Availability
0
Your Basket is Empty
BA164141

Afatinib - Bio-X

Irreversible blocker of three members of the ErbB family (ErbB1, ErbB2/HER2, and ErbB4) with IC50 in nanomolar range. The compound binds covalently to cysteine 797 residue in HER2 and blocks downstream cellular signalling, inhibits cellular growth and promotes apoptosis. Afatinib has been used for the treatment of tyrosine kinase inhibitor-resistant tumours with mutations in ErbB genes, especially for deletions in exon 19 and single nucleotide substitutions in exon 21. It has been used for treatment of non-small cell lung cancer (NSCLC), breast cancer, pancreatic cancer, colorectal cancer, etc.

Technical Data

CAS No: 850140-72-6
Synonyms: (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide; BIBW 2992
Product Code: BA164141
MDL No: MFCD12407405
Chemical Formula: C24H25ClFN5O3
Molecular Weight: 485.94

References


  • Li D et al (2008). BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 27(34):4702-11.
  • Hirsh V (2011). Afatinib (BIBW 2992) development in non-small-cell lung cancer. Future Oncol. 7(7):817-25.
  • Pan Y et al (2012). SKLB1206, a novel orally available multikinase inhibitor targeting EGFR activating and T790M mutants, ErbB2, ErbB4, and VEGFR2, displays potent antitumor activity both in vitro and in vivo. Mol Cancer Ther 11(4):952-62.
  • Solca et al., 2012. Target binding properties and cellular activity of afatinib (BBW 2992), an irreversible ErbB family blocker. J Pharmacol Exp Ther 343:342–350.
  • Modjtahedi et al., 2014. A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer. Naunyn Schmiedebergs Arch Pharmacol 387(6):505-21.

Solubility

Stability

Further Information


Datasheets

Specification: View
MSDS: View

Afatinib - Bio-X

CAS No:
850140-72-6
Synonyms:
(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
BIBW 2992
MDL No:
MFCD12407405
Chemical Formula:
Molecular Weight:
485.94
Product Structure
References:
1. Li D et al (2008). BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 27(34):4702-11.
2. Hirsh V (2011). Afatinib (BIBW 2992) development in non-small-cell lung cancer. Future Oncol. 7(7):817-25.
3. Pan Y et al (2012). SKLB1206, a novel orally available multikinase inhibitor targeting EGFR activating and T790M mutants, ErbB2, ErbB4, and VEGFR2, displays potent antitumor activity both in vitro and in vivo. Mol Cancer Ther 11(4):952-62.
4. Solca et al., 2012. Target binding properties and cellular activity of afatinib (BBW 2992), an irreversible ErbB family blocker. J Pharmacol Exp Ther 343:342–350.
5. Modjtahedi et al., 2014. A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer. Naunyn Schmiedebergs Arch Pharmacol 387(6):505-21.
Click for Specification
Click for MSDS

For requirements greater than the catalogue prepacks email: enquiries@carbosynth.com

Custom Synthesis

For custom synthesis or special requests email: enquiries@carbosynth.com, call +44 (0)1635 578444 or fill out our contact form

Please Wait...