GSK547

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GSK547

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	2226735-55-1
规格:	≥98%

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议

产品介绍

理化性质和储存条件

	Name: GSK547 CAS#: 2226735-55-1 Chemical Formula: C20H18F2N6O Exact Mass: 396.151 Molecular Weight: 396.4
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Technical Information	Synonym: GSK-547; GSK'547; GSK547; GSK 547; RIP1i Chemical Name: (S)-6-(4-(5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbonyl)piperidin-1-yl)pyrimidine-4-carbonitrile InChi Key: SJVGFKBLUYAEOK-SFHVURJKSA-N InChi Code: 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 SMILES Code: N#CC1=NC=NC(N2CCC(C(N3N=CC[C@H]3C4=CC(F)=CC(F)=C4)=O)CC2)=C1

实验参考方法

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.

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.