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Cat. No. Name Size Price Add Cart
KI3415AV-412QuoteQuote

Chemical Characteristic

Product NameAV-412
SynonymsMP-412, OSU-HDAC42
CAS No.451493-31-5
Molecular Weight 851.41
FormulaC41H44ClFN6O7S2
Chemical NameN-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide;4-methylbenzenesulfonic acid
SmilesC(=O)(C=C)Nc1cc2c(ncnc2cc1C#CC(C)(N1CCN(CC1)C)C)Nc1cc(c(cc1)F)Cl
Chemical Structure

Biological activities

AV-412 is a potent dual inhibitor of epidermal growth factor receptor (EGFR) and ErbB2 tyrosine kinases, including the mutant EGFRL858R,T790M. AV-412 inhibits all variants of EGFR kinase with IC50s ranging from 0.5 to 2 nM. AV-412 also inhibits ErbB2, Abl, Flt-1 and src with IC50s of 19 nM, 41 nM, 920 nM and 2 µM, respectively. In H1650 and H1975 cells, AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC50s of 43 and 282 nM, respectively. AV-412 inhibits EGF-dependent A431 cell proliferation with an IC50 of 100 nM. Moreover, AV-412 abrogates EGFR signaling in the gefitinib resistant H1975 cell line.[1] AV-412 inhibits the growth of H1781, H1975, and H1650 cells, with IC50s of 0.3, 0.5 and 1.4 µM, respectively.[2] In BALB/c nu/nu (athymic) mice studies using cancer xenograft models, AV-412 (30 mg/kg) exhibits complete inhibition of tumor growth of the A431 and BT-474 cell lines.[1] In mice, AV-412 completely inhibits the tumor growth of both H1650 and H1975 xenografts. AV-412 inhibits EGFR signaling in tumors in BALB/c AJcl nude mice.[1]

Protocols

In vitro, AV-412 is dissolved in DMSO.[1]

References

[1] Suzuki T, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007, 98(12): 1977-1984.
[2] Suzuki T, et al. Antitumor activity of a dual epidermal growth factor receptor and ErbB2 kinase inhibitor MP-412 (AV-412) in mouse xenograft models. Cancer Sci. 2009, 100(8): 1526-1531.

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