(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
SAR405
CAS: 1523406-39-4
Molecular Formula: C19H21ClF3N5O2
(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 - Names and Identifiers
(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 - Physico-chemical Properties
| Molecular Formula | C19H21ClF3N5O2 |
| Molar Mass | 443.85 |
| Density | 1.51±0.1 g/cm3(Predicted) |
| Boling Point | 526.5±60.0 °C(Predicted) |
| Solubility | DMSO: 27 mg/mL |
| pKa | 3.29±0.20(Predicted) |
| Storage Condition | -20℃ |
| Use | 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. |
| Target | Vps34; Autophagy; |
| In vitro study | SAR405 is a highly specific inhibitor of Vps34 with low selectivity for other protein kinases and phosphoinositide kinases. In the human recombinant Vps34 phosphorylated PtdIns substrate, the IC50 of SAR405 was 1 nM. Its binding equilibrium constant Kd is 1.52±0.77 nM (S. D.), dissociation rate constant K off is 3.03±0.55 10. |
(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 - Reference
| Reference Show more | 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. |
(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 - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
(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 - Reference Information
| biological activity | SAR405 is a low molecular weight PIK3C3/Vps34 inhibitor (Kd = 1.5 nM), with high selectivity, in the concentration of up to 10 M, there is no activity on the class I and II PI3Ks and mTOR. SAR405 prevents autophagy and acts synergistically with the inhibition of MTOR (mechanistic target of rapamycin) in tumor cells. |
| Target | Value |
| Vps34 | 1.2 nM |
Last Update：2024-04-09 15:16:56
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Product Name: SAR405 Visit Supplier Webpage Request for quotationCAS: 1523406-39-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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