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GNF-5837

Cat. No. M2585
GNF-5837 Structure
Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 125 In stock
50mg USD 355 In stock
100mg USD 580 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 535.49
Formula C28H21F4N5O2
CAS Number 1033769-28-6
Purity >99%
Solubility DMSO
Storage at -20°C
References

Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.
Albaugh, P. et al. ACS Med Chem Lett. 2012 Jan 1;3(2):140-5. PMID: 24900443.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GNF-5837 supplier, Trk, inhibitors

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