Rezivertinib

CAS No. 1835667-12-3

Rezivertinib( —— )

Catalog No. M34868 CAS No. 1835667-12-3

Rezivertinib (BPI-7711) is an orally available, selective and potent inhibitor of tyrosine kinase (EGFR) with antitumor activity for central nervous system disorders.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Rezivertinib
  • Note
    Research use only, not for human use.
  • Brief Description
    Rezivertinib (BPI-7711) is an orally available, selective and potent inhibitor of tyrosine kinase (EGFR) with antitumor activity for central nervous system disorders.
  • Description
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
  • In Vitro
    Rezivertinib (BPI-7711) selectively inhibits cellular proliferation of EGFR mutations in cell lines: GI50 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M) and > 1000 nM (A431, EGFR WT).
  • In Vivo
    Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression.Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model. Rezivertinib (50 mg/kg/day; orally) has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days).
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1835667-12-3
  • Formula Weight
    486.57
  • Molecular Formula
    C27H30N6O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 125 mg/mL (256.90 mM; Ultrasonic )
  • SMILES
    O=C(C=C)NC1=CC(NC=2N=CC=C(N2)C3=CN(C=4C=CC=CC34)C)=C(OC)C=C1OCCN(C)C
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Misako Nagasaka, et al. Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2021 May;16(5):740-763.?
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