Neratinib

CAS No. 698387-09-6

Neratinib( HKI-272 | HKI272 | HKI 272 )

Catalog No. M15679 CAS No. 698387-09-6

A potent, highly selective, irreversible HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 27 In Stock
10MG 39 In Stock
25MG 58 In Stock
50MG 77 In Stock
100MG 113 In Stock
200MG 177 In Stock
500MG 295 In Stock
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Biological Information

  • Product Name
    Neratinib
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, highly selective, irreversible HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays.
  • Description
    A potent, highly selective, irreversible HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src (IC50=0.8 and 1.4 uM), no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met; inhibits downstream signal transduction events and cell cycle regulatory pathways, leads to arrest at the G(1)-S phase transition, decreases cell proliferation; active in HER-2- and EGFR-dependent tumor xenograft models, orally bioavailable.Breast Cancer Approved.
  • In Vitro
    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
    Animal Model:Female athymic (nude) mice, tumor xenograftDosage: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
    HKI-272 | HKI272 | HKI 272
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR|HER2|PDK1|Src|VEGFR2?(KDR)
  • Research Area
    Cancer
  • Indication
    Breast Cancer

Chemical Information

  • CAS Number
    698387-09-6
  • Formula Weight
    557.0427
  • Molecular Formula
    C30H29ClN6O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 6.4 mg/mL (Need ultrasonic)
  • SMILES
    CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)/C=C/CN(C)C
  • Chemical Name
    2-Butenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)-

Shipping & Storage Information

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

Reference

1. Rabindran SK, et al. Cancer Res. 2004 Jun 1;64(11):3958-65. 2. Tsou HR, et al. J Med Chem. 2005 Feb 24;48(4):1107-31. 3. Ji H, et al. Proc Natl Acad Sci U S A. 2006 May 16;103(20):7817-22.
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