GSK3145095

CAS No. 1622849-43-7

GSK3145095( —— )

Catalog No. M22000 CAS No. 1622849-43-7

GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 133 In Stock
5MG 259 In Stock
10MG 441 In Stock
25MG 705 In Stock
50MG 981 In Stock
100MG 1332 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    GSK3145095
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic.
  • Description
    GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic. GSK3145095 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking RIP1 kinase-dependent cellular responses.?Highlighting its potential as a novel cancer therapy, the inhibitor was also able to promote a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures.?(In Vitro):GSK3145095 potently blocks the TNF response as shown by determination of overall cell viability as measured by cellular ATP levels (IC50 = 1.6 nM), cell death as measured by LDH release (IC50 = 0.5 nM) and RIP1-dependent inflammatory cytokine MIP-1β production, either as absolute levels for protein, or fold changes in mRNA expression (IC50 = 0.4 nM) .
  • In Vitro
    GSK3145095 potently blocks the TNF response as shown by determination of overall cell viability as measured by cellular ATP levels (IC50 = 1.6 nM), cell death as measured by LDH release (IC50 = 0.5 nM) and RIP1-dependent inflammatory cytokine MIP-1β production, either as absolute levels for protein, or fold changes in mRNA expression (IC50 = 0.4 nM) .
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    TNF
  • Recptor
    RIP1
  • Research Area
    Endocrine system;Cancer
  • Indication
    Neoplasms, Pancreatic

Chemical Information

  • CAS Number
    1622849-43-7
  • Formula Weight
    397.38
  • Molecular Formula
    C20H17F2N5O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:245mg/ml (616.54 Mm; Need ultrasonic)
  • SMILES
    FC1=CC2=C(NC(=O)[C@H](CC2)NC(=O)C2=NNC(CC3=CC=CC=C3)=N2)C(F)=C1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Harris PA, ET AL. Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer. ACS Med Chem Lett. 2019 May 9;10(6):857-862.
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