Neratinib Maleate

CAS No. 915942-22-2

Neratinib Maleate( —— )

Catalog No. M21827 CAS No. 915942-22-2

Irreversible ErbB receptor tyrosine kinase inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Neratinib Maleate
  • Note
    Research use only, not for human use.
  • Brief Description
    Irreversible ErbB receptor tyrosine kinase inhibitor.
  • Description
    Irreversible ErbB receptor tyrosine kinase inhibitor.(In Vitro):Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met.Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) .Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase.Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27.(In Vivo):Neratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR.
  • In Vitro
    Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met.Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) .Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase.Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27. Cell Proliferation Assay Cell Line:3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 Concentration:0.5 ng/mL–5 μg/mL Incubation Time:2 days (6 days for BT474)Result:Inhibited cell proliferation with IC50 values of 700 ± 78, 3 ± 0.14, 2 ± 0.18, 2 ± 0.06, 81± 9, 960 ± 165 and 690 ± 84 nM against 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 cells, respectively.Western Blot Analysis Cell Line:BT474 or A431 cells Concentration: 0, 2, 10, 50, 100 and 200 nM Incubation Time:3 h Result:Decreased ligand-independent receptor phosphorylation by 50% (IC50) at 5 nM in BT474 cells, repressed EGF-dependent phosphorylation of EGFR in A431 cells at a comparable dose (IC50 = 3 nM). Effectively repressed phosphorylation of MAPK and Akt in BT474 cells.Cell Cycle Analysis Cell Line:BT474 Concentration:0–2 nM Incubation Time:12–16 h Result:Blocked cell cycle progression, causing a G1-S arrest, a 50% decrease in the number of cells in the S (DNA synthesis) phase of the cell cycle was observed at a concentration of 2 nM.
  • In Vivo
    Neratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR. Animal Model:Female athymic (nude) mice, tumor xenograft Dosage:10, 20, 40, 60 or 80 mg/kg/day Administration:Gavage, 42 days Result:Reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3 and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    915942-22-2
  • Formula Weight
    673.11
  • Molecular Formula
    C30H29ClN6O3·C4H4O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (371.41 mM)
  • SMILES
    ——
  • Chemical Name
    (E)-N-[4-[3-Chloro-4-[(2-pyridinyl)methoxy]anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide maleate

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

molnova catalog
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