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GSK547

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GSK547

GSK547

Catalog No.: PC0101

Size: 5 mg,10 mg, 25 mg,50 mg, 100 mg, 200 mg, 500 mg

Description

GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1) that inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.

Molecular Weight 396.39
Formula C20H18F2N6O
CAS No. 2226735-55-1
Appearance Solid
Color White to off-white
SMILES N#CC1=NC=NC(N2CCC(C(N3N=CC[C@H]3C4=CC(F)=CC(F)=C4)=O)CC2)=C1
Shipping Room temperature in continental US; may vary elsewhere.
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
In Vitro GSK547 (0.1-100000 nM; 24 hours) pretreats L929 cells with recombinant TNFα and zVAD at various doses for 30 min, then cell death is induced with an IC50 of 32 nM after 24 hours.
GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM).
In Vivo GSK547 (GSK′547; RIP1i) robustly targets RIP1 in vivo. RIP1 inhibition results in immunogenic macrophage differentiation in pancreatic cancer, leading to adaptive immune activation and tumor protection for pancreatic ductal adenocarcinoma (PDA).
GSK547 (100 mg/kg/day; fed via food-based dosing; 15-50 days) reduces tumor burden and extends survival compared with mice treated with controls or Nec-1s.
All of our services are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.

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