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PRN1371

PRN1371
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Purity:99.72%
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PRN1371

Catalog No. TQ0015Cas No. 1802929-43-6
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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$74In Stock
2 mg$107In Stock
5 mg$178In Stock
10 mg$322In Stock
25 mg$547In Stock
50 mg$788In Stock
100 mg$1,080In Stock
1 mL x 10 mM (in DMSO)$223In Stock
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Product Introduction

Bioactivity
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 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.
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.
Chemical Properties
Molecular Weight561.46
FormulaC26H30Cl2N6O4
Cas No.1802929-43-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 12 mg/mL (21.38 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7811 mL8.9054 mL17.8107 mL89.0535 mL
5 mM0.3562 mL1.7811 mL3.5621 mL17.8107 mL
10 mM0.1781 mL0.8905 mL1.7811 mL8.9054 mL
20 mM0.0891 mL0.4453 mL0.8905 mL4.4527 mL

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