中文名 | SAR405 |
英文名 | SAR405 |
别名 | SAR405游离态 化合物SAR405 PIK3C3和VPS34抑制剂(SAR405) |
英文别名 | SAR405 CS-2552 SAR-405 SAR 405 (S)-1-((5-Chloropyridin-3-yl)methyl)-8-((R)-3-methylmorpholino)-2-(trifluoromethyl)-3,4-dihydr (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 (8S)-9-[(5-Chloro-3-pyridinyl)methyl]-6,7,8,9-tetrahydro-2-[(3R)-3-methyl-4-morpholinyl]-8-(trifluoromethyl)-4H-pyrimido[1,2-a]pyrimidin-4-one 4H-Pyrimido[1,2-a]pyrimidin-4-one, 9-[(5-chloro-3-pyridinyl)methyl]-6,7,8,9-tetrahydro-2-[(3R)-3-methyl-4-morpholinyl]-8-(trifluoromethyl)-, (8S)- |
CAS | 1523406-39-4 |
化学式 | C19H21ClF3N5O2 |
分子量 | 443.85 |
密度 | 1.51±0.1 g/cm3(Predicted) |
沸点 | 526.5±60.0 °C(Predicted) |
溶解度 | DMSO: 27 mg/mL |
酸度系数 | 3.29±0.20(Predicted) |
存储条件 | -20℃ |
靶点 | Vps34; Autophagy; |
体外研究 | SAR405是Vps34的高特异性抑制剂,对其他蛋白激酶和磷酸肌醇激酶选择性低。在人重组Vps34磷酸化PtdIns底物中,SAR405的IC50为1 nM。它的结合平衡常数Kd为1.52 ± 0.77 nM (± s.d.)、解离速率常数K off 为3.03 ± 0.55 10。 |
参考资料 展开查看 | 1: Pasquier B. SAR405, a PIK3C3/Vps34 inhibitor that prevents autophagy andsynergizes with MTOR inhibition in tumor cells. Autophagy. 2015 Apr3;11(4):725-6. doi: 10.1080/15548627.2015.1033601. PubMed PMID: 25905679; PubMedCentral PMCID: PMC4502822. 2: Marsh T, Debnath J. Ironing out VPS34 inhibition. Nat Cell Biol. 2015Jan;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 andselective Vps34 inhibitor alters vesicle trafficking and autophagy. Nat ChemBiol. 2014 Dec;10(12):1013-9. doi: 10.1038/nchembio.1681. Epub 2014 Oct 19.PubMed PMID: 25326666. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.253 ml | 11.265 ml | 22.53 ml |
5 mM | 0.451 ml | 2.253 ml | 4.506 ml |
10 mM | 0.225 ml | 1.127 ml | 2.253 ml |
5 mM | 0.045 ml | 0.225 ml | 0.451 ml |
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