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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

作用靶点：FGFR  |  c-Fms

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 K_d>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 (t_1/2=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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