GSK547


Catalog No. Size PriceQuantity
M20059-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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.

Product information

CAS Number: 2226735-55-1

Molecular Weight: 396.39

Formula: C20H18F2N6O

Chemical Name: 6-{4-[(5S)-5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbonyl]piperidin-1-yl}pyrimidine-4-carbonitrile

Smiles: N#CC1C=C(N=CN=1)N1CCC(CC1)C(=O)N1N=CC[C@H]1C1C=C(F)C=C(F)C=1

InChiKey: SJVGFKBLUYAEOK-SFHVURJKSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 125 mg/mL (315.35 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

Products are for research use only. Not for human use.

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