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LEE011 (succinate)

(CAS: 1374639-75-4)

Suppliers of LEE011 (succinate)

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Apexbio Technology LLC [email protected] +1-832-696-8203 USA

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Price and Availability: USD238/5mg (Ship Within 10-14 Days)

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

Fax: Purity: 0.98 Brand: Biochempartner

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

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

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

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

MedKoo Biosciences, Inc. [email protected] 919-279-0682 USA

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Santa Cruz Biotechnology, Inc. [email protected] Toll Free: 800-457-3801 Phone: 214-902-3900 USA

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

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Background Information of LEE011 (succinate)

LEE011 succinate 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)

Solubility Sources
DMSO MedChemexpress Co., Ltd.

Storage Condition of LEE011 (succinate)

Storage Condition Sources

MSDS Information

MSDS Sources
MedChemexpress Co., Ltd.

Quality Control and Spectral Data

QC Reports Sources
[HNMR] [NP-HPLC] 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) Novartis AG Breast tumor 2013/10/31 2014/4/30 Phase 2 Clinical
LEE011 (succinate) Novartis AG Melanoma 2013/4/30 2015/4/30 Phase 2 Clinical
LEE011 (succinate) - Launched

Chemical Information

M.Wt Formula CAS No. Synonyms
552.63 C27H36N8O5 1374639-75-4 LEE 011 succinate;LEE-011 succinate; 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate

Structure Information of LEE011 (succinate)

Smiles O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5.OC(CCC(O)=O)=O
InChI InChI=1S/C23H30N8O.C4H6O4/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)

Related Products

Other Form Products of LEE011 (succinate)

Name CAS Formula Suppliers
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 8
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 8
LEE011 1211441-98-3 C23H30N8O 21

Recommended Products in Same Target

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LDC000067 1073485-20-7 C18H18N4O3S 11
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 8
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 8
LEE011 1211441-98-3 C23H30N8O 21
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 6
Wogonin 632-85-9 C16H12O5 28
1-NM-PP1 221244-14-0 C20H21N5 17
WHI-P180 211555-08-7 C16H15N3O3 13
THZ1 1604810-83-4 C31H28ClN7O2 18
Senexin A 1366002-50-7 C17H14N4 8
CDK4-IN-1 1256963-02-6 C22H29ClN8 9
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 16
Purvalanol B 212844-54-7 C20H25ClN6O3 22
NU6102 444722-95-6 C18H22N6O3S 8

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MLN4924 905579-51-3 C21H25N5O4S 16
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Veliparib 912444-00-9 C13H16N4O 11
Veliparib (dihydrochloride) 912445-05-7 C13H18Cl2N4O 8
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Reparixin 266359-83-5 C14H21NO3S 9
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Carboplatin 41575-94-4 C6H12N2O4Pt 29
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SU14813 (maleate) 849643-15-8 C27H31FN4O8 8
5-Fluorouracil 51-21-8 C4H3FN2O2 31

Chemical and Physical Properties

Appearance:Light yellow to yellow Solid Melting point:
Boiling point: Flash Point:
Water Solubility: Solubility:Soluble in DMSO
Density: Merck:
BRN: Refractive Index:
Vapour: EINECS:
Optical Rotation: alpha:


[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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