Olmutinib

CAS No. 1802181-20-9

Olmutinib ( BI1482694,HM61713 )

Catalog No. M21951 CAS No. 1802181-20-9

Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase InhibitorOlmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.?

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 27 In Stock
5MG 47 In Stock
10MG 77 In Stock
25MG 120 In Stock
50MG 176 In Stock
100MG 267 In Stock
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Biological Information

  • Product Name
    Olmutinib
  • Note
    Research use only, not for human use.
  • Brief Description
    Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase InhibitorOlmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.?
  • Description
    Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase InhibitorOlmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.?In addition, olmutinib at reversal concentration affected neither the protein expression level nor the localization of ABCG2.?The results observed from the accumulation/efflux study of olmutinib showed that olmutinib reversed ABCG2-mediated MDR with an increasing intracellular drug accumulation due to inhibited drug efflux.?We also had consistent results with the ATPase assay that olmutinib stimulated ATPase activity of ABCG2 up to 3.5-fold.?Additionally, the molecular interaction between olmutinib and ABCG2 was identified by docking simulation.?Olmutinib not only interacts directly with ABCG2 but also works as a competitive inhibitor of the transport protein.
  • Synonyms
    BI1482694,HM61713
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1802181-20-9
  • Formula Weight
    486.6
  • Molecular Formula
    C26H26N6O2S?
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CN1CCN(CC1)c1ccc(cc1)Nc1nc2c(c(n1)Oc1cccc(c1)NC(=O)C=C)scc2
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Zhang W , Fan Y F , Cai C Y , et al. Olmutinib (BI1482694/HM61713), a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, Reverses ABCG2-Mediated Multidrug Resistance in Cancer Cells[J]. Frontiers in Pharmacology, 2018, 9.2. Zhang Z , Fu L , Guo X , et al. Olmutinib (HM61713) reversed multidrug resistance by inhibiting the activity of ATPbinding cassette subfamily G member 2 in vitro and in vivo[J]. 2018,008(004):563-574.
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