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GZD 824

GZD 824 Structure
CAS No.
1257628-77-5
Chemical Name:
GZD 824
Synonyms
GZD824;GZD8824;GZD-824;GZD 824;GZD-824 Free;Olverembatinib;GZD 824 USP/EP/BP;GZD824;GZD-824;GZD 824;Olverembatinib (GZD824);GZD-824; GZD 824;BENZAMIDE
CBNumber:
CB82666626
Molecular Formula:
C29H27F3N6O
Molecular Weight:
532.56
MOL File:
1257628-77-5.mol
MSDS File:
SDS
Modify Date:
2024/7/2 8:55:20

GZD 824 Properties

Boiling point 630.4±55.0 °C(Predicted)
Density 1.39±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : ≥ 100 mg/mL (187.77 mM)
form A crystalline solid
pka 9.04±0.40(Predicted)
color Off-white to yellow

GZD 824 Chemical Properties,Uses,Production

Description

GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively). It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.

Uses

GZD824 is a orally bioavailable inhibitor that targets phosphorylated and non-phosphorylated Breakpoint Cluster Region-Abelson (Bcr-Abl) kinases. It is a COVID19-related research product.

Definition

GZD 824 (Olverembatinib), another third-generation BCR-ABL tyrosine kinase inhibitor (TKI), was approved in 2021 in China for patients with T315I positive chronic phase chronic myeloid leukemia (CML-CP) or accelerated-phase CML (CML-AP). Like ponatinib, olverembatinib inhibits multikinases, including B-RAF, DDR1, FGFR, Flt3, KIT, PDGFRα/β, RET, and SRC.

General Description

Class: non-receptor tyrosine kinase
Treatment: CML
Elimination half-life = 17.5–36.5 h

target

BCR-ABL

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GZD 824 Spectrum

4-Methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamide 3-(2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide GZD8824 GZD824;GZD-824;GZD 824 GZD-824 Free GZD 824 GZD824 GZD-824 GZD-824; GZD 824;BENZAMIDE Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]- GZD 824 USP/EP/BP 3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide Olverembatinib Olverembatinib (GZD824) 3-[(1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]benzamide 4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-3-(2-{1H-pyrazolo[3,4-b]pyridin-5-yl}ethynyl)benzamide 1257628-77-5 257628-77-5 Inhibitors