AV-412_451493-31-5_DataSheet_MedChemExpress

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Product Name:
AV-412CAS No.:
451493-31-5Cat. No.:
HY-10346MWt:
851.41Formula:
C41H44ClFN6O7S2Purity :>98%
Solubility:Mechanisms:Biological Activity:
Pathways:JAK/STAT Signaling; Target:EGFR
Pathways:Protein Tyrosine Kinase/RTK; Target:EGFR Product Data Sheet
DMSO
References:
Caution: Not fully tested. For research purposes only
Medchemexpress LLC
[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 Dec;98(12):1977-84.[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 Aug;100(8):1526-31.[3]. Suzuki T, et al. Ubiquitination and downregulation of ErbB2 and estrogen receptor-alpha by
kinase inhibitor MP-412 in human breast cancer cells. J Cell Biochem. 2011 Sep;112(9):2279-86.AV-412(MP-412, 2 tosylate salt) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits
autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.
IC50 value: 0.51 nM (EGFR L858R); 0.79 nM (EGFRT790M); 19 nM (ErbB2) [1]
Target: EGFR; ErbB2; Mutant EGFR L858R/T790M in vitro: MP-412 (AV-412) is a potent dual inhibitor of EGFR and ErbB2 tyrosine kinases, including the mutant EGFR(L858R,T790M), which is clinically resistant to the EGFR-specific kinase inhibitors erlotinib and gefitinib. In an enzyme assay, MP-412 inhibited the EGFR variants and ErbB2 in the nanomolar range with over 100-fold selectivity compared with other kinases, apart from abl and flt-1, which were both moderately sensitive to the compound. In cells, MP-412 inhibited
autophosphorylation...
18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S A
E m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。