Afatinib dimaleate

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
Afatinib maleate, BIBW 2992MA2, Gilotrif
API & Intermediates
KAPI1F07
850140-73-7
MFCD22581558
15606394

image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
Afatinib dimaleate
C₂₄H₂₅ClFN₅O₃•[C₄H₄O₄]₂
718.09
≥99.9%(HPLC)
White to Off-white Solid
281-282°C
500mg,1g,10g,25g,50g,100g and 500g
-20°C Freezer
Afatinib dimaleate (also known as BIBW2992MA2) is an orally bioavailable dual receptor tyrosine kinase (RTK) inhibitor with potentially irreversible inhibiting EGFR and HER2 kinase activity. It 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.
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. [1]
A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours. [2]
Afatinib enhances the efficacy of conventional chemotherapeutic agents by eradicating cancer stem-like cells. [3]
Clinical Pharmacokinetics and Pharmacodynamics of Afatinib. [4]
References:
[1] D.Li, et al, Oncogene., 2008, 27(34), pp 4702-4711.
[2] F.A.L.M. Eskens, et al, Br. J. Cancer, 2008, 98(1), pp 80-85.
[3] X.K.Wang, et al, Cancer Res., 2014, 74(16), pp 4431-4435.
[4] S.Wind, et al, Clin. Pharmacokinet., 2017, 56(3), pp 235-250.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Warning
H302,H410
P264,P270,P273,P301+P312,P330,P391,P501

NONH for all modes of transport
Sales restrictions may apply.
1. Product Specification
2. Safety Data Sheet
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