Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

HomeProduct name listGNF 5837

GNF 5837

Synonym(s):(Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea;N-[3-[[2,3-Dihydro-2-oxo-3-(1H-pyrrol-2-ylmethylene)-1H-indol-6-yl]amino]-4-methylphenyl]-N′-[2-fluoro-5-(trifluoromethyl)phenyl]-urea;Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem

GNF 5837 Structural

What is GNF 5837?

The Uses of GNF 5837

GNF 5837 is a potent pan-Trk inhibitor which has selectivity for tropomyosin-receptor-kinase (Trk).

Biological Activity

gnf-5837 is reported to selectively suppress pan-trk potently in an oral-bioavailable manner. neurotrophins and their receptors (trks) are important in malignant transformations, chemotaxis, metastasis, and survival signaling and may contribute to the pathogenesis of a variety of tumors. the trk-inhibiting properties of gnf-5837 therefore make it a useful tool to investigate trk biology in cancer and other non-oncology indications. [1]

Biochem/physiol Actions

GNF-5837 is an orally bioavailable Trk inhibitor (IC50 = 8 and 12 nM for TrkA and TrkB, respectively). GNF-5837 inhibits growth of Ba/F3 cells expressing Tel-Trl fusions. IC50 values for growth inhibition are Tel-TrkA = 11 nM, Tel-TrkB = 9 nM and Tel-TrkC = 7 nM.

in vitro

the anti-trka activity of gnf-5837 was detected in ba/f3 and rie cells expressing both trka and ngf. in ba/f3 cells, this compound exhibited intensively anti-proliferation activity with an ic50 of 0.042 μm. rie cells expressing trka and ngf could only survive under low attachment condition and were resistant to detachment-induced apoptosis. gnf-5837 seemed to suppress cell growth and proliferation of rie cells intensively with an ic50 of 0.017 μm. moreover, gnf-5837 is reported to show inhibitory effects on c-kit and pdgfr in mo7e cells and rat-a10 cells, respectively. [1]

in vivo

mice models with tumor xenografts derived from rie cells expressing both trka and ngf were established in one study. gnf-5837 was then administered at ascending doses once daily to these mice for 10 days, with the aim to investigate the in vivo efficacy of gnf-5837. 72 and 100% tumor inhibition was reported at the dose of 50 and 100 mg/kg, respectively. at 25 mg/kg, only partial tumor growth inhibition was observed. [1]

storage

Store at +4°C

References

[1] albaugh f, fan y, mi y, sun fx, adrian f, li nx, jia y, sarkisova y, kreusch a, hood t, lu m, liu gx, huang sl, liu zs, loren j, tuntland t, karanewsky ds, seidel hm and molteni v. discovery of gnf-5837, a selective trk inhibitor with efficacy in rodent cancer tumor models. acs med. chem. lett. 2012. 3: 1405.

Properties of GNF 5837

Melting point: >228°C (dec.)
Boiling point: 616.0±55.0 °C(Predicted)
Density  1.497±0.06 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMSO: soluble5mg/mL, clear (warmed)
pka 12.16±0.20(Predicted)
form  powder
color  yellow to orange

Safety information for GNF 5837

Computed Descriptors for GNF 5837

Related products of tetrahydrofuran

You may like

  • GNF-5837 >95% CAS 1033769-28-6
    GNF-5837 >95% CAS 1033769-28-6
    1033769-28-6
    View Details
  • Gnf 5837 95% CAS 1033769-28-6
    Gnf 5837 95% CAS 1033769-28-6
    1033769-28-6
    View Details
  • Trk Inhibitor III, GNF-5837 CAS 1033769-28-6
    Trk Inhibitor III, GNF-5837 CAS 1033769-28-6
    1033769-28-6
    View Details
  • 1823368-42-8 98%
    1823368-42-8 98%
    1823368-42-8
    View Details
  • 2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    1307449-08-6
    View Details
  • Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    25408-95-1
    View Details
  • 2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    1805639-70-6
    View Details
  • Lithium Clavulanate
    Lithium Clavulanate
    61177-44-4
    View Details
Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.