Flezurafenib (JZP-815) is a selective RAF kinase inhibitor designed to target tumors with dysregulated RAS-RAF-MEK-ERK signaling. Preclinical studies have shown that Flezurafenib potently inhibits the kinase activity of both wild-type and mutant forms of BRAF and CRAF, with IC₅₀ values in the low nanomolar range (typically <10 nM for BRAF^V600E). In cellular models, it effectively suppressed ERK phosphorylation and inhibited proliferation in RAS- or BRAF-mutant cancer cell lines, particularly those with KRAS G12C and NRAS mutations. In vivo, Flezurafenib demonstrated strong tumor regression in xenograft models harboring KRAS- or BRAF-driven tumors, supporting its development in cancers with MAPK pathway activation
MedKoo Cat#: 126505
Name: Flezurafenib
CAS#: 2760321-00-2
Chemical Formula: C26H21FN4O3
Exact Mass: 456.1598
Molecular Weight: 456.48
Elemental Analysis: C, 68.41; H, 4.64; F, 4.16; N, 12.27; O, 10.51
The following data is based on the product molecular weight 456.48 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 |
