GSK547

CAS NO.：2226735-55-1
Empirical Formula: C20H18F2N6O
Molecular Weight: 396.39
MDL number: MFCD32062767
Update Date: 2024-11-19 23:02:33

What is GSK547?

Biological Activity

GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) with a 400-fold increase in oral exposure compared to GSK'963 in mouse pharmacokinetic studies.

in vitro

In vitro, treatment with GSK'547 directed bone marrow-derived macrophages to develop an immunogenic phenotype, with up-regulation of MHC-II, TNFa and IFNg expression, and decreased CD206, IL- 10 and TGFb expression. In addition, it also up-regulated STAT1 signaling and decreased STAT3, STAT5 and STAT6 signaling in bone marrow-derived macrophages. Macrophages treated with GSK'547 had stronger ability to capture antigens.

in vivo

Mice were given GSK'547 through food, the concentration of GSK'547 in vivo was stable within 24 hours, which was higher than the IC50 value in L929 cells. GSK'547 maintained high concentrations in vivo during the 6-week administration. GSK'547 was well tolerated with no obvious pathological features. In mice with in situ pancreatic ductal adenocarcinoma, It reduced tumor burden and prolonged survival compared to control and Nec-1s-treated groups. GSK'547 prevents established tumors and liver metastases.

Properties of GSK547

Boiling point:	578.3±60.0 °C(Predicted)
Density	1.43±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:65.0(Max Conc. mg/mL);163.98(Max Conc. mM)
form	Solid
pka	1.93±0.28(Predicted)
color	White to off-white

Safety information for GSK547

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.