A Bcr/Abl inhibitor
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GZD-824

Item No. 21508

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-benzamide
CAS Number
1257628-77-5
Synonyms
  • HQP1351
  • Olverembatinib
Molecular Formula
C29H27F3N6O
Formula Weight
532.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
274, 324 nm
SMILES
CN1CCN(CC2=CC=C(NC(C3=CC(C#CC4=CN=C(NN=C5)C5=C4)=C(C)C=C3)=O)C=C2C(F)(F)F)CC1
InChi Code
InChI=1S/C29H27F3N6O/c1-19-3-5-22(14-21(19)6-4-20-13-24-17-34-36-27(24)33-16-20)28(39)35-25-8-7-23(26(15-25)29(30,31)32)18-38-11-9-37(2)10-12-38/h3,5,7-8,13-17H,9-12,18H2,1-2H3,(H,35,39)(H,33,34,36)
InChi Key
TZKBVRDEOITLRB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).1 It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ren, X., Pan, X., Zhang, Z., et al. Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J. Med. Chem. 56(3), 879-894 (2013).