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PRN1371
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PRN1371
CAS No. : 1802929-43-6
MCE 站:PRN1371
产品活性:PRN1371 是高度选择性和有效的 FGFR1-4 和 CSF1R 抑制剂,对FGFR1,FGFR2,FGFR3,FGFR4 和 CSF1R 的 IC50 值分别为 0.6,1.3,4.1,19.3 和 8.1 nM。
研究领域:Protein Tyrosine Kinase/RTK
In Vitro: PRN1371 presents a unique profile of high biochemical and cellular potency (FGFR1 IC50=0.6 nM, SNU16 IC50=2.6 nM), prolonged target engagement (FGFR1 occupancy 24 h=96%), < 30% hERG inhibition at 1 μM, and good predicted ADME stability with BME reactivity Kd>100 μM. Broader kinome-wide biochemical profiling of PRN1371 against 251 kinases identifies only FGFR1−4 and CSF1R as being potently inhibited.
In Vivo: PK studies of PRN1371 in rat, dog, and cynomolgus monkey show rapid iv clearance in all species. PRN1371 shows rapid clearance (Cl=160 mL per min per kg), yet dosing po (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 confirms 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 body weight loss. PRN1371 free base has been administered orally once daily as powder in a capsule on a 28-day continuous schedule. Human plasma concentrations for doses ranging from 15 to 35 mg confirm good oral exposure, rapid systemic clearance, no accumulation from day 1 to day 15, and a dose-dependent increase in AUC. Serum phosphate, a pharmacodynamic marker of FGFR inhibition, is increased for all doses studied and shows a dose-dependent increase between 20 and 35 mg, despite the administration of prophylactic phosphate binders.
相关产品:Covalent Screening Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Covalent Screening Library | Reprogramming Compound Library | Anti-Lung Cancer Compound Library | SU 5402 | Heparan Sulfate | PD173074 | GW2580 | Gandotinib | Formotin | KW-2449 | Ferulic acid | PD-166866 | CP-547632 | Ki20227 | PP58 | SUN11602 | AZD7507 | R1530 | PLX647 | 2,5-Dihydroxybenzoic acid | Tyrosine kinase-IN-1 | cFMS Receptor Inhibitor II | PD-161570 | ARQ 069 | PD-089828 | SM1-71 | SU4984 | CSF1R-IN-1
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