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194423-06-8,MFCD02179194
Catalog No.:AA00ABGR

194423-06-8 | CL-387785

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1mg
≥95%
in stock  
$53.00   $37.00
- +
5mg
≥95%
in stock  
$166.00   $116.00
- +
25mg
>98.0%(GC)
in stock  
$190.00   $133.00
- +
100mg
95%
in stock  
$658.00   $461.00
- +
250mg
95%
in stock  
$835.00   $584.00
- +
1g
95%
in stock  
$1,636.00   $1,145.00
- +
  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00ABGR
Chemical Name:
CL-387785
CAS Number:
194423-06-8
Molecular Formula:
C18H13BrN4O
Molecular Weight:
381.2260
MDL Number:
MFCD02179194
SMILES:
CC#CC(=O)Nc1ccc2c(c1)c(ncn2)Nc1cccc(c1)Br
Properties
Computed Properties
 
Complexity:
514  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
24  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
3  
XLogP3:
4.3  

Literature

Title: EGFR participates downstream of ERα in estradiol-17β-D-glucuronide-induced impairment of Abcc2 function in isolated rat hepatocyte couplets.

Journal: Archives of toxicology 20160401

Title: Inhibition of the mTOR/S6K signal is necessary to enhance fluorouracil-induced apoptosis in gastric cancer cells with HER2 amplification.

Journal: International journal of oncology 20120801

Title: Irreversible protein kinase inhibitors: balancing the benefits and risks.

Journal: Journal of medicinal chemistry 20120726

Title: 3'-deoxy-3'-18F-fluorothymidine PET/CT to guide therapy with epidermal growth factor receptor antagonists and Bcl-xL inhibitors in non-small cell lung cancer.

Journal: Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20120301

Title: Clinical and molecular evidences of epithelial to mesenchymal transition in acquired resistance to EGFR-TKIs.

Journal: Lung cancer (Amsterdam, Netherlands) 20110801

Title: Epidermal growth factor treatment switches δ-opioid receptor-stimulated extracellular signal-regulated kinases 1 and 2 signaling from an epidermal growth factor to an insulin-like growth factor-1 receptor-dependent mechanism.

Journal: Molecular pharmacology 20110201

Title: Resistance to an irreversible epidermal growth factor receptor (EGFR) inhibitor in EGFR-mutant lung cancer reveals novel treatment strategies.

Journal: Cancer research 20071101

Title: Transcriptional profiling identifies cyclin D1 as a critical downstream effector of mutant epidermal growth factor receptor signaling.

Journal: Cancer research 20061201

Title: Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer.

Journal: The Journal of clinical investigation 20061002

Title: Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.

Journal: Journal of medicinal chemistry 20060223

Title: Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants.

Journal: PLoS medicine 20051101

Title: An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor.

Journal: Cancer research 20050815

Title: EGFR pharmacogenomics: the story continues to mutate and evolve.

Journal: American journal of pharmacogenomics : genomics-related research in drug development and clinical practice 20050101

Title: High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter.

Journal: Molecular pharmacology 20040601

Title: 6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.

Journal: Journal of medicinal chemistry 20010816

Title: Discafani CM, et al. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N--[(3-bromophenyl)amino-6-quinazolinyl-2-butynamide (CL-387,785). Biochem Pharmacol. 1999 Apr 15;57(8):917-25.

Title: Sweeney WE, et al. Treatment of polycystic kidney disease with a novel tyrosine kinase inhibitor. Kidney Int. 2000 Jan;57(1):33-40.

Title: Greulich H, et al. Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. PLoS Med. 2005 Nov;2(11):e313.

Title: Kobayashi S, et al. An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res. 2005 Aug 15;65(16):7096-101.

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