| Name | PRN1371 |
| Description | PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R). |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 12 mg/mL (21.37 mM), Sonication and heating are recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.56 mM), Sonication is recommended.
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| Keywords | PRN-1371 | PRN1371 | PRN 1371 | Inhibitor | inhibit | Fibroblast growth factor receptor | FGFR4 | FGFR3 | FGFR2 | FGFR1 | FGFR | CSF-1R | CSF1R | CSF-1 receptor | colony stimulating factor 1 receptor | c-Fms | cFms |
| Inhibitors Related | Amlexanox | Regorafenib monohydrate | Nintedanib | PLX5622 | Ferulic Acid | Pexidartinib | Nintedanib esylate | Regorafenib | Formononetin | Lenvatinib mesylate | Lenvatinib | Pazopanib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
