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ChemicalBook--->CAS DataBase List--->1257628-77-5

1257628-77-5

1257628-77-5 Structure

1257628-77-5 Structure
IdentificationBack Directory
[Name]

GZD 824
[CAS]

1257628-77-5
[Synonyms]

GZD824
GZD-824
GZD8824
GZD 824
GZD-824 Free
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
[Molecular Formula]

C29H27F3N6O
[MDL Number]

MFCD26142930
[MOL File]

1257628-77-5.mol
[Molecular Weight]

532.559
Chemical PropertiesBack Directory
[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
Hazard InformationBack Directory
[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
Spectrum DetailBack Directory
[Spectrum Detail]

GZD 824(1257628-77-5)1HNMR
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