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GNF 5837

CAS No.
1033769-28-6
Chemical Name:
GNF 5837
Synonyms
CS-997;GNF 5837;GNF-5837, >97%;GNF-5837, >=98%;GNF5837; GNF 5837;GNF 5837 USP/EP/BP;Trk Inhibitor III, GNF-5837;Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem;(Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-;1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea
CBNumber:
CB62667487
Molecular Formula:
C28H21F4N5O2
Molecular Weight:
535.49
MDL Number:
MFCD24386809
MOL File:
1033769-28-6.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59

GNF 5837 Properties

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

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H335-H319
Precautionary statements  P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  36/37/39
WGK Germany  3
NFPA 704
0
2 0

GNF 5837 price More Price(41)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML0844 GNF 5837 ≥98% (HPLC) 1033769-28-6 5mg $150 2024-03-01 Buy
Sigma-Aldrich 648451 Trk Inhibitor III, GNF-5837 1033769-28-6 10mg $332 2024-03-01 Buy
Cayman Chemical 14883 GNF 5837 ≥95% 1033769-28-6 1mg $57 2024-03-01 Buy
Cayman Chemical 14883 GNF 5837 ≥95% 1033769-28-6 5mg $97 2024-03-01 Buy
Sigma-Aldrich SML0844 GNF 5837 ≥98% (HPLC) 1033769-28-6 25mg $239.2 2024-03-01 Buy
Product number Packaging Price Buy
SML0844 5mg $150 Buy
648451 10mg $332 Buy
14883 1mg $57 Buy
14883 5mg $97 Buy
SML0844 25mg $239.2 Buy

GNF 5837 Chemical Properties,Uses,Production

Uses

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]

IC 50

a potent and selective pan-trk inhibitor, suppressing the activity of trka and trkb with ic50 of 8 and 12 nm, respectively.

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.

364-73-8
1033769-28-6
Synthesis of GNF 5837 from 4-Bromo-1-fluoro-2-nitrobenzene
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View Lastest Price from GNF 5837 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
GNF 5837 pictures 2019-07-06 GNF 5837
1033769-28-6
US $2.00 / kg 1kg 99% 100kg Career Henan Chemical Co
  • GNF 5837 pictures
  • GNF 5837
    1033769-28-6
  • US $2.00 / kg
  • 99%
  • Career Henan Chemical Co

GNF 5837 Spectrum

Trk Inhibitor III, GNF-5837 GNF 5837 (Z)-1-(3-(3-((1H-PYRROL-2-YL)METHYLENE)-2-OXOINDOLIN-6-YLAMINO)-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 GNF 5837 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 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 GNF5837 GNF-5837, >=98% 1-[2-Fluoro-5-(trifluoromethyl)phenyl]-3-(4-methyl-3-{[(3Z)-2-oxo-3-(1H-pyrrol-2-ylmethylene)-2,3-dihydro-1H-indol-6-yl]amino}phenyl)urea (Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro- GNF 5837 USP/EP/BP Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem CS-997 GNF-5837, >97% GNF5837; GNF 5837 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]- 1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea 1033769-28-6 C28H21F4N5O2 Inhibitors