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PD168393, a first generation quinazolin amine irreversible EGFR inhibi…

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PD168393, a first generation quinazolin amine irreversible EGFR inhibitors

 

 

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PD168393 is a first generation quinazolin amine irreversible EGFR inhibitors that alkylates Cys-773 within the

ATP binding pocket [1]. While this compound did not progress into clinical application due to limited effect on

EGFR mutant T790M, numerous EGFR research used this as a reference compound to explore new

combinatory treatment strategies, evaluate application of EGFR inhibitors in new in vitro and in vivo cancer

model systems, and compare mechanisms of action for new generations of EGFR inhibitors [2,3].

 

 

Details

Chemical Formula:

 

C17H13BrN4O

CAS No.:

 

194423-15-9

Molecular Weight:

 

369.22

Purity:

 

> 98%

Appearance:

 

Orange

Chemical Name:

 

N-(4-((3-bromophenyl)amino)quinazolin-6-yl)acrylamide

Solubility:

 

Up to 200 mM in DMSO

Synonyms:

 

PD168393

Storage:

 

For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.

 

References

1.

Fry DW, et al. Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci 1998; 95(20):12022-7. Pubmed ID: 9751783

2.

Sos ML, et al. Chemogenomic Profiling Provides Insights into the Limited Activity of Irreversible EGFR Inhibitors in Tumor Cells Expressing the T790M EGFR Resistance Mutation. Cancer Res 2010; 70(3): 868–74. Pubmed ID:20103621

3.

Ghosh AK, et al. Covalent Inhibition in Drug Discovery. Chem Med Chem 2019; 14(9): 889–906. Pubmed ID: 30816012

 

 

Ordering information

   

Catalog No.

Product Name

Size

C1683

PD168393

2mg, 10mg & 50mg

     

 

▣ 관련 페이지 ; Cellagen Technology

 

   

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