LEE011 succinate hydrateCDK inhibitor CAS# 1374639-79-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1374639-79-8 | SDF | Download SDF |
| PubChem ID | 127255617 | Appearance | Powder |
| Formula | C27H38N8O6 | M.Wt | 570.64 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Ribociclib succinate hydrate | ||
| Solubility | DMSO : ≥ 19 mg/mL (33.30 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | butanedioic acid;7-cyclopentyl-N,N-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide;hydrate | ||
| SMILES | CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5.C(CC(=O)O)C(=O)O.O | ||
| Standard InChIKey | PZJOFPMHNJJJSC-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H30N8O.C4H6O4.H2O/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30;5-3(6)1-2-4(7)8;/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28);1-2H2,(H,5,6)(H,7,8);1H2 | ||
| 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 | LEE011 succinate hydrate is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.In Vitro:Treating a panel of 17 neuroblastoma cell lines with LEE011 (Ribociclib) across a four-log dose range (10 to 10,000 nM). Treatment with LEE011 significantly inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. LEE011 treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at LEE011 concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively[2].In Vivo:CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with LEE011 (200 mg/kg) or with a vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models. Tumor growth is significantly delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment[2]. References: | |||||
LEE011 succinate hydrate Dilution Calculator
LEE011 succinate hydrate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.7524 mL | 8.7621 mL | 17.5242 mL | 35.0484 mL | 43.8105 mL |
| 5 mM | 0.3505 mL | 1.7524 mL | 3.5048 mL | 7.0097 mL | 8.7621 mL |
| 10 mM | 0.1752 mL | 0.8762 mL | 1.7524 mL | 3.5048 mL | 4.381 mL |
| 50 mM | 0.035 mL | 0.1752 mL | 0.3505 mL | 0.701 mL | 0.8762 mL |
| 100 mM | 0.0175 mL | 0.0876 mL | 0.1752 mL | 0.3505 mL | 0.4381 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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LEE011 succinate hydrate is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.
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