AV-412

AV-412

CAT N°: 29039
Price:

From 182.00 154.70

AV-412 is a dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively).{46529} It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 ?M) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 ?M) induces ubiquitination and degradation of HER2 in SK-BR-3 cells.{46530} It decreases levels of HER2 and estrogen receptor ? (ER?) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 ?M. AV-412 inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 ?M).{46529} It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-2-propenamide, 4-methylbenzenesulfonate (1:2)
  • Correlated keywords
    • 451492-95-8 1022984-77-5 AV412 MP412 L858R T790M L858RT790M HER-2 MEK-1 FLT SKBR3 BR3 SKBR ER Hsp-70 MCF7 A-431 BT474
  • Product Overview:
    AV-412 is a dual inhibitor of EGFR and HER2 (IC50s = 1.4, 0.51, 0.79, 2.3, and 19 nM for the EGFR, EGFRL858R, EGFRT790M, EGFRL858R,T790M, and HER2 recombinant intracellular kinase domains, respectively).{46529} It is selective for EGFR and HER2 over IRK, MEK1, PKA, and PKC (IC50s = >10 ?M) but also inhibits Abl, FLT1, and Src (IC50s = 41, 920, and 2,000 nM, respectively). AV-412 (10 and 30 ?M) induces ubiquitination and degradation of HER2 in SK-BR-3 cells.{46530} It decreases levels of HER2 and estrogen receptor ? (ER?) and increases levels of Hsp70 in MCF-7 cells when used at a concentration of 10 ?M. AV-412 inhibits EGF-stimulated growth of A431 cells (IC50 = 0.1 ?M).{46529} It reduces tumor growth in an A431 mouse xenograft model when administered at doses of 10 and 30 mg/kg and in a BT-474 mouse xenograft model at 30 mg/kg.

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