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Pralsetinib

(Synonyms: 普拉替尼; BLU-667)

目录号: PL10969 纯度: ≥99%

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。

CAS No. :2097132-94-8

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中文名称	Pralsetinib
中文别名	BLU-667;普拉替尼
英文名称	Pralsetinib
英文别名	BLU-667;Pralsetinib;Blu667;trans-Pralsetinib;Pralsetinib free base;1WPE73O1WV;BLU123244;X581238;cis-Pralsetinib;cis-N-{(1S)-1-[6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethyl}-1-methoxy-4-{4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl}cyclohexane-1-carboxamide;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-;cy;N-[(1S)-1-[6-(4-fluoropyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide
Cas No.	2097132-94-8
分子式	C₂₇H₃₂FN₉O₂
分子量	533.60
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	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。

产品详情

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。

生物活性

Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC 50 s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 0.4 nM (Wild type RET), 0.3 nM (RET V804L), 0.4 nM (RET V804M), 0.4 nM (RET M918T), 0.4 nM (CCDC6-RET)

体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Subbiah V, et al. Precision Targeted Therapy With BLU-667 for RET-Driven Cancers. American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (187.41 mM)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. Subbiah V, et al. Precision Targeted Therapy With BLU-667 for RET-Driven Cancers. American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Pralsetinib

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