RGNCY-0042 (SAR405, VPS34 inhibitor )

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SAR405 is a low molecular mass kinase inhibitor of VPS34 (KD 1.5nM) and has a highly selective protein and lipid kinase profile.  Inhibition of VPS34 kinase activity by SAR405 affects both late endosome-lysome compartments and prevents autophagy.  In addition, the concomitant inhibition of VSP34 and mTOR with SAR405 and the US FDA approved mTOR inhibitor, Everolimus, results in synergistic anti-proliferative activity in renal cancer cell lines, indicating a potential clinical application in cancer.  VSP34 IC50 = 1.2nM.

SMILES: C[C@H](COCC1)N1C(N=C2N3CC[C@@H](C(F)(F)F)N2CC4=CN=CC(Cl)=C4)=CC3=O

Systematic Name: (S)-9-((5-chloropyridin-3-yl)methyl)-2-((R)-3-methylmorpholino)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one

Molecular Weight: 443.86

Formula: C19H21ClF3N5O2

PMID: 25326666

Reference: A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy.  Ronan B, Flamand O, et al. Nat Chem Biol.10(12):1013-9 (2014).

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