257 nM respectively. The selectivity of GSK2801 to BAZ2A/B is more than 50 times that of BRD4.
target	Kd: 136 nM (BAZ2A) and 257 nM (BAZ2B)
in vitro study	GSK2801 binds TAF1L(2) with an affinity K B of 0.31μM (K D : 3.2 μ M) and a binding enthalpy changeΔ H of − 8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity K B of 0.826 μ M (K D : 1.1 μ m) and Δ h of − 9.8 kcal/mol. GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC.
in vivo research	in order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.

Last Update：2024-04-09 21:54:55

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Product Name: GSK2801 Visit Supplier Webpage Request for quotation
CAS: 1619994-68-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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1-(7-(2-Methylsulfonyl-phenyl)-4-propoxy-1-aza-bicyclo[4.3.0]nona-2,4,6,8-tetraen-9-yl)-ethanone Request for Quotation