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MedKoo CAT#: 407111
Description: Olverembatinib, also known as GZD824, is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I. GZD824 tightly bound to Bcr-Abl(WT) and Bcr-Abl(T315I) with K(d) values of 0.32 and 0.71 nM, respectively, and strongly inhibited the kinase functions with nanomolar IC(50) values. 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. GZD824 also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy. It 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). GZD824 represents a promising lead candidate for development of Bcr-Abl inhibitors to overcome acquired imatinib resistance. (J Med Chem. 2013 Feb 14;56(3):879-94)
MedKoo Cat#: 407111
Name: Olverembatinib (GZD824)
Chemical Formula: C29H27F3N6O
Exact Mass: 532.21984
Molecular Weight: 532.22
Elemental Analysis: C, 65.40; H, 5.11; F, 10.70; N, 15.78; O, 3.00
Related CAS #: 1257628-77-5
Synonym: GZD824; GZD 824; GZD-824; Olverembatinib;
IUPAC/Chemical Name: 3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide
InChi Key: TZKBVRDEOITLRB-UHFFFAOYSA-N
InChi Code: InChI=1S/C29H27F3N6O/c1-19-3-5-22(14-21(19)6-4-20-13-24-17-34-36-27(24)33-16-20)28(39)35-25-8-7-23(26(15-25)29(30,31)32)18-38-11-9-37(2)10-12-38/h3,5,7-8,13-17H,9-12,18H2,1-2H3,(H,35,39)(H,33,34,36)
SMILES Code: CC1=CC=C(C=C1C#CC2=CN=C3C(C=NN3)=C2)C(NC4=CC=C(C(C(F)(F)F)=C4)CN5CCN(CC5)C)=O
1: Ren X, Pan X, Zhang Z, Wang D, Lu X, Li Y, Wen D, Long H, Luo J, Feng Y, Zhuang X, Zhang F, Liu J, Leng F, Lang X, Bai Y, She M, Tu Z, Pan J, Ding K. 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 Feb 14;56(3):879-94. doi: 10.1021/jm301581y. Epub 2013 Jan 28. PubMed PMID: 23301703.