AV 412

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Cat.No. 4397 - AV 412 | C27H28ClFN6O | CAS No. 451492-95-8
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)
Datasheet
Citations
Reviews
Literature

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 10.14 20
DMSO 50.7 100

Preparing Stock Solutions

The following data is based on the product molecular weight 507. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.97 mL 9.86 mL 19.72 mL
5 mM 0.39 mL 1.97 mL 3.94 mL
10 mM 0.2 mL 0.99 mL 1.97 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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, EGFR, EGFR, Tocris Bioscience

Citations for AV 412

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Literature in this Area

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