Uplarafenib (also known as B-Raf IN 10) is a potent small-molecule inhibitor targeting the RAF kinase family, with a particular emphasis on BRAF and its oncogenic mutants. According to the IUPHAR/BPS Guide to PHARMACOLOGY, uplarafenib exhibits inhibitory activity across a spectrum of kinases, including ARAF, BRAF (wild-type and mutants such as V600E and V600E/T529I), CRAF-1, FAK, FGFR1-4, JNK1-13, Lck, Lyn, MET, PIM1-3, PYK2, KDR, SRC, and RET, demonstrating picomolar to nanomolar potencies . In vitro studies have shown that uplarafenib achieves over 89% inhibition of BRAF and BRAF V600E at a concentration of 1 μM, with IC₅₀ values ranging between 50–100 nM for BRAF and less than 50 nM for BRAF V600E . Functionally, uplarafenib suppresses the proliferation of melanoma cell lines A375 and SK-MEL-28, both harboring BRAF V600E mutations, with IC₅₀ values below 500 nM, while showing minimal activity against BRAF wild-type lines such as CHL-1 and SK-MEL-31 .
MedKoo Cat#: 140256
Name: Uplarafenib
CAS#: 1425485-87-5
Chemical Formula: C22H21F3N4O4S
Exact Mass: 494.1236
Molecular Weight: 494.49
Elemental Analysis: C, 53.44; H, 4.28; F, 11.53; N, 11.33; O, 12.94; S, 6.48
The following data is based on the product molecular weight 494.49 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 |
