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CAS No. : 2376047-73-1
MCE 国际站:SIAIS178
产品活性:SIAIS178 是一种 PROTAC 类的有效的,选择性的 BCR-ABL 降解剂,IC50 为 24 nM。SIAIS178 通过募集 Von Hippel-Lindau (VHL) E3 泛素连接酶来降解 BCR-ABL 蛋白。SIAIS178 具有抗肿瘤活性。
研究领域:PROTAC | Protein Tyrosine Kinase/RTK
作用靶点:PROTACs | Bcr-Abl
In Vitro: SIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner. SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5.
SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines.
In Vivo: SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement .
SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.
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