Molecular Weight(MW): 434.54
Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
Cited by 7 Publications
4 Customer Reviews
IB analysis of whole cell lysates derived from mouse CT26 or 4T1 tumor cell lines treated with or without the CDK4/6 inhibitor, ribociclib.
Nature, 2017, 553(7686):91-95. Ribociclib (LEE011) purchased from Selleck.
(B) The effects of AZD2014, BEZ235, lapatinib, LEE011, pazopanib on PI3K/AKT signaling in sarcoma PDC line were determined by immunoblotting analysis. Cells were treated with 1 μM of the indicated drugs for 72 h.
Transl Oncol, 2016, 9(3):197-202.. Ribociclib (LEE011) purchased from Selleck.
Analysis of apoptosis in leukemia cells induced by LEE011. Annexin V staining of cells following 48-h treatment with LEE011 at 2 or 5 µM compared with DMSO controls. Following 5-µM LEE011 treatment, the K562 apoptotic cell percentage was 5.9 ± 0.75 vs. 1.2 ± 0.66% for the DMSO group, P = 0.001; in MV4-11 cells, the apoptotic cell percentage was 24.2 ± 3.06 vs. 0.53 ± 0.40% for the DMSO group, P = 0.005; in U937 cells, the apoptotic cell percentage was 9.9 ± 2.81 vs. 0.57 ± 0.42% for the DMSO group, P = 0.027; in HL-60 cells, the apoptotic cell percentage was 28.23 ± 6.01 vs. 0.9 ± 0.8% for the DMSO group, P = 0.015; in THP-1 cells, the apoptotic cell percentage was 1.76 ± 0.4 vs. 1.56 ± 0.45% for the DMSO group, P = 0.59; in CCRF cells, the apoptotic cell percentage was 13.77 ± 3.16 vs. 1.2 ± 0.36% for the DMSO group, P = 0.019; in NB4 cells, the apoptotic cell percentage was 12.1 ± 1.35 vs. 0.86 ± 0.25% for the DMSO group, P = 0.004; and in SHI-1 cells the apoptotic cell percentage was 12.6 ± 2.81 vs. 1.87 ± 0.75% for the DMSO group, P = 0.017. These analyses were repeated three times. *P < 0.05; **P < 0.01
Cancer Cell Int, 2017, 17:35. Ribociclib (LEE011) purchased from Selleck.
Purity & Quality Control
Choose Selective CDK Inhibitors
|Description||Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.|
|Features||Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.|
LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence. 
|In vivo||LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity. |
|In vitro||DMSO||7 mg/mL (16.1 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03701334||Not yet recruiting||Early Breast Cancer||Novartis Pharmaceuticals|Translational Research in Oncology|Novartis||December 27 2018||Phase 3|
|NCT03740334||Not yet recruiting||Acute Lymphoblastic Leukemia ALL||Dana-Farber Cancer Institute|Novartis||November 30 2018||Phase 1|
|NCT03673124||Not yet recruiting||Low Grade Serous Carcinoma||Gynecologic Oncology Group|Novartis||November 30 2018||Phase 2|
|NCT03613220||Not yet recruiting||HR+ HER2 Breast Cancer||Novartis Pharmaceuticals|Novartis||October 30 2018||Phase 2|
|NCT03671330||Recruiting||Breast Cancer||Novartis Pharmaceuticals|Novartis||August 29 2018||Phase 2|
|NCT03477396||Active not recruiting||Estrogen Receptor and/or Progesterone Receptor Positive|HER2/Neu Negative|Stage IV Breast Cancer AJCC v6 and v7||City of Hope Medical Center|National Cancer Institute (NCI)||June 14 2018||Phase 2|
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