| Identification | Back Directory | [Name]
KU004 | [CAS]
1260401-93-1 | [Synonyms]
KU004
4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[3-(tetrahydro-4-methyl-4-oxido-1,4-azaphosphorin-1(2H)-yl)-1-propyn-1-yl]- | [Molecular Formula]
C29H27ClFN4O2P | [MOL File]
1260401-93-1.mol | [Molecular Weight]
548.98 |
| Chemical Properties | Back Directory | [Boiling point ]
742.947±60.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.376±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [pka]
5.465±0.20(predicted) |
| Hazard Information | Back Directory | [Uses]
KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative[1][2]. | [References]
[1] Tian C, et al. A novel dual EGFR/HER2 inhibitor KU004 induces cell cycle arrest and apoptosis in HER2-overexpressing cancer cells. Apoptosis. 2015 Dec;20(12):1599-612. DOI:10.1007/s10495-015-1164-7
[2] Tian C, et al. Inhibition of glycolysis by a novel EGFR/HER2 inhibitor KU004 suppresses the growth of HER2+ cancer. Exp Cell Res. 2017 Aug 15;357(2):211-221. DOI:10.1016/j.yexcr.2017.05.019 |
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