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LEE011 (succinate hydrate)

(CAS: 1374639-79-8)

Suppliers of LEE011 (succinate hydrate)

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Ark Pharm, Inc. [email protected] +1 (847) 367-3680 USA

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BOC Sciences [email protected] 1-631-504-6093

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Biochempartner Co., Ltd [email protected] 0086-13720134139; 0086-15971444841 China

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CHEMSCENE, LLC [email protected] 732-484-9848 USA

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Price and Availability: USD60/5mg () USD84/10mg ()

DC Chemicals [email protected]; [email protected] +86-21-58447131 China

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Lancrix Chemicals. [email protected] 86 21 50817262 China

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MedChemexpress Co., Ltd. [email protected] 609-228-6898 USA

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Price and Availability: USD60/5mg () USD84/10mg ()
Quality Control & MSDS Files: NP-HPLC HNMR MSDS

Shanghai Haoyuan Chemexpress Co., Ltd. [email protected] +86 (21) 5187-0955 / +86 (21) 5895-5995 China

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Price and Availability: USD60/5mg () USD84/10mg ()

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Background Information of LEE011 (succinate hydrate)

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.

Solubility of LEE011 (succinate hydrate)

Solubility Sources
DMSO MedChemexpress Co., Ltd.

Storage Condition of LEE011 (succinate hydrate)

Storage Condition Sources

MSDS Information

MSDS Sources
MedChemexpress Co., Ltd.

Quality Control and Spectral Data

QC Reports Sources
[NP-HPLC] [HNMR] MedChemexpress Co., Ltd.

Mechanism and Indications

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications Breast tumor Melanoma

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
LEE011 (succinate hydrate) Novartis AG Breast tumor 2013/10/31 2014/4/30 Phase 2 Clinical
LEE011 (succinate hydrate) Novartis AG Melanoma 2013/4/30 2015/4/30 Phase 2 Clinical
LEE011 (succinate hydrate) - Launched

Chemical Information

M.Wt Formula CAS No. Synonyms
570.64 C27H38N8O6X 1374639-79-8 LEE 011 succinate hydrate;LEE-011 succinate hydrate;

Structure Information of LEE011 (succinate hydrate)

Smiles O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5.OC(CCC(O)=O)=O.[F,Cl,Br,I].O
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

Related Products

Other Form Products of LEE011 (succinate hydrate)

Name CAS Formula Suppliers
LEE011 (succinate) 1374639-75-4 C27H36N8O5 9
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 8
LEE011 1211441-98-3 C23H30N8O 21

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LEE011 (succinate) 1374639-75-4 C27H36N8O5 9
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Chemical and Physical Properties

Appearance: Melting point:
Boiling point: Flash Point:
Water Solubility: Solubility:
Density: Merck:
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Optical Rotation: alpha:

Reference

[1].Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Oct 28.
PURPOSE: Neuroblastoma is a pediatric cancer that continues to exact significant morbidity and mortality. Recently, a number of cell-cycle proteins, particularly those within the Cyclin D/CDK4/CDK6/RB network, have been shown to exert oncogenic roles in neuroblastoma, suggesting that their therapeutic exploitation might improve patient outcomes. Experimental Procedures: We evaluated the effect of dual CDK4/CDK6 inhibition on neuroblastoma viability using LEE011 (Novartis Oncology), a highly specific CDK4/6 inhibitor. RESULTS: Treatment with LEE011 significantly reduced proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis at nanomolar concentrations (mean IC50 = 307 ± 68 nmol/L in sensitive lines). LEE011 caused cell-cycle arrest and cellular senescence that was attributed to dose-dependent decreases in phosphorylated RB and FOXM1, respectively. In addition, responsiveness of neuroblastoma xenografts to LEE011 translated to the in vivo setting in that there was a direct correlation of in vitro IC50 values with degree of subcutaneous xenograft growth delay. Although our data indicate that neuroblastomas sensitive to LEE011 were more likely to contain genomic amplification of MYCN (P = 0.01), the identification of additional clinically accessible biomarkers is of high importance. CONCLUSIONS: Taken together, our data show that LEE011 is active in a large subset of neuroblastoma cell line and xenograft models, and supports the clinical development of this CDK4/6 inhibitor as a therapy for patients with this disease. Clin Cancer Res; 19(22); 6173-82. ?2013 AACR.

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