ChemicalBook > CAS DataBase List > GSK547
GSK547
- Product Name
- GSK547
- CAS No.
- 2226735-55-1
- Chemical Name
- GSK547
- Synonyms
- RIP1I;GSK547;CPD3508;GSK547 (RIP1i;RIP1 inhibitor 547;RIP1 inhibitor GSK547;GSK547, 10 mM in DMSO;Inhibitor,RIP kinase,inhibit,GSK-547,GSK547,Receptor-interacting protein kinases,RIPK,GSK 547;(S)-6-(4-(5-(3,5-Difluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbonyl)piperidin-1-yl)pyrimidine-4-carbonitrile;4-Pyrimidinecarbonitrile, 6-[4-[[(5S)-5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl]carbonyl]-1-piperidinyl]-
- CBNumber
- CB54806610
- Molecular Formula
- C20H18F2N6O
- Formula Weight
- 396.39
- MOL File
- 2226735-55-1.mol
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GSK547 Property
- 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)
- pka
- 1.93±0.28(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1S/C20H18F2N6O/c21-15-7-14(8-16(22)9-15)18-1-4-26-28(18)20(29)13-2-5-27(6-3-13)19-10-17(11-23)24-12-25-19/h4,7-10,12-13,18H,1-3,5-6H2/t18-/m0/s1
- InChIKey
- SJVGFKBLUYAEOK-SFHVURJKSA-N
- SMILES
- C1=NC(N2CCC(C(N3[C@H](C4=CC(F)=CC(F)=C4)CC=N3)=O)CC2)=CC(C#N)=N1
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Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
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N-Bromosuccinimide Price
Biorbyt Ltd
- Product number
- orb573228
- Product name
- GSK547
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1802
- Updated
- 2021/12/16
Biorbyt Ltd
- Product number
- orb573228
- Product name
- GSK547
- Purity
- >98%
- Packaging
- 250mg
- Price
- $3580.2
- Updated
- 2021/12/16
Biorbyt Ltd
- Product number
- orb573228
- Product name
- GSK547
- Purity
- >98%
- Packaging
- 1g
- Price
- $5803.8
- Updated
- 2021/12/16
DC Chemicals
- Product number
- DC12513
- Product name
- RIP1inhibitorGSK547
- Purity
- >98%
- Packaging
- 1g
- Price
- $2300
- Updated
- 2021/12/16
DC Chemicals
- Product number
- DC12513
- Product name
- RIP1inhibitorGSK547
- Purity
- >98%
- Packaging
- 100mg
- Price
- $600
- Updated
- 2021/12/16
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GSK547 Chemical Properties,Usage,Production
Uses
GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].
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.
target
| Target | Value |
| RIP1 () |