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Home / Biochemicals / Small Molecules

GNF 5837

SKU : BHB21300152

A Potent pan-Trk (Neurotrophin Receptor) Inhibitor

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Mfr.No.	G-145, G-145_10 mg, G-145_100 mg, G-145_25 mg, G-145_5 mg, G-145_50 mg
Description	GNF 5837 (#G-145) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C28H21F4N5O2.
Background	Three tropomyosin-related kinase (TrkA, TrkB, and TrkC) receptors bind the following neurotrophic factors with varied affinities: nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), neurotrophin-3 (NT-3), and neurotrophin-4 (NT-4); BDNF and NT-4 activate TrkB, while NGF and NT-3 activate TrkA and TrkC; NT-3 also activates the other two TRKs, albeit more weakly. After ligand binding, TRKs form dimers, and the subsequent kinase activation results in transphosphorylation of tyrosine residues which in turn enable the binding of cytoplasmic proteins that exhibit phosphotyrosine-binding (PTB) or Src-homology-2 (SH2) domains, such as phospholipase C (PLC-gamma1), p85 and Shc1-3.GNF-5837 is a novel oxindole urea inhibitor of TRKs. With exceptional binding affinity to TrkA, TrkB, and TrkC (IC50 = 0.011, 0.009, and 0.007 uM/L, respectively), GNF-5837 is a pan-TRK inhibitor that has enhanced selectivity for TRKs, and demonstrates efficiency in mammalian models of tumor. Many carcinomas - not necessarily nerve tissue-related - involve TRK signaling by NTs; GNF-5837 can therefore have useful application in cancer research in addition to other of its many other uses in many biological research branches4,5.
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	1 nM - 10 uM.
Reconstitution	40 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
Cas Number	1033769-28-6
Molecular Weight	535.49
Solubility	40 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
Target	TrkA, TrkB, TrkC receptors
Source	Synthetic
Activity	GNF 5837 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)1.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: (Z)-1-(3-(3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-6-ylamino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea.

Purity	>95%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: Up to four weeks at 4°C or three months at -20°C.

Product Manual	SDS

Reference	Reichardt, L.F. (2006) Philos. Trans. R. Soc. Lond. B. Biol. Sci. 361, 1545. Rich, R.L. and Myszka, D.G. (2010) J. Mol. Recognit. 23, 1. Berry, A. et al. (2012) Neural. Plast. 2012, 784040. Albaugh, P. et al. (2012) ACS Med. Chem. Lett. 3, 140. Hondermarck, H. (2012) Cytokine Growth Factor Rev. 23, 357. Albaugh, P. et al. (2012) ACS Med. Chem. Lett. 3, 140.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300152-1	G-145_10 mg	10 mg	$184		Add to Cart
BHB21300152-2	G-145_100 mg	100 mg	$1445		Add to Cart
BHB21300152-3	G-145_25 mg	25 mg	$425		Add to Cart
BHB21300152-4	G-145_5 mg	5 mg	$117		Add to Cart
BHB21300152-5	G-145_50 mg	50 mg	$798		Add to Cart

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