Olverembatinib (Synonyms: GZD824; HQP1351) |
カタログ番号GC62207 |
オルベレンマチニブ (GZD824) は、経口で有効な強力な汎 Bcr-Abl 阻害剤です。オルベレンマチニブは、広範囲の Bcr-Abl 変異体を強力に阻害します。オルベレンマチニブは、天然の Bcr-Abl および Bcr-AblT315I をそれぞれ 0.34 nM および 0.68 nM の IC50 で強力に阻害します。オルベレンマチニブには抗腫瘍活性があります。
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Cas No.: 1257628-77-5
Sample solution is provided at 25 µL, 10mM.
GZD824 (HQP1351) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity[1].
GZD824 shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants[1].GZD824 selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells[1].GZD824 inhibits Bcr-Abl signaling in K562 (1-20 nM; 4.0 hours) and Ba/F3 stable cell lines expressing native Bcr-Abl (0.1-100 nM; 4.0 hours) or Bcr-AblT315I(0.1-100 nM; 4.0 hours)[1].
GZD824 suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl WT[1].GZD824 (1-20 mg/kg; i.g.; daily; for 10 days) significantly increases the median survival of the mice bearing allografted Ba/F3 cells expressing Bcr-AblT315I[1].GZD824 exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg)[1].GZD824 exhibits terminal elimination half-lives (rat 5.6 h) due to high plasma clearance (rat 1.7 L/h/kg) following intravenous administration (rat 5 mg/kg)[1].
[1]. Ren X, Pan X, Zhang Z, 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.
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