| Identification | Back Directory | [Name]
GZD824 | [CAS]
1421783-64-3 | [Synonyms]
CS-1086
HQP1351
GZD824.2CH3SO3H
GZD824DIMESYLATE
GZD824 GZD824DIMESYLATE
Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-, methanesulfonate
4-Methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamide methanesulfonate (1:2)
Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-, methanesulfonate (1:2)
4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-, methanesulfonate (1:2) -Benzamide GZD824 Dimesylate
GZD824 GZD824DIMESYLATE Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-, meth | [Molecular Formula]
C29H27F3N6O.2CH4O3S | [MDL Number]
MFCD26142656 | [MOL File]
1421783-64-3.mol | [Molecular Weight]
724.771 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, away from moisture and light | [solubility ]
≥36.25 mg/mL in DMSO; ≥33.95 mg/mL in H2O with ultrasonic; ≥4.71 mg/mL in EtOH with ultrasonic | [form ]
solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I). It is a COVID19-related research product. | [Biological Activity]
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]. | [References]
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. |
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| Company Name: |
D&C Chemicals
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| Tel: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0.htm |
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