Belvarafenib, also known as GDC-5573, HM95573, RG6185, is a selective inhibitor of the RAF family kinases designed to inhibit the MAPK pathway, which is frequently activated in human tumors and drives tumor growth. ARAF mutants conferred resistance to belvarafenib in both a dimer- and a kinase activity-dependent manner. Belvarafenib induced ARAF mutant dimers, and dimers containing mutant ARAF were active in the presence of inhibitor. ARAF mutations may serve as a general resistance mechanism for RAF dimer inhibitors as the mutants exhibit reduced sensitivity to a panel of type II RAF inhibitors.
MedKoo Cat#: 561840
Name: Belvarafenib
CAS#: 1446113-23-0 (free base)
Chemical Formula: C23H16ClFN6OS
Exact Mass: 478.0779
Molecular Weight: 478.93
Elemental Analysis: C, 57.68; H, 3.37; Cl, 7.40; F, 3.97; N, 17.55; O, 3.34; S, 6.69
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.2 | 96.40 | |
| DMSO:PBS (pH 7.2) (1:2) | 0.3 | 0.69 | |
| DMF | 30.0 | 62.64 |
The following data is based on the product molecular weight 478.93 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 |
