LY-900009Potent Notch inhibitor CAS# 209984-68-9 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 209984-68-9 | SDF | Download SDF |
| PubChem ID | 57327010 | Appearance | Powder |
| Formula | C23H27N3O4 | M.Wt | 409.48 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO mg/mL Water mg/mL Ethanol mg/mL | ||
| Chemical Name | (2S)-2-hydroxy-3-methyl-N-[(2S)-1-[[(7S)-5-methyl-6-oxo-7H-benzo[d][1]benzazepin-7-yl]amino]-1-oxopropan-2-yl]butanamide | ||
| SMILES | CC(C)C(C(=O)NC(C)C(=O)NC1C2=CC=CC=C2C3=CC=CC=C3N(C1=O)C)O | ||
| Standard InChIKey | JURYTIUJMYPBNN-GKCIPKSASA-N | ||
| Standard InChI | InChI=1S/C23H27N3O4/c1-13(2)20(27)22(29)24-14(3)21(28)25-19-17-11-6-5-9-15(17)16-10-7-8-12-18(16)26(4)23(19)30/h5-14,19-20,27H,1-4H3,(H,24,29)(H,25,28)/t14-,19-,20-/m0/s1 | ||
| 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 | LY-900009 is a potent inhibitor of Notch with IC50 value of 0.27 nM. | |||||
| Targets | Notch | |||||
| IC50 | 0.27 nM | |||||
LY-900009 Dilution Calculator
LY-900009 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4421 mL | 12.2106 mL | 24.4212 mL | 48.8424 mL | 61.053 mL |
| 5 mM | 0.4884 mL | 2.4421 mL | 4.8842 mL | 9.7685 mL | 12.2106 mL |
| 10 mM | 0.2442 mL | 1.2211 mL | 2.4421 mL | 4.8842 mL | 6.1053 mL |
| 50 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 0.9768 mL | 1.2211 mL |
| 100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.4884 mL | 0.6105 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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LY-900009 is a selective small-molecule inhibitor of γ-secretase with IC50 value of 0.27nM [1].
Notch signaling plays a critical role in stem cell function and is deragulated in different forms of cancer. Γ-secretase cleaves Notch receptor and regulates its signaling. LY-900009 is an oral notch inhibitor for the treatment of cancer but is now terminated in Phase I [2].
The phase I study shows that LY900009 causes adverse events including diarrhea, vomiting, nausea, fatigue, anorexia, hypophosphatemia and rash at different grades. Treatment of 60mg LY900009 shows dose-limiting toxicities of fatigue and diarrhea respectively in 2 patients. The maximum tolerated dose (MTD) of LY900009 is identified at 30mg. And the elimination half-life is about 2-3 hrs. As a γ-secretase inhibitor, LY900009 also decreases plasma levels of amyloid-β in a dose-dependent manner [3].
References:
[1] Warren J. Porter. Discovery of a Novel Notch Inhibitor. The 8th SCI-RSC symposium on proteinase inhibitor design. April 15-16, 2013.
[2] Williams R. Discontinued drugs in 2012: oncology drugs. Expert Opin Investig Drugs. 2013 Dec;22(12):1627-44.
[3] Shubham Pant, Suzanne Fields Jones, Carla Kurkjian et al. A first-in-human phase I study of the oral Notch inhibitor LY900009 in patients with advanced cancer. ASCO Annual Meeting. 2012
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