Afatinib

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
Afatinib free base, BIBW 2992, Tomtovok™
API & Intermediates
KAPI1F06
439081-18-2
MFCD12407405
10184653

image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
Afatinib
C24H25ClFN5O3
485.94
≥99.5%(HPLC)
White to Off-white Solid
281-282°C
500mg,1g,10g,25g,50g,100g and 500g
-20°C Freezer
Afatinib (also known as BIBW2992) is an irreversible kinase inhibitor and binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) to inhibit tyrosine kinase autophosphorylation. It showed positive results in assays against a variety of human cancer cell lines, including A431, murine NIH-3T3 cells, and breast cancer cell line BT-474.
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. [1]
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. [2]
Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks. [3]
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. [4]
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR). [5]
Combinational therapy of crizotinib and afatinib for malignant pleural mesothelioma. [6]
References:
[1] D.Li, et al, Oncogene., 2008, 27(34), pp 4702-4711.
[2] K.L.Stevens, et al, Bioorg. Med. Chem. Lett., 2009. 19(1), pp 21-26.
[3] T.Barf. et al, J. Med. Chem., 2012, 55(14), pp 6243-6262.
[4] Y.Pan, et al, Mol. Cancer Ther., 2012, 11(4), pp 952-962.
[5] R.A.Ward, et al, J. Med. Chem., 2013, 56(17), pp 7025-7048.
[6] L.Huang, et al, Am. J. Cancer Res., 2017, 7(2), pp 203-217.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Warning
H302,H315,H319,H332,H335
P264,P302+P352,P304+P340,P305+P351+P338

NONH for all modes of transport
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2. Safety Data Sheet
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