AV 412

Cat. No. 4397new

AV 412 C27H28ClFN6O [451492-95-8]

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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

Biological Activity

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

M.Wt:
507
Formula:
C27H28ClFN6O
Solubility:
Soluble to 100 mM in DMSO and to 20 mM in 1eq. HCl
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
451492-95-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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, supplier, AV412, epidermal, growth, factor, receptor, tyrosine, kinases, EGFR, ErbB2, RTKs, inhibitors, inhibits, potent, Abl, Tocris Bioscience, EGFR Inhibitor products

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