1. Apoptosis
  2. RIP kinase

GSK547 

目录号: HY-114492
产品使用指南

GSK547是一种高效的选择性RIP1抑制剂,可抑制巨噬细胞介导的胰腺癌适应性免疫耐受.

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GSK547 Chemical Structure

GSK547 Chemical Structure

CAS No. : 2226735-55-1

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Description

GSK547, a highly selective and potent RIP1 inhibitor, inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].

IC50 & Target

RIP1[1]

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[1].
GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM)[1].

Cell Viability Assay[1]

Cell Line: L929 cells (Mouse L-cells NCTC 929)
Concentration: 0.1 nM; 10 nM; 1000 nM; 100000 nM
Incubation Time: 24 hours
Result: Reduced viability of L929 cells after co-treatment with TNFα and zVAD with an IC50 of 32 nM.

Western Blot Analysis[1]

Cell Line: Bone marrow-derived macrophages (BMDM)
Concentration:
Incubation Time: 30 minutes
Result: Up-regulated STAT1 signaling in 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)[1].
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[1].

Animal Model: The wild-type (WT) mice orthotopically implanted with Pdx1Cre;KrasG12D;Trp53R172H (KPC)-derived tumor cells[1]
Dosage: ~100 mg/kg
Administration: Fed via food-based dosing, daily, 15-50 days
Result: Reduced tumor burden and extended survival.
References
Molecular Weight

396.39

Formula

C₂₀H₁₈F₂N₆O

CAS No.

2226735-55-1

SMILES

N#CC1=NC=NC(N2CCC(C(N3N=CC[C@H]3C4=CC(F)=CC(F)=C4)=O)CC2)=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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产品名称:
GSK547
目录号:
HY-114492
需求量:

GSK547

Cat. No.: HY-114492