GZD 824

CAS No. 1257628-77-5

GZD 824 ( GZD824; GZD 824; GZD-824 )

Catalog No. M17912 CAS No. 1257628-77-5

GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).

Purity : 98%

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 36 In Stock
5MG 58 In Stock
10MG 87 In Stock
25MG 200 In Stock
50MG 320 In Stock
100MG 507 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    GZD 824
  • Note
    Research use only, not for human use.
  • Brief Description
    GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).
  • Description
    GZD824 is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I. GZD824 tightly bound to Bcr-Abl(WT) and Bcr-Abl(T315I) with K(d) values of 0.32 and 0.71 nM, respectively, and strongly inhibited the kinase functions with nanomolar IC(50) values. GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. GZD824 also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy. It induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT) or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I). GZD824 represents a promising lead candidate for development of Bcr-Abl inhibitors to overcome acquired imatinib resistance.
  • Synonyms
    GZD824; GZD 824; GZD-824
  • Pathway
    Endocrinology/Hormones
  • Target
    AChR
  • Recptor
    Abl (E254K)
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1257628-77-5
  • Formula Weight
    532.57
  • Molecular Formula
    C29H27F3N6O
  • Purity
    98%
  • Solubility
    DMSO : ≥ 100 mg/mL; 187.77 mM
  • SMILES
    CN1CCN(Cc2c(cc(NC(=O)c3cc(C#Cc4cc5c([nH]nc5)nc4)c(C)cc3)cc2)C(F)(F)F)CC1
  • Chemical Name
    3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide

Shipping & Storage Information

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

Reference

1. Ren X, et al. J Med Chem. 2013, 56(3), 879-894.
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