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GNF-7
CAS No. : 839706-07-9
MCE 国际站：GNF-7
产品活性：GNF-7 是一种多重激酶抑制剂。GNF-7 是 Bcr-Abl 的抑制剂，对 Bcr-AblWT 和 Bcr-AblT315I 作用的 IC50 值分别为 133 nM 和 61 nM。GNF-7 对 ACK1 和 GCK 也具有抑制活性，IC50 分别为 25 nM 和 8 nM。GNF-7 可用于血液恶性肿瘤的研究。
研究领域：Protein Tyrosine Kinase/RTK
In Vitro: GNF-7 potently inhibits wild-type Bcr-Abl (IC50<5 nM) and Bcr-Abl mutants such as T315I (IC50=11 nM), G250E (IC50<5 nM), E255V (IC50=10 nM), F317L (IC50<5 nM) and M351T (IC50<5 nM) in cellular assays.
?GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream.
?GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines.
In Vivo: GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model.
?GNF-7 exhibits moderate oral bioavailability (mice 36%) and Cmax (mice 3616 nM) following oral administration (mice 20 mg/kg).
?GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg)?? following intravenous injection (mice 5 mg/kg).
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