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
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
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.
N-Bromosuccinimide Price
- Product number
- G932000
- Product name
- GZD824
- Packaging
- 5mg
- Price
- $175
- Updated
- 2021/12/16
- Product number
- G932000
- Product name
- GZD824
- Packaging
- 25mg
- Price
- $605
- Updated
- 2021/12/16
- Product number
- B1402
- Product name
- GZD824
- Packaging
- 25mg
- Price
- $360
- Updated
- 2021/12/16
- Product number
- CS-0020021
- Product name
- GZD824(dimesylate)
- Purity
- 99.20%
- Packaging
- 10mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- B1402
- Product name
- GZD824
- Packaging
- 5mg
- Price
- $115
- Updated
- 2021/12/16
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
GZD824 Suppliers
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- 17752881701
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- 021-50323701
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- Country
- United States
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View Lastest Price from GZD824 manufacturers
- 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