AV-412 chemical structure
Chemical structureResearch use only
CAT. NO. DC23948Featured

AV-412

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Product overview

Description & Application

A potent dual inhibitor of EGFR and ErbB2; inhibits EGFR/EGFR L858R/EGFR T790M/EGFR L858R, T790M/ErbB2 with IC50 of 1.5/0.5/0.8/2.3/19 nM respectively; also inhibits Abl (IC50=41 nM), weakly inhibits Flt3 and Src; inhibits autophosphorylation of EGFR and ErbB2 with IC50 of 43 and 282 nM; inhibits EGF-dependent cell proliferation with IC50 of 100 nM; active in cancer xenograft models.Solid TumorsPhase 1 Discontinued

ParameterValue
Chemical NameAV-412
CAS No.451493-31-5
Synonyms2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl);MP-412;AV 412;N-[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;MP412;N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butynyl]-6-quinazolinyl]-2-propenamide bis(4-methylbenzenesulfonate);MP 412;AV-412 Tosylate;AV-412;GLXC-10834;bis(4-methylbenzene-1-sulfonic acid); N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)prop-2-enamide;451493-31-5;HY-10346;MP412 cpd;2-Propenamide, N-(4-((3-chloro-4-fluorophenyl)amino]-7-(3-methyl-3-(4-methyl-1-piperazinyl)-1-butynyl]-6-quinazolinyl]-, bis(4-methylbenzenesulfonate);bis(4-methylbenzene-1-sulfonic acid); N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl]quinazolin-6-yl}prop-2-enamide;MP-412 Tosylate;N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide bis(4-methylbenzenesulfonate);451493-31-5 (tosylate);2-PROPENAMIDE, N-(4-((3-CHLORO-4-FLUOROPHENYL)AMINO)-7-(3-METHYL-3-(4-METHYL-1-PIPERAZINYL)-1-BUTYN-1-YL)-6-QUINAZOLINYL)-, 4-METHYLBENZENESULFONATE (1:2);2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-methylbenzenesulfonate (1:2);EGFR/HER2 Inhibitor AV-412;BCP23783;AC-36815;UNII-Z541VW0W40;2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-, 4-methyl benzenesulfonate (1:2);N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl)-6-quinazolinyl)acrylamide;AV-412;MP-412;MP 412 [WHO-DD];av-412 free base; bis(para-toluene sulfonate);2-Propenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-,4-Methylbenzenesulfonate(1:2);N-[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;MS-31574;AKOS027338673;Z541VW0W40;SCHEMBL4760106;AV412 cpd;EX-A756;MP-412 DITOSYLATE;AV-412 bis-tisylate;BTA49331;Q27295006;MP-412; MP 412; MP412; AV-412; AV 412; AV412;DB06021
FormulaC27H28N6OFCl.2[C7H8O3S]
M.Wt851.405460000001
SMILESO=S(C1=CC=C(C)C=C1)(O)=O.C=CC(NC2=CC3=C(NC4=CC=C(F)C(Cl)=C4)N=CN=C3C=C2C#CC(N5CCN(C)CC5)(C)C)=O.O=S(C6=CC=C(C)C=C6)(O)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

A potent dual inhibitor of EGFR and ErbB2; inhibits EGFR/EGFR L858R/EGFR T790M/EGFR L858R, T790M/ErbB2 with IC50 of 1.5/0.5/0.8/2.3/19 nM respectively; also inhibits Abl (IC50=41 nM), weakly inhibits Flt3 and Src; inhibits autophosphorylation of EGFR and ErbB2 with IC50 of 43 and 282 nM; inhibits EGF-dependent cell proliferation with IC50 of 100 nM; active in cancer xenograft models.Solid TumorsPhase 1 Discontinued

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

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