ChemicalBook > CAS DataBase List > GZD824

GZD824

Product Name
GZD824
CAS No.
1421783-64-3
Chemical Name
GZD824
Synonyms
CS-1086;HQP1351;GZD824.2CH3SO3H;GZD824DIMESYLATE;Olverembatinib dimesylate;Olverembatinib Dimesylate (GZD824);GZD824 GZD824DIMESYLATE;3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide dimethanesulfonate; 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)
CBNumber
CB82677404
Molecular Formula
C31H35F3N6O7S2
Formula Weight
724.7708096
MOL File
1421783-64-3.mol
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GZD824 Property

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
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

TRC
Product number
G932000
Product name
GZD824
Packaging
5mg
Price
$175
Updated
2021/12/16
TRC
Product number
G932000
Product name
GZD824
Packaging
25mg
Price
$605
Updated
2021/12/16
ApexBio Technology
Product number
B1402
Product name
GZD824
Packaging
25mg
Price
$360
Updated
2021/12/16
ChemScene
Product number
CS-0020021
Product name
GZD824(dimesylate)
Purity
99.20%
Packaging
10mg
Price
$180
Updated
2021/12/16
ApexBio Technology
Product number
B1402
Product name
GZD824
Packaging
5mg
Price
$115
Updated
2021/12/16
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GZD824 Chemical Properties,Usage,Production

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.

GZD824 Preparation Products And Raw materials

Raw materials

Preparation Products

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GZD824 Suppliers

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Hunan Huayi Zhide Pharmaceutical Technology Co., Ltd.
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View Lastest Price from GZD824 manufacturers

Career Henan Chemical Co
Product
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 1421783-64-3
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2019-12-23

1421783-64-3, GZD824Related Search:

Bafetinib GW788388 Dabrafenib Veliparib Ponatinib Crizotinib

  • 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
  • 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
  • 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)
  • GZD824DIMESYLATE
  • CS-1086
  • 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
  • GZD824.2CH3SO3H
  • HQP1351
  • Olverembatinib dimesylate
  • Olverembatinib Dimesylate (GZD824)
  • region-Abelson,phosphorylated,imatinib,Olverembatinib dimesylate,inhibit,linase,Inhibitor,nonphosphorylated,breakpoint,resistance,HQP1351 dimesylate,Bcr-Abl,Bcr-Abl(T315I),cluster
  • 3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide dimethanesulfonate
  • 1421783-64-3
  • C29H27F3N6O2CH4O3S
  • Inhibitors