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GZD824 Bcr-Abl inhibitor,novel orally bioavailable

Catalog No.B1402
Size Price Stock Qty
10mM (in 1mL DMSO)
$170.00
In stock
5mg
$115.00
In stock
25mg
$360.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

GZD824

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Chemical Properties

Cas No. 1421783-64-3 SDF Download SDF
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 dimethanesulfonate
Canonical SMILES CC1=CC=C(C(NC2=CC=C(CN3CCN(C)CC3)C(C(F)(F)F)=C2)=O)C=C1C#CC4=CN=C5C(C=NN5)=C4.CS(=O)(O)=O.CS(=O)(O)=O
Formula C29H27F3N6O.2CH4O3S M.Wt 724.77
Solubility >36.3mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

GZD824 is an orally bioavailable inhibitor of Bcr-Abl with IC50 values of 0.34 and 0.68 nM for Bcr-AblWT and Bcr-AblT315I, respectively [1].

Bcr-Abl is a fused protein that interacts with the interleukin-3 receptorβ(c) subunit and has tyrosine kinase activity. Abl activates cell cycle-related proteins and enzymes and increases cell division. Bcr-Abl inhibits DNA repair and causes genomic instability.

GZD824 is an orally bioavailable Bcr-Abl inhibitor. GZD824 exhibited high affinity with Kd values of 0.32 and 0.71 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GZD824 inhibited Bcr-Abl with IC50 values of 0.34, 0.68, 0.27, 0.71, 0.15, 0.35, 0.29 and 0.35 nM for Bcr-AblWT, Bcr-AblT315I, Bcr-AblE255K, Bcr-AblG250E, Bcr-AblQ252H, Bcr-AblH396P, Bcr-AblM351T and Bcr-AblY253F, respectively. In a competitive binding assay, GZD824 bound to the ATP-binding sites of native Abl with Kd values of 0.32 and 0.34 nM for non-phosphorylated and phosphorylated Abl. In stably transformed Ba/F3 cells, GZD824 potently inhibited cells growth with IC50 values of 1.0 and 7.1 nM for Bcr-AblWT and Bcr-AblT315I expressed cells, respectively [1].

In mouse xenograft tumor models, GZD824 inhibited tumor growth. In mice bearing an allograft leukemia model, GZD824 significantly increased survival [1].

Reference:
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, 2013, 56(3): 879-894.