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GNF-5837 [1033769-28-6]

Research Use Only
SYN-1183
SYNkinase
CAS Number1033769-28-6
Product group Chemicals
Estimated Purity>95%
Molecular Weight535.5
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Overview

  • Supplier
    SYNkinase
  • Product Name
    GNF-5837 [1033769-28-6]
  • Delivery Days Customer
    10
  • CAS Number
    1033769-28-6
  • Certification
    Research Use Only
  • Estimated Purity
    >95%
  • Molecular Formula
    C28H21F4N5O2
  • Molecular Weight
    535.5
  • Scientific Description
    Chemical. CAS: 1033769-28-6. Formula: C28H21F4N5O2. MW: 535.5. Inhibitor of pan-Trk activity (IC(50) = 8 and 12nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC(50) = 11, 9 and 7nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC(50) = 42 and 17nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC(50) = 1 and 0.5microM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC(50) = 3.0 and 5.6microM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50mg/kg, p.o.). - Inhibitor of pan-Trk activity (IC(50) = 8 and 12nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC(50) = 11, 9 and 7nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC(50) = 42 and 17nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC(50) = 1 and 0.5microM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC(50) = 3.0 and 5.6microM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50mg/kg, p.o.).
  • Storage Instruction
    2°C to 8°C
  • UNSPSC
    51202000