A pan-Trk inhibitor
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GNF-5837

Item No. 14883

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[2,3-dihydro-2-oxo-3-(1H-pyrrol-2-ylmethylene)-1H-indol-6-yl]amino]-4-methylphenyl]-N'-[2-fluoro-5-(trifluoromethyl)phenyl]-urea
CAS Number
1033769-28-6
Molecular Formula
C28H21F4N5O2
Formula Weight
535.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 3 mg/mlEthanol: 1 mg/ml
λmax
257, 366, 450 nm
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 Code
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-
InChi Key
YYDUWLSETXNJJT-MTJSOVHGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    GNF-5837 is a potent, bioavailable pan-Trk inhibitor that blocks the proliferation of cells expressing Tel-TrkA, Tel-TrkB, and Tel-TrkC (IC50s = 7, 9, and 11 nM, respectively).1 It less effectively inhibits c-Kit and PDGFRβ (IC50s = 0.91 and 0.87 µM, respectively), while requiring micromolar concentrations to inhibit an array of other receptor and non-receptor tyrosine kinases. GNF-5837 inhibits the growth of Ba/F3 and rat intestinal epithelial (RIE) cells expressing both TrkA and nerve growth factor (NGF) with IC50 values of 42 and 17 nM, respectively, but does not have anti-proliferative activity of parental cells at concentrations up to 10 µM.1 GNF-5837 displays good bioavailability in mice and rats when given intravenously but not orally.1 It induces regression of tumor xenografts derived from RIE cells expressing both TrkA and NGF.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Albaugh, P., Fan, Y., Mi, Y., et al. Discovery of GNF-5837, a selective TRK inhibitor with efficacy in rodent cancer tumor models. ACS Med. Chem. Lett. 3(2), 140-145 (2012).