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PRN1371

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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).

PRN1371

PRN1371

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Purity: 98.65%
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).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$74In StockIn Stock
2 mg$107In StockIn Stock
5 mg$178In StockIn Stock
10 mg$322In StockIn Stock
25 mg$547In StockIn Stock
50 mg$788In StockIn Stock
100 mg$1,080In StockIn Stock
1 mL x 10 mM (in DMSO)$223In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.65%
Color:White
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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).
Targets&IC50
FGFR3:4.1 nM (IC50), CSF1R:8.1 nM (IC50), FGFR4:19.3 nM (IC50), FGFR2:1.3 nM (IC50), FGFR1:0.6 nM (IC50)
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.
Chemical Properties
Molecular Weight561.46
FormulaC26H30Cl2N6O4
Cas No.1802929-43-6
SmilesCNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCN3CCN(CC3)C(=O)C=C)c2n1
Relative Density.1.341 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 12 mg/mL (21.37 mM), Sonication and heating are recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.56 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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