RGNCY-0023 (CCT241161, pan RAF/SFK inhibitor)
Another member of the series of orally available pan-RAF/SFK inhibitor is active against treatment-naive BRAF and NRAS mutant tumors. It is active in tumors from patients who developed resistance to BRAF-selective inhibitors and a BRAF plus MEK inhibitor combination. This compound series could provide a first-line therapy for treatment naïve patients and a 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 0.03μM and 0.01μM for BRAF kinase and SRC kinase respectively.
Systematic Name: 1-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-(methylthio)-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl)oxy)phenyl)urea
Molecular Weight: 541.63
PubMed Ref.: 25500121
Reference: 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.
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Tags: Cancer, Kinase, Melanoma, Src, SFK, RAF, Tumor, BRAF, NRAS, MEK, RGNCY-0023, CCT241161