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Description: Potent inhibitor of EGFR, ErbB2 and Abl receptor tyrosine kinases
Chemical Name: N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-2-propenamide
Purity: ≥98% (HPLC)
Biological Activity for AV 412
AV 412 is a potent inhibitor of EGFR, ErbB2 and Abl receptor tyrosine kinases (IC50 values are 0.5-2, 19 and 41 nM, respectively). Also weak inhibitor of FLT1 and Src. Inhibits EGFR and ErbB2 autophosphorylation in vitro in NSCLC and T-47D breast cancer cell lines, respectively. Inhibits tumor growth of EGFR-overexpressing A431 and ErbB2 overexpressing BT-474 tumor xenografts in mice.
Technical Data for AV 412
| M. Wt | 507 |
| Formula | C27H28ClFN6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 451492-95-8 |
| PubChem ID | 9806229 |
| InChI Key | ZAJXXUDARPGGOC-UHFFFAOYSA-N |
| Smiles | FC(C=C1)=C(Cl)C=C1NC2=NC=NC3=CC(C#CC(C)(C)N4CCN(C)CC4)=C(NC(C=C)=O)C=C32 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for AV 412
References for AV 412
References are publications that support the biological activity of the product.
Suzuki et al (2009) Antitumor activity of a dual epidermal growth factor receptor and ErbB2 kinase inhibitor MP-412 (AV-412) in mouse xenograft models. Cancer Sci. 100 1526 PMID: 19459856
Suzuki et al (2007) Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor. Cancer Sci. 98 1977 PMID: 17888033
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Keywords: AV 412, AV 412 supplier, AV412, epidermal, growth, factor, receptor, tyrosine, kinases, EGFR, ErbB2, RTKs, inhibitors, inhibits, potent, Abl, 4397, Tocris Bioscience
Citations for AV 412
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Currently there are no citations for AV 412.
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