AV-412

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP01955CAS No. ：451492-95-8Purity：98%

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CAS No.	451492-95-8	Cat. No.	BCP01955
Name	AV-412
Synonyms	AV412;AV 412;MP-412;MP 412;MP412;
SMILES
Chemical Name
Formula	C27H28ClFN6O	M. Wt	507
Purity	98%	Storage	Store at 4-8°C
Description	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 of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100 nM. Moreover, MP-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR [1]. MP-412 inhibited phosphorylation of EGFR and its downstream signaling in NCI-H1650 and NCI-H1975 cell lines, which harbor the E746-A750 deletion and L858R + T790M point mutations, respectively, in