Afatinib

CAS No. 439081-18-2

Afatinib ( BIBW2992 )

Catalog No. M14490 CAS No. 439081-18-2

Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Purity : >98%(HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Afatinib
  • Note
    Research use only, not for human use.
  • Brief Description
    Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.
  • Description
    Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity. Upon administration, afatinib selectively and irreversibly binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these RTKs. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many Y cell types.
  • Synonyms
    BIBW2992
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR (L858R); EGFR (L858R/T790M); EGFR (wt); HER2
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    439081-18-2
  • Formula Weight
    485.94
  • Molecular Formula
    C24H25ClFN5O3
  • Purity
    >98%(HPLC)
  • Solubility
    Ethanol: 15 mg/mL (30.86 mM); DMSO: 97 mg/mL (199.61 mM)
  • SMILES
    CN(C)C/C=C/C(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)O[C@H]4CCOC4
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Prim N, et al. Rev Pneumol Clin. 2014 Oct;70(5):279-85.
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