Pralsetinib
作者：齐岳
发布时间：2023-09-07
09:26:02
点击数：
产品名称：Pralsetinib
产品描述：
| 产品描述 | Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion). |
| 靶点活性 | RET V804L:0.3 nM, RET V804M:0.4 nM, RET M918T:0.4 nM, Wild type RET:0.4 nM, CCDC6-RET:0.4 nM |
| 体外活性 | Pralsetinib demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants. Pralsetinib 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 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). |
| 体内活性 | Pralsetinib potently inhibits the growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR-2. Pralsetinib 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. |
| 别名 | Blu667, 普拉替尼 |
| 分子量 | 533.6 |
| 分子式 | C27H30FN9O2 |
| CAS No. | 2097132-94-8 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 95 mg/mL (178.04 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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