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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.
Product Information
RGNCY-0022 Product Information
SMILES: CC(C)C)C1=NN(C2=CC=CC=C2)C(NC(NC(C(F)=C3)
=CC=C3OC4=C5C(NC(C=N5)=O)=NC=C4)=O)=C1
Formula: C27H24FN7O3
Systematic Name: 1-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-fluoro-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl)oxy)phenyl)urea
Molecular Weight: 513.53
PubMed Ref.: 25500121
References: 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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Please visit their website to see the current batch of cutting-edge compounds. If you don’t see what you want, submit a request and they will add it to their site and offer it to the Reagency community so everyone can share the cost of synthesis.
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