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MedKoo CAT#: 406844
CAS#: 1523406-39-4
Description: SAR-405 is a potent and selective PIK3C3/Vps34 inhibitor that prevents autophagy and synergizes with MTOR inhibition in tumor cells. SAR405 treatment also inhibits autophagy induced either by starvation or by MTOR (mechanistic target of rapamycin) inhibition. Combining SAR405 with everolimus results in a significant synergy on the reduction of cell proliferation using renal tumor cells.
MedKoo Cat#: 406844
Name: SAR-405
CAS#: 1523406-39-4
Chemical Formula: C19H21ClF3N5O2
Exact Mass: 443.1336
Molecular Weight: 443.8552
Elemental Analysis: C, 51.42; H, 4.77; Cl, 7.99; F, 12.84; N, 15.78; O, 7.21
Synonym: SAR-405; SAR 405; SAR405.
IUPAC/Chemical 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
InChi Key: SPDQRCUBFSRAFI-DOMZBBRYSA-N
InChi Code: InChI=1S/C19H21ClF3N5O2/c1-12-11-30-5-4-26(12)16-7-17(29)27-3-2-15(19(21,22)23)28(18(27)25-16)10-13-6-14(20)9-24-8-13/h6-9,12,15H,2-5,10-11H2,1H3/t12-,15+/m1/s1
SMILES Code: O=C1C=C(N2[C@H](C)COCC2)N=C3N(CC4=CC(Cl)=CN=C4)[C@H](C(F)(F)F)CCN31
1: Pasquier B. SAR405, a PIK3C3/Vps34 inhibitor that prevents autophagy and
synergizes with MTOR inhibition in tumor cells. Autophagy. 2015 Apr
3;11(4):725-6. doi: 10.1080/15548627.2015.1033601. PubMed PMID: 25905679; PubMed
Central PMCID: PMC4502822.
2: Marsh T, Debnath J. Ironing out VPS34 inhibition. Nat Cell Biol. 2015
Jan;17(1):1-3. PubMed PMID: 25679028.
3: Ronan B, Flamand O, Vescovi L, Dureuil C, Durand L, Fassy F, Bachelot MF,
Lamberton A, Mathieu M, Bertrand T, Marquette JP, El-Ahmad Y, Filoche-Romme B,
Schio L, Garcia-Echeverria C, Goulaouic H, Pasquier B. A highly potent and
selective Vps34 inhibitor alters vesicle trafficking and autophagy. Nat Chem
Biol. 2014 Dec;10(12):1013-9. doi: 10.1038/nchembio.1681. Epub 2014 Oct 19.
PubMed PMID: 25326666.