ChemicalBook > CAS DataBase List > HKI 357
HKI 357
- Product Name
- HKI 357
- CAS No.
- 848133-17-5
- Chemical Name
- HKI 357
- Synonyms
- HKI 357;Inhibitor,HKI-357,ErbB-1,HER1,inhibit,NSCLCs,Epidermal growth factor receptor,HKI 357,EGFR,ERBB2,HKI357;(E)-N-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide;(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)-
- CBNumber
- CB63037308
- Molecular Formula
- C31H29ClFN5O3
- Formula Weight
- 574.05
- MOL File
- 848133-17-5.mol
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HKI 357 Property
- 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
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N-Bromosuccinimide Price
Cayman Chemical
- Product number
- 14847
- Product name
- HKI 357
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
Cayman Chemical
- Product number
- 14847
- Product name
- HKI 357
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $239
- Updated
- 2024/03/01
Cayman Chemical
- Product number
- 14847
- Product name
- HKI 357
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $323
- Updated
- 2024/03/01
Tocris
- Product number
- 3580
- Product name
- HKI357
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $956
- Updated
- 2021/12/16
Tocris
- Product number
- 3580
- Product name
- HKI357
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $227
- Updated
- 2021/12/16
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HKI 357 Chemical Properties,Usage,Production
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
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. td> |
target
EGFR 34 nM (IC 50 ) | ErbB2 33 nM (IC 50 ) |
HKI 357 Preparation Products And Raw materials
Raw materials
Preparation Products
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HKI 357 Suppliers
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