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+86 137 2013 4139
| CAS: | 1257628-77-5 | Cat No: | JKN00201 | Purity: | 98% |
Note: All products of the company are for scientific research only, and do not provide products and services for any individual
Product Description
| CAS | 1257628-77-5 | Cat No | JKN00201 | |
| Name | Olverembatinib | |||
| Synonyms | GZD-824 | |||
| Smiles | 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 | |||
| 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 | |||
| Formula | C29H27F3N6O | MWt | 532.22 | |
| Purity | 98% | Storage | Store at 4--8℃ | |
| 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). | |||
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