GSK547

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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.

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