CCT196969 pan RAF/SFK inhibitor RGNCY-0022
Per 10 mg
This orally available pan-RAF/SFK inhibitor is active against treatment-naive BRAF and NRAS mutant tumors. It is also active in tumors from patients who developed resistance to BRAF-selective inhibitors and a BRAF plus MEK inhibitor combination. Such compounds could provide first-line therapy for treatment naïve patients and second-line therapy for a range of patients with relapsed melanoma. Phase 1 clinical trials will commence in 2015 with this series of compounds. IC50 0.1μM and 0.03μM for BRAF kinase and SRC kinase respectively.
Girotti, Maria Romina, et al. "Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma." Cancer cell 27.1 (2015): 85-96.