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796888-12-5

796888-12-5 structure
796888-12-5 structure
  • Name: LCH-7749944
  • Chemical Name: N-[2-(3-methoxyanilino)-4-quinazolinyl]-N-(tetrahydro-2-furanylmethyl)amine
  • CAS Number: 796888-12-5
  • Molecular Formula: C20H22N4O2
  • Molecular Weight: 350.414
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2018-07-11 14:13:41
  • Modify Date: 2024-01-12 08:46:23
  • LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis[1].

Name N-[2-(3-methoxyanilino)-4-quinazolinyl]-N-(tetrahydro-2-furanylmethyl)amine
Synonyms N2-(3-Methoxyphenyl)-N4-(tetrahydro-2-furanylmethyl)-2,4-quinazolinediamine
2,4-Quinazolinediamine, N2-(3-methoxyphenyl)-N4-[(tetrahydro-2-furanyl)methyl]-
N-[2-(3-methoxyanilino)-4-quinazolinyl]-N-(tetrahydro-2-furanylmethyl)amine
Description LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis[1].
Related Catalog
Target

PAK4:14.93 μM (IC50)

In Vitro LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner[1]. LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells[1]. LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase[1]. LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner[1]. Cell Proliferation Assay[1] Cell Line: MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells Concentration: 5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM Incubation Time: 24 hours Result: Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner. Apoptosis Analysis[1] Cell Line: SGC7901 cells Concentration: 5, 10, 20 μM Incubation Time: 12, 24, 48 hours Result: Induced apoptosis of SGC7901 cells. Cell Cycle Analysis[1] Cell Line: SGC7901 cells Concentration: 5, 10, 20 μM Incubation Time: 12, 24, 48 hours Result: Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase. Western Blot Analysis[1] Cell Line: SGC7901 cells Concentration: 5, 10, 20, 30 μM Incubation Time: 24 hours Result: Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.
References

[1]. Zhang J, et al. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells. Cancer Lett. 2012 Apr 1;317(1):24-32.

Density 1.3±0.1 g/cm3
Boiling Point 580.0±58.0 °C at 760 mmHg
Molecular Formula C20H22N4O2
Molecular Weight 350.414
Flash Point 304.6±32.3 °C
Exact Mass 350.174286
LogP 2.18
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.680