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Pralsetinib

Catalog No. TQ0277 CAS 2097132-94-8

Synonyms: Blu667

Pralsetinib (Blu667) (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).

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Pralsetinib, CAS 2097132-94-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 51.00
5 mg	In stock	$ 105.00
10 mg	In stock	$ 148.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 558.00
100 mg	In stock	$ 785.00
1 mL * 10 mM (in DMSO)	In stock	$ 123.00

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Purity: 98.1%

Purity: 97.88%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pralsetinib (Blu667) (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).
Targets&IC50	CCDC6-RET:0.4 nM, RET (WT):0.4 nM, RET (M918T):0.4 nM, RET (V804M):0.4 nM, RET (V804L):0.3 nM
In vitro	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).
In vivo	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.

Synonyms	Blu667
Molecular Weight	533.6
Formula	C27H32FN9O2
CAS No.	2097132-94-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (178.04 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library EMA Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Inhibitor Library Bioactive Compounds Library Max Anti-Lung Cancer Compound Library

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Cabozantinib TPX-0046 JNJ-38158471 Agerafenib DUN73423 Selpercatinib Vepafestinib WHI-P180

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pralsetinib 2097132-94-8 Apoptosis Tyrosine Kinase/Adaptors c-RET Inhibitor BLU 667 BLU-667 Blu667 inhibit RET inhibitor

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