871026-18-5
Chemical Structure
SYR127063
- CAS No.: 871026-18-5
- Formula:C23H20ClF3N4O3
- Molecular Weight:492.88
IUPAC Name: 2-(2-(4-((3-chloro-4-(3-(trifluoromethyl)phenoxy)phenyl)amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethoxy)ethan-1-ol
InChIKey: CMMUJJHJYMYOJR-UHFFFAOYSA-N
SMILES: FC(F)(F)C=1C=CC=C(OC2=CC=C(C=C2Cl)NC3=NC=NC=4C=CN(C43)CCOCCO)C1
Biological Activity: SYR127063 is a potent and selective human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor with an IC50 of 11 nM. SYR127063 binds to the active site of the HER2 kinase domain in an ATP-competitive manner, thereby preventing the formation of the conserved salt bridge required for kinase activation. SYR127063 can be used in research related to breast cancer, ovarian cancer and gastric cancer[1][2].
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SYR127063 | SYR127063 is a potent and selective human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor with an IC50 of 11 nM. SYR127063 binds to the active site of the HER2 kinase domain in an ATP-competitive manner, thereby preventing the formation of the conserved salt bridge required for kinase activation. SYR127063 can be used in research related to breast cancer, ovarian cancer and gastric cancer. | |||||||||||||||||||||
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- [1]. Aertgeerts K, et al. Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein. The Journal of biological chemistry. 2011 May 27;286(21):18756-65.
- [2]. Hakaman, H., et al. In-Silico molecular docking analysis of monoclonal antibodies, approved inhibitors, and plant-based inhibitors targeting extracellular and intracellular HER2 receptor. Berkala Penelitian Hayati, 31(1), 33–48.
Keywords
