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Pralsetinib

CAS No. : 2097132-94-8

產品活性：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 IC₅₀s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively.

研究領域：Protein Tyrosine Kinase/RTK

作用靶點：RET

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).

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.

相關產品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Drug Repurposing Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Lung Cancer Compound Library  |  Targeted Therapy Drug Library   |  Anti-Liver Cancer Compound Library   |  Rare Diseases Drug Library  |  FDA-Approved Anticancer Drug Library  |  Heterocyclic Compound Library  |  Withdrawn Drug Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  trans-Pralsetinib  |  BT-13  |  RET-IN-16  |  WF-47-JS03  |  Pyrazoloadenine  |  GSK3179106  |  RET-IN-1  |  Lenvatinib-d₅  |  Pz-1  |  Regorafenib monohydrate  |  RET-IN-14  |  AD57  |  AD80  |  FLT3/ITD-IN-4  |  RET-IN-18  |  Regorafenib-¹³C,d₃  |  RET V804M-IN-1  |  RET-IN-19  |  Enbezotinib  |  RET-IN-6  |  BT44  |  TG101209  |  Regorafenib-d₃  |  Amuvatinib  |  WHI-P180  |  RET-IN-10  |  Zeteletinib

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