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CAS No.: 1033769-28-6

GNF-5837 Catalog No. CSN15870

Synonyms: GNF-5837

GNF-5837 is a potent pan-Trk inhibitor which display 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).

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400-920-2911

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技术信息

生物活性

描述The tropomyosin receptor kinase (TRK) family includes three members of highly homologous receptor tyrosine kinases, TRKA, TRKB, and TRKC that specifically bind to neurotrophins. The binding of neutrophins to the extracellular domains of TRKs causes the kinases to autophosphorylate at several intracellular tyrosine sites and trigger downstream signals involving RAS/ERK, PI3K/AKT, and PLC-γ1 transduction pathways. GNF-5837 is a selective inhibitor of TRKs with IC₅₀s of 8nM and 12nM for TRKA and TRKB, respectively^[3]. In proliferation assays utilizing TRK dependent Ba/F3 cells, the inhibitory IC₅₀s of GNF-5837 against cells containing the fusion proteins Tel-TRKA, Tel-TRKB and Tel-TRKC were 11nM, 9nM and 7nM, respectivelyv. In GOT1 cell lines, 2h treatment of GNF-5837 at the concentration of 10nM blocked TRKA activation upon NGF stimulation. The IC₅₀ of GNF-5837 on GOT1 cell proliferation after 144h of incubation was ～660nM. At the concentrations of 5nM, 50nM and 500nM, 24h treatment of GNF-5837 caused downregulation of PI3K-Akt-mTOR signaling and Ras-Raf-MEK-ERK signaling^[4]. In xenografts of RIE cells expressing both TRKA and NGF, GNF-5837 was orally administrated daily for 10 days. 72% and 100% tumor regression was observed at the doses of 50mg/kg and 100mg/kg, respectively, while at 25 mg/kg, only partial tumor growth inhibition was achieved^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
BA/F3 cells	-	Proliferation assay	-	Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKC, IC50=7 nM	24900443
Mo7e cells	-	Function assay	-	Inhibition of c-Kit in human Mo7e cells, IC50=1 μM	24900443

参考文献

[1] Shargh VH, Hondermarck H, et al. Albumin hybrid nanoparticles loaded with tyrosine kinase A inhibitor GNF-5837 for targeted inhibition of breast cancer cell growth and invasion. Int J Pharm. 2016 Dec 30;515(1-2):527-534.
[2] Albaugh P, Fan Y, et al. Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. ACS Med Chem Lett. 2012 Jan 1;3(2):140-5.
[3] Albaugh P, Fan Y, Mi Y, Sun F, Adrian F, Li N, Jia Y, Sarkisova Y, Kreusch A, Hood T, Lu M, Liu G, Huang S, Liu Z, Loren J, Tuntland T, Karanewsky DS, Seidel HM, Molteni V. Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. ACS Med Chem Lett. 2012 Jan 1;3(2):140-5.
[4] Aristizabal Prada ET, Heinzle V, Knösel T, Nölting S, Spöttl G, Maurer J, Spitzweg C, Angele M, Schmidt N, Beuschlein F, Stalla GK, Blaser R, Kuhn KA, Auernhammer CJ. Tropomyosin receptor kinase: a novel target in screened neuroendocrine tumors. Endocr Relat Cancer. 2018 May;25(5):547-560.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8674 mL
- 9.3372 mL
- 18.6744 mL
- 5 mM
- 0.3735 mL
- 1.8674 mL
- 3.7349 mL
- 10 mM
- 0.1867 mL
- 0.9337 mL
- 1.8674 mL

技术信息

CAS号

1033769-28-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H21F4N5O2

运输

蓝冰

分子量

535.49

别名

GNF-5837

溶解度

DMSO	370.0 mg/mL (691.0 mM)
Water	insoluble

动物实验配方

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