| Identification | Back Directory | [Name]
HKI 357 | [CAS]
848133-17-5 | [Synonyms]
HKI 357
(2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
2-Butenamide, N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)- | [Molecular Formula]
C31H29ClFN5O3 | [MDL Number]
MFCD26792555 | [MOL File]
848133-17-5.mol | [Molecular Weight]
574.05 |
| Chemical Properties | Back Directory | [Boiling point ]
747.6±60.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble to 100 mM in DMSO and to 25 mM in ethanol | [form ]
Powder | [pka]
12.37±0.43(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Uses]
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation[1]. | [Biological Activity]
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50 of 34 nM and 33 nM, respectively. It can inhibit EGFR autophosphorylation (detected at Y1068), and AKT and MAPK phosphorylation. | [in vitro]
HKI-357 (0.01-10 μM) is effective in suppressing ligand-induced EGFR autophosphorylation and its downstream signaling, as determined by AKT and MAPK phosphorylation in NCI-H1975 cells. HKI-357 is also effective in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation. Western Blot Analysis < tr> | Cell Line: | NCI-H1975 bronchoalveolar cell line | | Concentration: | 0.01, 0.01, 0.1, 1 and 10 μM | | Incubation Time: | | | Result: | Suppressed ligand-induced EGFR autophosphorylation and its downstream signaling AKT and MAPK phosphorylation. | | [target]
| EGFR 34 nM (IC 50 ) | ErbB2 33 nM (IC 50 ) | | [IC 50]
EGFR: 34 nM (IC50); ErbB2: 33 nM (IC50) | [References]
[1] Kwak EL, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7665-70. DOI:10.1073/pnas.0502860102 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|