PRN-1371 is an irreversible covalent pan-FGFR inhibitor (IC50s = 0.7, 1.3, 4.4, and 19.3 nM for FGFR-1, -2, -3, and -4, respectively). It is selective for FGFR over VEGFR2 (IC50 = 705 nM) and a panel of 250 kinases (IC50s = >1 µM for all) but does inhibit colony stimulating factor 1 receptor (CSF1R) activity by greater than 90% at 1 µM. PRN-1371 inhibits proliferation in a panel of ten cancer cell lines containing various FGFR mutants (IC50s = 2-231 nM) and induces apoptosis in SNU-16 gastric and RT4 bladder cancer cells (EC50s = 15.9 and 11.8 nM, respectively). It reduces tumor growth in an SNU-16 mouse xenograft model and a patient-derived xenograft (PDX) mouse model of liver cancer when administered at a dose of 15 mg/kg twice per day.
MedKoo Cat#: 206849
Name: PRN-1371
CAS#: 1802929-43-6
Chemical Formula: C26H30Cl2N6O4
Exact Mass: 560.1706
Molecular Weight: 561.46
Elemental Analysis: C, 55.62; H, 5.39; Cl, 12.63; N, 14.97; O, 11.40
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMSO | 15.0 | 26.00 |
The following data is based on the product molecular weight 561.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
