| Name | Pralsetinib |
| 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). |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.18 mM), Sonication is recommended.
DMSO : 126.25 mg/mL (236.6 mM), Sonication is recommended.
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| Keywords | RET | Pralsetinib | Inhibitor | inhibit | cRET | BLU-667 | BLU 667 |
| Inhibitors Related | Regorafenib monohydrate | Regorafenib Hydrochloride | KBP-7018 | TG-89 | Tafetinib | Regorafenib | DUN73423 | AST 487 | Amuvatinib | Lenvatinib mesylate | Lenvatinib | Selpercatinib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Kinase Inhibitor Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
