GZD824(Benzamide)|cas 1257628-77-5|DC Chemicals

Cas No.:	1257628-77-5
Chemical Name:	Olverembatinib (GZD824)
Synonyms:	GZD824;3-(2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide;GZD-824
SMILES:	O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(C#CC4=CN=C(NN=C5)C5=C4)=C3
Formula:	C₂₉H₂₇F₃N₆O
M.Wt:	532.22
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. IC50 Value: 0.34/0.68 nM(Bce-Abl wt/T315I) [1]Target: Bcr-Abl in vitro: GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. It also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy.in vivo: GZD824 induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT) or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I) [1]. Clinical trial: GZD824 is on the way of unknown clinical status.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

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