Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 43.00 | |
10 mg | In stock | $ 77.00 | |
25 mg | In stock | $ 126.00 | |
50 mg | In stock | $ 198.00 | |
100 mg | In stock | $ 328.00 | |
200 mg | In stock | $ 426.00 | |
500 mg | In stock | $ 692.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 51.00 |
Description | GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM). |
Targets&IC50 | TrkA:8 nM, TrkB:12 nM |
In vitro | In Ba/F3 cells overexpressing the constitutively active Tel-TRKC fusion, GNF-5837 shows potent anti-Trk activity and potent antiproliferation activity with IC50 of 0.042 μM. [1] |
In vivo | In both male Balb/c mice and Sprague–Dawley rats, GNF-5837 has the low drug clearance, and moderate biovailability. In mice bearing Rie xenografts expressing TrkA and NGF, GNF-5837 (100 mg/kg/d p.o.) significantly inhibits tumor growth. [1] |
Kinase Assay | Inhibition of biochemical TrkA,TrkB and TrkC: TrkA and TrkC biochemical assays are carried out by HTRF method.The reaction mixtures contains 1 μM peptide substrate,1 μM ATP,and either 1.8 nM TrkA or 34 nM TrkC in the reaction buffer (50 mM HEPES pH 7.1,10 mM MgCl2,2 mM MnCl2,0.01% BSA,2.5 mM DTT and 0.1 mM Na3VO4) at a final volume of 10 μL.All reactions are carried out at room temperature in white ProxiPlate? 384-well Plus plates and are quenched with 5 μL of 0.2 mM EDTA at 60 min.Five μL of the detection reagents (2.5 ng PT66K and 0.05 μg SAXL per well) are added,the plates are incubated at room temperature for 1 h and then read in EnVision reader.Compounds are diluted into assay mixture (final DMSO 0.5%),and IC50 values are determined by 12-point (from 50 to 0.000282 μΜ) inhibition curves in duplicate under the assay conditions.TrkB biochemical assay is carried out by caliper microfluidic method.The reaction mixtures contained 1 μM peptide substrate,10 μM ATP,and 2 nM TrkB in a reaction buffer containing 100 mM HEPES,pH 7.5,5 mM MgCl2,0.01% Triton X-100,0.1% BSA,1 mM DTT,10 μΜNa3VO4,and 10 μΜBeta-Glycerophosphate.The reactions are carried out at room temperature for 3 hrs,and the products are determined by Caliper EZ-reader.Compounds are diluted into assay mixture (final DMSO 1%),and IC50 values are determined by 12-point (from 50 to 0.000282 μΜ) inhibition curves in duplicate under the assay conditions. |
Cell Research | Compounds are tested for their ability to inhibit the proliferation of wt Ba/F3 cells and Ba/F3 cells transformed with constitutively expressed luciferase reporter and BCR-ABL or Tel-KDR or other Tel fusion kinases. Parental Ba/F3 cells are maintained in media containing recombinant mouse IL3 and the kinase transformed Ba/F3 cells are maintained in media without IL-3. 7.5 nL of compounds are spotted to each well of 1536-well assay plates by Liquid handling System Echo 555 (Labcyte). 700 cells are then plated into each well of the assay plates in 7 μL culture media per well and compounds are tested at 0.17 nM to 10 uM in 3-fold serial dilutions. The cells were then incubated for 48 hours at 37 °C. 3 μL of Bright-Glo® is added to each well and the plates are read using ViewLux. (Only for Reference) |
Synonyms | GNF 5837 |
Molecular Weight | 535.49 |
Formula | C28H21F4N5O2 |
CAS No. | 1033769-28-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 5.4 mg/mL (10 mM)
DMSO: 53.6 mg/mL (100 mM)
You can also refer to dose conversion for different animals. More
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GNF-5837 1033769-28-6 Angiogenesis Tyrosine Kinase/Adaptors Trk receptor PDGFR c-Kit Tropomyosin related kinase receptor Trk Receptor GNF 5837 inhibit Inhibitor GNF5837 inhibitor