GNF-5837

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GNF-5837 是一种特异性、口服生物可利用的 TrkA/TrkB 泛 TRK 抑制剂（IC50：8/12 nM）。

GNF-5837 is a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF. The properties of GNF-5837 make it a good tool for the elucidation of TRK biology in cancer and other nononcology indications.

Cell Viability Assay Cell Line:GOT1 cells Concentration:0.1 nM , 0.5 nM , 1 nM , 5 nM , 10 nM , 50 nM , 100 nM and 500 nM Incubation Time:72 hours, 96 hours and 144 hours Result:Cell viability assay determined a clear decrease of GOT1 cell viabilityin a time- and dose- dependent manner.Western Blot AnalysisCell Line:GOT1 cells Concentration:5 nM, 50 nM and 500 nM Incubation Time:24 hours Result:Significant levels of TrkA expression, faint TrkC expression and no TrkB expression.Cell Cycle Analysis Cell Line:GOT1 cells Concentration:5 nM, 500 nM Incubation Time:72 hours Result:Induced G1 cell cycle arrest.Apoptosis Analysis Cell Line:GOT1 cells Concentration:500 nM Incubation Time:144 hours Result:Induced apoptosis.

Animal Model:Mouse xenograft model Dosage:25 mg/kg, 50 mg/kg, 100 mg/kg Administration:Oral administration; once daily; for 10 days Result:72 and 100% tumor regression was observed at 50 and 100 mg/kg, respectively. At 25 mg/kg, only partial tumor growth inhibition was achieved.

GNF5837 | GNF-5837 | GNF 5837

Others

Other Targets

Kit| PDGFRβ| TrkA| TrkB| TrkC

Cancer

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1033769-28-6

535.49

C28H21F4N5O2

>98% (HPLC)

DMSO : ≥ 32 mg/mL; 59.76 mM

Cc1c(cc(cc1)NC(=O)Nc1c(ccc(c1)C(F)(F)F)F)Nc1cc2c(cc1)/C(=C/c1ccc[nH]1)/C(=O)N2

(Z)-1-(3-((3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea

(-20℃)

With Ice Pack

≥ 2 years