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Pralsetinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pralsetinib图片
CAS NO:2097132-94-8
包装与价格:
包装价格(元)
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品名称
普拉替尼
BLU667
产品介绍
Pralsetinib 是高效的、选择性的RET抑制剂。它能够抑制 WT RET (IC50:0.4 nM),RET 突变体 V804L (IC50:0.3 nM),V804M (IC50:0.4 nM),M918T (IC50:0.4 nM) 和 CCDC6-RET (IC50:0.4 nM) 的融合。

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).

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.

Cas No.

2097132-94-8

分子式

C27H32FN9O2

分子量

533.6

别名

普拉替尼;Blu667

储存和溶解度

DMSO:95 mg/mL (178.04 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years