AV-412 ≥95%

Supplier: ADIPOGEN CORP MS

Synonyms: MP-412, AV-412 free base, N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide

SYN-1012-M001 SYN-1012-M005 SYN-1012-M010
102991-338EA 283.85 USD
102991-338 102991-340 102991-342
AV-412 ≥95%
AV-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 enzyme assays assay the compound inhibited the EGFR variants and ErbB2 in the nanomolar range with over 100-fold selectivity compared with other kinases, apart from ABL and FLT1, which were both moderately sensitive to the compound. In cells, AV-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 100nM. Moreover, AV-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. In animal studies using cancer xenograft models, AV-412 (30mg/kg) demonstrated complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively.

Formula: C₂₇H₂₈ClFN₆O
MW: 507 g/mol
Storage Temperature: Freezer
MDL Number: MFCD16038939
CAS Number: 451492-95-8

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Specification Test Results

Purity 95%
Appearance/Color Solid.
Solubility Soluble in DMSO or ethanol.

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