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GNF-5837 is a Potent pan-Trk inhibitor. It Displays 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) and Exhibits selectivity for Trk receptors over a range of kinases, with some activity at PDGFR and c-Kit (IC50 values are 0.87 and 0.91 μM respectively). It's Orally bioavailable.GNF-5837 suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50 mg/kg, p.o.).
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Source | J Neurosci (2016). Figure 9. GNF-5837 |
| Method | RT-PCR | |
| Cell Lines | C57BL/6J mice | |
| Concentrations | 500 ng | |
| Incubation Time | - | |
| Results | As a positive control, we demonstrated that pretreatment with GNF-5837 inhibited NGF-induced thermal hyperalgesia |
| Molecular Weight | 535.49 |
| Formula | C28H21F4N5O2 |
| CAS Number | 1033769-28-6 |
| Solubility (25°C) | DMSO 50 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Trk Products |
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| GW441756
GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. |
| ANA-12
ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively. |
| 7,8-Dihydroxyflavone
7,8-Dihydroxyflavone acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF). |
| Larotrectinib (LOXO-101)
Larotrectinib (LOXO-101) is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. |
| LOXO-101 sulfate
LOXO-101 sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
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