1421783-64-3

1421783-64-3 - Names and Identifiers

Name	GZD824
Synonyms	GZD824 CS-1086 GZD824DIMESYLATE GZD824 GZD824DIMESYLATE GSK-3 INHIBITOR IX, 6-BROMOINDIRUBIN-3-OXIME, 6-BROMOINDIRUBIN-3'-OXIME, MLS 2052 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 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
CAS	1421783-64-3

1421783-64-3 - Physico-chemical Properties

Molecular Formula	C31H35F3N6O7S2
Molar Mass	724.7708096
In vitro study	GZD824 effectively inhibited the growth of cells expressing wild-type BCR-ABL Ba/F3 with an IC50 of 1.0 nM. In high agreement with biochemical kinase inhibition and protein binding affinity assay results, GZD824 also strongly inhibited the proliferation of Ba/F3 cells expressing the Bcr-AblT315I mutant and 14 resistance-associated BCR-ABL mutants. In addition, in K562 leukemia cells, GZD824 efficiently inhibited BCR-ABL and downstream CRKL and STAT5 activation in a concentration-dependent manner. GZD824 effectively inhibited the growth of cells expressing wild-type BCR-ABL Ba/F3 with an IC50 of 1.0 nM. In high agreement with biochemical kinase inhibition and protein binding affinity assay results, GZD824 also strongly inhibited the proliferation of Ba/F3 cells expressing the Bcr-AblT315I mutant and 14 resistance-associated BCR-ABL mutants. In addition, in K562 leukemia cells, GZD824 efficiently inhibited BCR-ABL and downstream CRKL and STAT5 activation in a concentration-dependent manner.
In vivo study	In the K562 tumor xenograft and KU812 xenograft models, GZD824(5 and 10 mg/kg/day) dose-dependently inhibited tumor growth and there was no mortality or loss of body weight. In addition, GZD824(20 mg/kg/day) inhibited tumor growth in Allograft mice expressing Bcr-AblWT and BCR-AblT315I Ba/F3 cells. In the K562 tumor xenograft and KU812 xenograft models, GZD824(5 and 10 mg/kg/day) dose-dependently inhibited tumor growth, and there was no death or weight loss. In addition, GZD824(20 mg/kg/day) inhibited tumor growth in Allograft mice expressing Bcr-AblWT and BCR-AblT315I Ba/F3 cells.

1421783-64-3 - Introduction

GZD824 is an organic compound with the chemical name GZD824 chloride dimesylate. Its molecular formula is C34H36ClN7O9S2 and its molecular weight is 777.31g/mol. GZD824 is a multi-targeted tyrosine kinase inhibitor with anti-tumor activity. It can inhibit the growth and spread of tumor cells by inhibiting the activity of a variety of target tyrosine kinases.

The preparation method of GZD824 mainly includes chemical synthesis and purification process. During the chemical synthesis, GZD824 chloride was first synthesized and then reacted with dimethanesulfonic acid to produce gzd824. Finally, after purification and crystallization steps, pure GZD824 was obtained.

As for safety information, GZD824 is a laboratory-prepared compound, so there is no extensive toxicological and safety data. Appropriate laboratory practices, such as wearing protective gloves, glasses, and respiratory equipment outside the laboratory, should be used and handled with the compound. At the same time, direct contact with the skin and inhalation of its particles should be avoided during operation.

In summary, GZD824 is a multi-targeted tyrosine kinase inhibitor with anti-tumor activity. It can be prepared by chemical synthesis and purification methods, and its toxicological and safety data need to be further studied and evaluated. Appropriate laboratory safety measures need to be taken during operation.

Last Update：2024-04-10 22:29:15