Pralsetinib

SKU: orb1296082

Description

Pralsetinib (BLU-667) is a potent and selective RET kinase inhibitor effective against wild-type RET, multiple mutants (V804L, V804M, M918T), and the CCDC6-RET fusion. It is a valuable research tool for investigating RET-driven pathologies, with demonstrated activity in both cellular assays and in vivo models of RET-altered cancers.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2097132-94-8
• MW: 533.6
• Purity: 99.89% (May vary between batches)
• Formula: C₂₇H₃₂FN₉O₂
• SMILES: CO[C@]1(CC[C@@H](CC1)c1nc(C)cc(Nc2cc(C)[nH]n2)n1)C(=O)N[C@@H](C)c1ccc(nc1)-n1cc(F)cn1
• Target: c-RET
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.18 mM);DMSO:126.25 mg/mL (236.6 mM)

Bioactivity

• Target IC50:
  CCDC6-RET:0.4 nM|RET (M918T):0.4 nM|RET (WT):0.4 nM|RET (V804M):0.4 nM|RET (V804L):0.3 nM
• 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.
  Read more...
• 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).
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, cRET, Blu667, BLU-667, BLU 667, Pralsetinib, RET

Compound Identifiers

PubChem CID

129073603