Product   Name

Afatinib  diMaleate (BIBW2992 DiMaleate)

General   deion

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

Synonym

(Z)-but-2-enedioic acid; (E)-N-[4-(3-chloro-4-fluoroanilino)-7-[(3S)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide.  

Purity

≥99% (HPLC)

CAS   Number

850140-73-7

Formula

C²⁴H²⁵ClFN⁵O³·2(C⁴H⁴O⁴)

Molecular   Weight

717.18

Suitability

BioReagent, suitable for cell culture, etc.

l    Physical and Chemical Information

Appearance

White or Off-white to yellow solid

Solubility(25℃)

DMSO

≥50mg/mL

Ethanol

Very slightly soluble

Water

Very slightly soluble

l  Biological Information

Biochem/Physiol   Actions

Afatinib Dimaleate is the dimaleate salt form of afatinib, 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 cancer cell types.

l  Packaging & Storage

Packaging

25mg; 100mg; 500mg

Storage   temp.

0-5℃

l  Precautions and Disclaimer

This   product is for R&D use only, not for drug, household, or other uses.

l  References

1.    https://ncit.nci.nih.gov

2.    https://pubchem.ncbi.nlm.nih.gov