| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P408403-1ml |
1ml |
现货  |
|
| 别名 | 普拉替尼 (BLU-667) |
|---|---|
| 英文别名 | CS 3009, Gavreto | Cyclohexanecarboxamide, N-[(1S)-1-[6-(4-fluoro-1H-pyrazol-1-yl)-3-pyridinyl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]-, cis- |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Pralsetinib (BLU-667) |
| 生化机理 | Pralsetinib（BLU-667，CS 3009，Gavreto）是一种高效选择性 RET（c-RET）抑制剂，对 WT RET 的 IC50 为 0.4 nM。它对常见的致癌 RET 改变（包括 RET (M918T)）也有很强的活性（IC50 0.4 nmol/L）。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 激酶插入域受体抑制剂；ret 原癌基因抑制剂 |
| 产品介绍 |
Pralsetinib (Blu667) 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。 Information Pralsetinib (BLU-667) Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, incl BLU-667 is at least 100-fold more selective for RET over 96% of kinases tested (a panel of 371 kinases). BLU-667 specifically abrogates RET signaling in RET-altered cancers from diverse lineages. RET pathway inhibition with BLU-667 also more potently inhibits proliferation of RET-altered cell lines relative to multikinase inhibitors. In vivo In vivo, BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2. BLU-667 is well tolerated throughout the in vivo studies. cell lines： Concentrations：0-1 μM Incubation Time：90 minutes Powder Purity:≥98% |
| 分子量 | 533.6 |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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