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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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Hazard and Precautionary Statements (GHS)

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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

< 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 )

HKI 357 Preparation Products And Raw materials

Raw materials

Preparation Products

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HKI 357 Suppliers

China 21 United Kingdom 1 United States 8 USA 1 Global 31
Tocris Bioscience
Tel
--
Fax
--
Email
customerservice@tocris.co.uk
Country
United Kingdom
ProdList
5726
Advantage
77

848133-17-5, HKI 357Related Search:


  • 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)-
  • 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
  • 848133-17-5
  • C31H29ClFN5O3