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Pralsetinib
CAS No. : 2097132-94-8
MCE 国际站：Pralsetinib
产品活性：Pralsetinib (BLU-667) 是一种高效的选择性 RET 抑制剂。Pralsetinib (BLU-667) 抑制 WT RET，RET 突变体 V804L，V804M，M918T 和 CCDC6-RET 融合，IC50 分别为 0.4、0.3、0.4、0.4、0.4 nM。
研究领域：Protein Tyrosine Kinase/RTK
作用靶点：RET
In Vitro: Pralsetinib (BLU-667) demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants.
?Pralsetinib (BLU-667) demonstrates potent activity (IC50=0.4 nM) against common oncogenic RET alterations, including RET M918T, an activating mutation found in MTC, as well as the CCDC6-RET fusion observed in PTC and NSCLC.
?Pralsetinib (BLU-667) suppresses RET pathway signaling in a panel of RET-driven cell lines: LC2/ad (CCDC6-RET, NSCLC), MZ-CRC-1 (RET M918T, MTC), and TT (RET C634W, MTC).
In Vivo: Pralsetinib (BLU-667) potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2).
?Pralsetinib (BLU-667) shows dose dependent activity against both KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors with doses as low as 10 mg/kg twice-daily.
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