Afatinibdimaleate , 10mMinDMSO , 850140-73-7

CAS NO.：850140-73-7

Empirical Formula: C28H29ClFN5O7

Molecular Weight: 602.02

MDL number: MFCD28969755

EINECS: 810-416-1

PRODUCT Properties

• Melting point: >237oC (dec.)
• storage temp.: Refrigerator
• solubility: DMSO (Slightly), Methanol (Slightly)
• form: Solid
• color: White to Pale Yellow
• InChIKey: LIENDGDDWJRJLO-LBXKZPGENA-N
• SMILES: C(/C(=O)O)=C/C(=O)O.N(C1C=CC(F)=C(Cl)C=1)C1=NC=NC2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC1=2 |&1:25,r|

Description and Uses

Afatinib dimaleate was approved by the U.S. Food and Drug Administration (FDA) in 2013 for the treatment of non-small cell lung cancer (NSCLC). Specifically, it was approved for patients presenting with metastatic NSCLC tumors which contain epidermal growth factor receptor (EGFR) exon deletions or exon 21 mutations. Afatinib dimaleate is a covalent inhibitor of ErbB tyrosine kinases (tyk), which downregulates ErbB signaling by irreversible binding of EGFR tyk binding sites. While no manufacturing route has been disclosed to date, the most scalable published route likely derives from two Boehringer Ingelheim patents.

Afatinib Dimaleate is a salt of Afatinib {BIBW 2992), an aminocrotonylamino-substituted quinazoline derivative used for treating cancer and diseases of the respiratory tract, lungs, gastrointestinal tract, bile duct, and gallbladder. An anilino-quinazoline that irreversibly inhibits EGFR and HER2 kinase activity.

Safety

• Symbol(GHS): GHS07,GHS08
• Signal word: Warning
• Hazard statements: H362-H319-H302-H372-H361
• Precautionary statements: P201-P260-P263-P264-P270-P308+P313-P264-P280-P305+P351+P338-P337+P313P-P264-P270-P301+P312-P330-P501-P260-P264-P270-P314-P501-P201-P202-P281-P308+P313-P405-P501
• HS Code: 29339900