产品名称

SAR405

产品货号

Axon 2716 CAS [1523406-39-4] MF C19H21ClF3N5O2MW 443.85 Purity: 98% Optical purity: >99% ee Soluble in DMSO Description SAR405 is a potent kinase inhibitor of PI3K class III (PIK3C3), highly specific on VPS34 (with IC50 value of 1 nM and Kd value of 1.5 nM for PIK3C3/VPS34). This compound has an exquisite protein and lipid kinase selectivity profile that is explained by its unique binding mode and molecular interactions within the ATP binding cleft of human Vps34. Inhibition of Vps34 kinase activity by SAR405 affects both late endosome-lysosome compartments and prevents autophagy. Concomitant inhibition of Vps34 and mTOR, with SAR405 and mTOR inhibitor everolimus, results in synergistic antiproliferative activity in renal tumor cell lines. KEYWORDS: SAR405 | VPS34 inhibitor | PI3K inhibitor | SAR 405 | SAR-405 | CAS [1523406-39-4] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes | Vsp34 | PI3K(class III) | Autophagy | PIK3C3 | Kinase

产品价格

现货询价，电话：010-67529703

产品规格

产品品牌

axonmedchem

产品概述

产品详情

SAR405

Based on 8 reference(s) in Google Scholar 9 10 8

Axon 2716

CAS [1523406-39-4]

MF C19H21ClF3N5O2
MW 443.85

Purity: 98%
Optical purity: >99% ee
Soluble in DMSO

SAR405

Description

SAR405 is a potent kinase inhibitor of PI3K class III (PIK3C3), highly specific on VPS34 (with IC50 value of 1 nM and Kd value of 1.5 nM for PIK3C3/VPS34). This compound has an exquisite protein and lipid kinase selectivity profile that is explained by its unique binding mode and molecular interactions within the ATP binding cleft of human Vps34. Inhibition of Vps34 kinase activity by SAR405 affects both late endosome-lysosome compartments and prevents autophagy. Concomitant inhibition of Vps34 and mTOR, with SAR405 and mTOR inhibitor everolimus, results in synergistic antiproliferative activity in renal tumor cell lines.

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

B Pasquier. SAR405, a PIK3C3/Vps34 inhibitor that prevents autophagy and synergizes with MTOR inhibition in tumor cells. Autophagy. 2015 Apr 3;11(4):725-6.

PIK3C3/Vps34 inhibitor

Chemical name

(S)-1-((5-Chloropyridin-3-yl)methyl)-8-((R)-3-methylmorpholino)-2-(trifluoromethyl)-3,4-dihydro-1H-pyrimido[1,2-a]pyrimidin-6(2H)-one

Parent CAS No.

[1523406-39-4]

产品资料