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PRN1371

Catalog No. TQ0015 CAS 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).

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PRN1371, CAS 1802929-43-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 74.00
2 mg	In stock	$ 107.00
5 mg	In stock	$ 178.00
10 mg	In stock	$ 322.00
25 mg	In stock	$ 547.00
50 mg	In stock	$ 788.00
100 mg	In stock	$ 1,080.00
1 mL * 10 mM (in DMSO)	In stock	$ 223.00

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Purity: 99.72%

Biological Description

Chemical Properties

Storage & Solubility Information

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	FGFR4:19.3 nM (IC50), FGFR3:4.1 nM (IC50), CSF1R:8.1 nM (IC50), FGFR1:0.6 nM (IC50), FGFR2:1.3 nM (IC50)
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.

Molecular Weight	561.46
Formula	C26H30Cl2N6O4
CAS No.	1802929-43-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12 mg/mL (21.38 mM), Sonication and heating are recommended.

References and Literature

1. Brameld KA, et al. Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. J Med Chem. 2017 Aug 10;60(15):6516-6527.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Bioactive Compound Library Covalent Inhibitor Library

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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.

Keywords

PRN1371 1802929-43-6 Angiogenesis Tyrosine Kinase/Adaptors c-Fms FGFR CSF-1R PRN 1371 inhibit CSF1R Inhibitor colony stimulating factor 1 receptor PRN-1371 CSF-1 receptor Fibroblast growth factor receptor inhibitor

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