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GNF-5837 CAS: 1033769-28-6

Category: Inhibitors
Product Name: GNF-5837
Cat No: I000201
CAS No: 1033769-28-6
Synonyms: (Z)-1-(3-((3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea
Molecular Formula: C28H21F4N5O2
Molecular Weight: 535.5
SMILES: FC1=CC=C(C(F)(F)F)C=C1NC(NC2=CC(NC3=CC(NC(/C4=C\C5=CC=CN5)=O)=C4C=C3)=C(C)C=C2)=O
InChI: InChI=1S/C28H21F4N5O2/c1-15-4-6-19(35-27(39)37-25-11-16(28(30,31)32)5-9-22(25)29)13-23(15)34-18-7-8-20-21(12-17-3-2-10-33-17)26(38)36-24(20)14-18/h2-14,33-34H,1H3,(H,36,38)(H2,35,37,39)/b21-12-
InChIKey: YYDUWLSETXNJJT-MTJSOVHGSA-N
Solubility: DMSO: ≥ 32 mg/mL
Target: Trk
IC50: 7/9/11 nM (Tel-TrkC/Tel-TrkB/Tel-TrkA) [1]
Storage: Store at +4°C
CAS 1033769-28-6,GNF-5837
  • Description

GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively).
IC50 Value: 7/9/11 nM (Tel-TrkC/Tel-TrkB/Tel-TrkA) [1]
Target: pan-Trk
GNF-5837 is an orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC50 = 8 and 12 nM 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 (IC50 = 11, 9 and 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC50 = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC50 = 1 and 0.5 μM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC50 = 3.0 and 5.6 μM). GNF-5837 displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. GNF-5837 weakly antagonize relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. GNF-5837 suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50 mg/kg, p.o.) [1].

  • Spec

Appearance:Orange to red solid powder
Purity: > 98%

  • References


1:Albumin hybrid nanoparticles loaded with tyrosine kinase A inhibitor GNF-5837 for targeted inhibition of breast cancer cell growth and invasion. Shargh VH, Hondermarck H, Liang M.Int J Pharm. 2016 Dec 30;515(1-2):527-534. doi: 10.1016/j.ijpharm.2016.10.057. Epub 2016 Oct 25. PMID: 27793712
2:Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. Albaugh P, Fan Y, Mi Y, Sun F, Adrian F, Li N, Jia Y, Sarkisova Y, Kreusch A, Hood T, Lu M, Liu G, Huang S, Liu Z, Loren J, Tuntland T, Karanewsky DS, Seidel HM, Molteni V.ACS Med Chem Lett. 2012 Jan 1;3(2):140-5. doi: 10.1021/ml200261d. eCollection 2012 Feb 9. PMID: 24900443 Free PMC Article


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