SRT1720 HClSIRT1 activator CAS# 1001645-58-4 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 1001645-58-4 | SDF | Download SDF |
| PubChem ID | 25232708 | Appearance | Powder |
| Formula | C25H24ClN7OS | M.Wt | 506.02 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | SRT1720 | ||
| Solubility | Soluble in DMSO > 10 mM | ||
| Chemical Name | N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]quinoxaline-2-carboxamide;hydrochloride | ||
| SMILES | C1CN(CCN1)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=NC6=CC=CC=C6N=C5.Cl | ||
| Standard InChIKey | DTGRRMPPXCRRIM-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C25H23N7OS.ClH/c33-24(22-13-27-20-7-3-4-8-21(20)28-22)29-19-6-2-1-5-18(19)23-15-32-17(16-34-25(32)30-23)14-31-11-9-26-10-12-31;/h1-8,13,15-16,26H,9-12,14H2,(H,29,33);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | SRT1720 is a selective activator of SIRT1 with EC50 of 0.16 μM, but is >230-fold less potent for SIRT2 and SIRT3. | |||||
| Targets | SIRT1 | |||||
| IC50 | 0.16 μM (EC50) | |||||
| Cell experiment: [1] | |
| Cell lines | MDA-MB-231 cells |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reacting condition | Below a concentration of 5 µM, 24h |
| Applications | SRT1720 is a SIRT1 activator. It increased the VEGF concentration by about 30% relative to the control, suggesting that SRT1720 might promote the angiogenesis of tumors. |
| Animal experiment : [1] | |
| Animal models | BALB/c mice (5-week-old females) injected with 4T1 cells |
| Dosage form | From Day 2 before tumor implantation, SRT1720 (100 mg/kg body weight) was given to the mouse 5 times per week. The size of the tumors was measured on Days 4, 8, 12, 16 and 20. The primary tumor was removed on Day 21 and was weighed and frozen at -20˚C. On Day 28, the mice were sacrificed and the lungs were intratracheally fixed with a Bouin's solution for 24 h. |
| Application | SRT1720 did not substantially affect the size and weight of primary tumors, but dramatically increased lung metastasis by about 150%. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Suzuki K, Hayashi R, Ichikawa T, et al. SRT1720, a SIRT1 activator, promotes tumor cell migration, and lung metastasis of breast cancer in mice. Oncology reports, 2012, 27(6): 1726-1732. | |
SRT1720 HCl Dilution Calculator
SRT1720 HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9762 mL | 9.881 mL | 19.7621 mL | 39.5241 mL | 49.4052 mL |
| 5 mM | 0.3952 mL | 1.9762 mL | 3.9524 mL | 7.9048 mL | 9.881 mL |
| 10 mM | 0.1976 mL | 0.9881 mL | 1.9762 mL | 3.9524 mL | 4.9405 mL |
| 50 mM | 0.0395 mL | 0.1976 mL | 0.3952 mL | 0.7905 mL | 0.9881 mL |
| 100 mM | 0.0198 mL | 0.0988 mL | 0.1976 mL | 0.3952 mL | 0.4941 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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SRT1720 is a small-molecule compound which has the ability of activating the sirtuin subtype SIRT1 in vitro. The activity of SRT1720 as a SIRT1 activator is stronger than that of resveratrol. It affects mitochondrial respiration in a Sirt1- and PGC-1α-dependent manner. SRT1720 has been demonstrated to enhance insulin sensitivity and improve measures of mitochondrial capacity and oxidative metabolism. Treatment of multiple myeloma (MM) cells with SRT1720 inhibits growth and induced apoptosis in MM cells resistant to conventional and bortezomib therapies without significantly affecting the viability of normal cells. SRT1720 is able to enhance the cytotoxic activity of bortezomib or dexamethasone. Anti-MM activity of SRT1720 is related to: 1) activation of caspase-8, caspase-9, caspase-3, poly(ADP) ribose polymerase; 2) increase in reactive oxygen species; 3) induction of phosphorylated ataxia telangiectasia mutated/checkpoint kinase 2 signaling; 4) decrease in vascular endothelial growth factor-induced migration of MM cells and associated angiogenesis; and 5) inhibition of nuclear factor-κB.
References
Robin K. Minor, Joseph A. Baur, Ana P. Gomes, Theresa M. Ward, Anna Csiszar, Evi M. Mercken, Kotb Abdelmohsen, Yu-Kyong Shin, Carles Canto, Morten Scheibye-Knudsen, Melissa Krawczyk ,Pablo M. Irusta, Alejandro Martı´n-Montalvo, Basil P. Hubbard, Yongqing Zhang, Elin Lehrmann, Alexa A. White, Nathan L. Price, William R. Swindell, Kevin J. Pearson, Kevin G. Becker, Vilhelm A. Bohr, Myriam Gorospe, Josephine M. Egan, Mark I. Talan, Johan Auwerx, Christoph H. Westphal, James L. Ellis, Zoltan Ungvari, George P. Vlasuk, Peter J. Elliott, David A. Sinclair, Rafael de Cabo. SRT1720 improves survival and healthspan of obese mice. Scientific Reports. 2011; 1(70): 1038 – 1131.
Kensuke Suzuki, Ryuji Hayashi, Tomomi Ichikawa, Shingo Imanishi, Toru Yamada, Minehiko Inomata, Toshiro Miwa, Shoko Matsui, Isao Usui, Masaharu Urakaze, Yuji Matsuya, Hirofumi Ogawa, Hiroaki Sakurai, Ikuo Saiki, Kazuyuki Tobe. SRT1720, a SIRT1 activator, promotes tumor cell migration, and lung metastasis of breast cancer in mice. Oncology reports. 2012; 27: 1726 -1732.
Dharminder Chauhan, Madhavi Bandi, Ajita V. Singh, Arghya Ray, Noopur Raje, Paul Richardson and Kenneth C.Anderson. Preclinical evaluation of a novel SIRT1 modulator SRT1720 in multiple myeloma cells. British Journal of Haematology. 2011; 155: 588–598.
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