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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $74 | In Stock | |
2 mg | $107 | In Stock | |
5 mg | $178 | In Stock | |
10 mg | $322 | In Stock | |
25 mg | $547 | In Stock | |
50 mg | $788 | In Stock | |
100 mg | $1,080 | In Stock | |
1 mL x 10 mM (in DMSO) | $223 | In Stock |
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. |
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) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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