LEE011 succinate hydrateCDK inhibitor CAS# 1374639-79-8 |
- Anguizole
Catalog No.:BCC1365
CAS No.:442666-98-0
- Asunaprevir (BMS-650032)
Catalog No.:BCC1374
CAS No.:630420-16-5
- Balapiravir
Catalog No.:BCC1396
CAS No.:690270-29-2
Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| 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. |
||
| 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. |
||
| 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: | |||||
Cell Assay
[2]
Cells are grown for 24 hours in 35 mm plates, treated with 500 nM LEE011 for 6 days, and then fixed and stained overnight. Cells are then imaged for SA-β-gal using an Axio Observer D.1 phase contrast microscope. The percentage of SA-β-gal positive cells is determined by counting the number of positive cells present in three separate microscope frames, and then normalizing to the control. To assess apoptotic activity, cells are plated in triplicate in 96 well plates, treated with LEE011, and assayed for caspase 3/7 activation 16 hours after treatment with Caspase-Glo 3/7. Cells treated with SN-38 are used as a positive control[2].
Animal Administration
[2]
Mice[2] The BE2C, NB-1643, or EBC1 cell line-derived xenografts are implanted subcutaneously into the right flank of CB17 SCID-/- mice. Animals bearing engrafted tumors of 200-600 mm3 are then randomized to oral treatment with 200 mg/kg LEE011 in 0.5 % methylcellulose (n=10) or vehicle (n=10) daily for a total of 21 days. Tumor burden is determined periodically throughout treatment according to the formula (π/6)×d2, where d represents the mean tumor diameter obtained by caliper measurement.
References:
[1]. VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10.
[2]. Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.
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. | |||||
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
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.
- LEE011 succinate
Catalog No.:BCC4102
CAS No.:1374639-75-4
- BRD4770
Catalog No.:BCC5525
CAS No.:1374601-40-7
- TUG 891
Catalog No.:BCC6235
CAS No.:1374516-07-0
- LY 235959
Catalog No.:BCC6892
CAS No.:137433-06-8
- 15,16-Epoxy-15-ethoxy-6beta,13-dihydroxylabd-8-en-7-one
Catalog No.:BCN7428
CAS No.:1374328-47-8
- Diacerein
Catalog No.:BCN2291
CAS No.:13739-02-1
- Spathulatol
Catalog No.:BCN6877
CAS No.:1373888-27-7
- PF-5274857
Catalog No.:BCC3838
CAS No.:1373615-35-0
- Nω-Propyl-L-arginine hydrochloride
Catalog No.:BCC6965
CAS No.:137361-05-8
- GSK J4 HCl
Catalog No.:BCC2230
CAS No.:1373423-53-0
- GSK J1
Catalog No.:BCC2231
CAS No.:1373422-53-7
- Boc-Val-OH
Catalog No.:BCC3465
CAS No.:13734-41-3
- CO-1686 (AVL-301)
Catalog No.:BCC1490
CAS No.:1374640-70-6
- Rhapontisterone
Catalog No.:BCC8245
CAS No.:137476-71-2
- GNE0877
Catalog No.:BCC5369
CAS No.:1374828-69-9
- Regiolone
Catalog No.:BCN7193
CAS No.:137494-04-3
- 1-Benzoylpiperazine
Catalog No.:BCC8456
CAS No.:13754-38-6
- Poricoic acid A(F)
Catalog No.:BCN3741
CAS No.:137551-38-3
- Poricoic acid B
Catalog No.:BCN8260
CAS No.:137551-39-4
- VT-464 racemate
Catalog No.:BCC5399
CAS No.:1375603-36-3
- [Lys5,MeLeu9,Nle10]-NKA(4-10)
Catalog No.:BCC5994
CAS No.:137565-28-7
- Taxifolin 7-O-rhamnoside
Catalog No.:BCN6851
CAS No.:137592-12-2
- Bisindolylmaleimide II
Catalog No.:BCC7868
CAS No.:137592-45-1
- GR 64349
Catalog No.:BCC5800
CAS No.:137593-52-3
