Products

CCT196969 pan RAF/SFK inhibitor RGNCY-0022

$320.00 (AUD)
Per 10 mg

802M 7d

Formula

Small Molecule

Tags

Small molecules Cancer Melanoma SFK

Description

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.






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.

Uploaded Files

RGNCY-0022 Product Information.pdf