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LEE011

(CAS: 1211441-98-3)

Suppliers of LEE011

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AOBIOUS INC [email protected] (508) 306-0937 USA

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AbMole BioScience [email protected] 1-800-660-8580 USA

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Adipogen Corporation [email protected] (858) 457-8383 USA

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AdooQ BioScience, LLC [email protected] 855-GO-ADOOQ (855-462-3667) (US & Canada Toll Free) 866-930-6790 (US & Canada Toll Free) +1-323-389-9269 (Outside of US & Canada) USA

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

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Axon Medchem BV [email protected];[email protected] +31 50 3118007 Netherlands

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

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BioVision, Inc., [email protected] 408-493-1800 Toll Free: 800-891-9699 (US Only) USA

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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: USD72/5mg () USD96/10mg ()

Cayman Chemical Company [email protected] Toll Free (USA and Canada Only): (800) 364-9897; Direct: (734) 971-3335;Technical Support Toll Free (USA and Canada Only): (888) 526-5351;Technical Support Direct: (734) 975-3888 USA

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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: USD72/5mg () USD96/10mg ()
Quality Control & MSDS Files: LCMS HNMR MSDS

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

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Quality Control & MSDS Files: CoA MSDS HNMR HPLC MS

Pure Chemistry Scientific Inc. [email protected] 857-928-2050 / 857-366-6788 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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Target Molecule Corp. [email protected] (857) 239-0968 USA

Fax: 857-239-8801Purity: .98 Brand: TargetMol

Price and Availability: USD45/2mg () USD90/5mg () USD165/10mg () USD268/25mg () USD448/50mg ()

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Background Information of LEE011

LEE011 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

Solubility Sources
DMSO MedChemexpress Co., Ltd.
Soluble in DMSO, not in water MedKoo Biosciences, Inc.

Storage Condition of LEE011

Storage Condition Sources
Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. MedKoo Biosciences, Inc.

MSDS Information

MSDS Sources
MedChemexpress Co., Ltd.
MedKoo Biosciences, Inc.

Quality Control and Spectral Data

QC Reports Sources
[LCMS] [HNMR] MedChemexpress Co., Ltd.
[CoA] [HNMR] [HPLC] [MS] MedKoo Biosciences, Inc.

Mechanism and Indications

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications Breast tumor Stage IV melanoma Metastatic breast cancer Melanoma

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
LEE011 Novartis AG Breast tumor 2013/10/31 2014/4/30 Phase 2 Clinical
LEE011 Novartis AG Stage IV melanoma 2013/9/30 2016/10/31 Phase 2 Clinical
LEE011 Novartis AG Metastatic breast cancer 2013/10/31 2016/4/30 Phase 2 Clinical
LEE011 Novartis AG Metastatic breast cancer 2013/9/30 2016/6/30 Phase 2 Clinical
LEE011 Novartis AG Melanoma 2013/4/30 2015/4/30 Phase 2 Clinical
LEE011 - Launched

Chemical Information

M.Wt Formula CAS No. Synonyms
434.54 C23H30N8O 1211441-98-3 LEE 011;LEE-011; 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide

Structure Information of LEE011

Smiles O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5
InChI InChI=1S/C23H30N8O/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/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28)

Related Products

Other Form Products of LEE011

Name CAS Formula Suppliers
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 8
LEE011 (succinate) 1374639-75-4 C27H36N8O5 9
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 8

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AMG 925 1401033-86-0 C26H29N7O2 15
LDC000067 1073485-20-7 C18H18N4O3S 11
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 8
LEE011 (succinate) 1374639-75-4 C27H36N8O5 9
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 8
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
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Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 16
Purvalanol B 212844-54-7 C20H25ClN6O3 22
NU6102 444722-95-6 C18H22N6O3S 8

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Name CAS Formula Suppliers
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MLN4924 905579-51-3 C21H25N5O4S 16
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SB-590885 405554-55-4 C27H27N5O2 18
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Cyclophosphamide 50-18-0 C7H15Cl2N2O2P 19
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Retaspimycin 857402-23-4 C31H45N3O8 9
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Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 20
Litronesib 910634-41-2 C23H37N5O4S2 7
Veliparib 912444-00-9 C13H16N4O 11
Veliparib (dihydrochloride) 912445-05-7 C13H18Cl2N4O 8
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Ixabepilone 219989-84-1 C27H42N2O5S 19

Chemical and Physical Properties

Appearance:Light yellow to yellow Solid Melting point:
Boiling point: Flash Point:
Water Solubility: Solubility:In vitro:DMSO,7 mg/mL(16.1 mM);In vitro:Water,Insoluble;In vitro:Ethanol,Insoluble;
Density: Merck:
BRN: Refractive Index:
Vapour: EINECS:
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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