Agerafenib (also known as RXDX-105, CEP-32496, and AC013773) is an orally bioavailable, ATP-competitive pan-RAF inhibitor with selective activity against wild-type BRAF, CRAF, and certain oncogenic BRAF fusions, while sparing BRAF V600E. In preclinical studies, agerafenib exhibited potent inhibition of RAF1 and BRAF with IC₅₀ values of 0.3 nM and 0.4 nM, respectively, and demonstrated submicromolar antiproliferative effects in cancer cell lines harboring RET fusions and BRAF fusions (IC₅₀s typically < 100 nM). In xenograft models, RXDX-105 significantly suppressed tumor growth in RET- and BRAF-fusion-positive tumors with minimal activity in BRAF V600E-driven tumors, aligning with its unique kinase selectivity profile.
MedKoo Cat#: 205903
Name: RXDX-105 (CEP-32496)
CAS#: 1188910-76-0 (free base)
Chemical Formula: C24H22F3N5O5
Exact Mass: 517.1573
Molecular Weight: 517.47
Elemental Analysis: C, 55.71; H, 4.29; F, 11.01; N, 13.53; O, 15.46
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.0 | 38.65 | |
| DMF | 10.0 | 19.32 | |
| Ethanol | 2.0 | 3.86 |
The following data is based on the product molecular weight 517.47 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 |
