PRN1371

SKU: orb1296270

Description

PRN1371 is a potent small molecule inhibitor targeting FGFR1-4 and CSF1R with low nanomolar IC50 values. It is a valuable research tool for studying oncogenic signaling and tumor microenvironment dynamics in both cellular assays and in vivo cancer models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1802929-43-6
• MW: 561.46
• Purity: 99.72% (May vary between batches)
• Formula: C₂₆H₃₀Cl₂N₆O₄
• SMILES: CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCN3CCN(CC3)C(=O)C=C)c2n1
• Target: c-Fms,FGFR,CSF-1R
• Solubility: DMSO:12 mg/mL (21.37 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.56 mM)

Bioactivity

• Target IC50:
  FGFR1:0.6 nM (IC50)|CSF1R:8.1 nM (IC50)|FGFR3:4.1 nM (IC50)|FGFR4:19.3 nM (IC50)|FGFR2:1.3 nM (IC50)
• In Vivo:
  In PK studies of rat, dog, and cynomolgus monkey, PRN1371show rapid iv clearance in all species. PRN1371 shows rapid clearance (Cl=160 mL per min per kg), yet dosing p.o (20 mg/kg) demonstrates high oral exposure (AUC=4348 h·ng/mL) and a reasonable half-life (t1/2=3.8 h). Low levels of pFGFR2 confirm the ability of PRN1371 to block FGFR2 activity in tumor tissue. PRN1371 induces a dose-dependent reduction in tumor volume and up to 68% tumor growth inhibition at the highest dose of 10 mg/kg b.i.d. following 27 days of treatment. All doses are well tolerated with no significant bodyweight loss.
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• In Vitro:
  PRN1371 exhibits high biochemical and cellular potency (FGFR1 IC50: 0.6 nM, SNU16 IC50: 2.6 nM), sustained target engagement (FGFR1 occupancy 24 h = 96%), less than 30% hERG inhibition at 1 μM, and favorable predicted ADME stability with BME reactivity Kd > 100 μM.
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Storage & Handling

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

Alternative Names

PRN1371, PRN-1371, PRN 1371, inhibit, Inhibitor, FGFR1, FGFR2, FGFR3, FGFR4, Fibroblast growth factor receptor, FGFR, CSF-1 receptor, CSF1R, CSF-1R, colony stimulating factor 1 receptor, cFms, c-Fms

Compound Identifiers

PubChem CID

118295624