中文名称 | 4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-3-[2-(1H-吡唑并[3,4-b]吡啶-5-基)乙炔基]苯甲酰胺 | 耐克替尼 | 奥雷巴替尼 |
---|---|
英文名称 | Olverembatinib (GZD824; HQP1351) |
CAS号 | 1257628-77-5 |
分子式 | C29H27F3N6O |
分子量 | 532.56 |
外观 | Off-white to yellow powder |
储存条件 | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
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.
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).
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