RGNCY-0022 (CCT196969, pan RAF/SFK inhibitor)

IN STOCK!!  E-mail us at info@reagency.co if you are interested in this product.

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.


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

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.

Data Sheet


Interested in this reagent? E-mail us at info@reagency.co and let us know.

Tags: Cancer, Kinase, Melanoma, Src, SFK, RAF, Tumor, RGNCY-0022, CCT196969, BRAF, NRAS, MEK