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 |
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10MG | 87 | In Stock |
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25MG | 200 | In Stock |
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50MG | 320 | In Stock |
|
100MG | 507 | In Stock |
|
200MG | Get Quote | In Stock |
|
500MG | Get Quote | In Stock |
|
1G | Get Quote | In Stock |
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Biological Information
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Product NameGZD 824
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NoteResearch use only, not for human use.
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Brief DescriptionGZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).
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DescriptionGZD824 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.
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SynonymsGZD824; GZD 824; GZD-824
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PathwayEndocrinology/Hormones
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TargetAChR
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RecptorAbl (E254K)
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1257628-77-5
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Formula Weight532.57
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Molecular FormulaC29H27F3N6O
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Purity98%
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SolubilityDMSO : ≥ 100 mg/mL; 187.77 mM
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SMILESCN1CCN(Cc2c(cc(NC(=O)c3cc(C#Cc4cc5c([nH]nc5)nc4)c(C)cc3)cc2)C(F)(F)F)CC1
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Chemical Name3-((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
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Ren X, et al. J Med Chem. 2013, 56(3), 879-894.
molnova catalog
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