AdipoGen Life Sciences

Afatinib

Product Code:
 
SYN-1100
Product Group:
 
Inhibitors and Activators
Regulatory Status:
 
RUO
Shipping:
 
-20°C
1 / 1
Chemical Structure
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Chemical Structure

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SYN-1100-M100100 mgEnquire
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Further Information

Alternate Names/Synonyms:
Tovok; BIBW-2992
Appearance:
Solid.
CAS:
439081-18-2
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
InChiKey:
ULXXDDBFHOBEHA-CWDCEQMOSA-N
Long Description:
Chemical. CAS: 439081-18-2. Formula: C24H25ClFN5O3. MW: 486. Afatinib is an irreversible kinase inhibitor and binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) to inhibit tyrosine kinase autophosphorylation. This results in a downregulation of ErbB signaling and subsequent inhibition of proliferation of cell lines expressing wild-type EGFR, selected EGFR exon 19 deletion mutations, or exon 21 L858R mutations. It also inhibited in vitro proliferation of cell lines overexpressing HER2. Overall, tumor growth was inhibited by Afatinib very effectively with low nanomolar IC(50) values ranging from approximately 6nM to below 500nM.
Molecular Formula:
C24H25ClFN5O3
Molecular Weight:
486
Package Type:
Plastic Vial
Product Description:
Afatinib is an irreversible kinase inhibitor and binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) to inhibit tyrosine kinase autophosphorylation. This results in a downregulation of ErbB signaling and subsequent inhibition of proliferation of cell lines expressing wild-type EGFR, selected EGFR exon 19 deletion mutations, or exon 21 L858R mutations. It also inhibited in vitro proliferation of cell lines overexpressing HER2. Overall, tumor growth was inhibited by Afatinib very effectively with low nanomolar IC(50) values ranging from approximately 6nM to below 500nM.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO or ethanol.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.

References

Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors: K.L. Stevens, et al.; Bioorg. Med. Chem. Lett. 19, 21 (2009) | Irreversible protein kinase inhibitors: balancing the benefits and risks: T. Barf & A. Kaptein; J. Med. Chem. 55, 6243 (2012) | Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR): R.A. Ward, et al.; J. Med. Chem. 56, 7025 (2013)